Dopamine-neurotransmission and nociception in zebrafish: An anti-nociceptive role of dopamine receptor drd2a
Eur J Pharmacol. 2021 Sep 20:174517. doi: 10.1016/j.ejphar.2021.174517. Online ahead of print.ABSTRACTDopamine (DA) is an important modulator in nociception and analgesia. Spinal DA receptors are involved in descending modulation of the nociceptive transmission. Genetic variations within DA neurotransmission have been associated with altered pain sensitivity and development of chronic pain syndromes. The variant rs6277 in dopamine receptor 2 a (drd2a) has been associated with a decreased D2 receptor availability and increased nociception. The aim of this study is to further characterize the role of DA neurotransmission in ...
Source: European Journal of Pharmacology - September 23, 2021 Category: Drugs & Pharmacology Authors: Roel R I van Reij Maud M A Salmans Ivo Eijkenboom Nynke J van den Hoogen Elbert A J Joosten Jo M Vanoevelen Source Type: research

Strategies for active tumor targeting-an update
Eur J Pharmacol. 2021 Sep 20:174512. doi: 10.1016/j.ejphar.2021.174512. Online ahead of print.ABSTRACTA complete cure for cancer is still the holy grail for scientists. The existing treatment of cancer is primarily focused on surgery, radiation and conventional chemotherapy. However, chemotherapeutic agents also affect healthy tissues or organs due to a lack of specificity. While passive targeting is studied for anticancer drugs focused on the enhanced permeability and retention effect, it failed to achieve drug accumulation at the tumor site and desired therapeutic efficacy. This review presents an outline of the current ...
Source: European Journal of Pharmacology - September 23, 2021 Category: Drugs & Pharmacology Authors: Darshan Vyas Mital Patel Sarika Wairkar Source Type: research

Roles of 5-HT < sub > 3 < /sub > and 5-HT < sub > 7 < /sub > receptors in acute pruriceptive processing in mice
Eur J Pharmacol. 2021 Sep 20:174513. doi: 10.1016/j.ejphar.2021.174513. Online ahead of print.ABSTRACTThe roles of serotonin (5-HT) and/or noradrenaline in acute pruriceptive processing have been demonstrated using antidepressants, such as milnacipran, a serotonin and noradrenaline reuptake inhibitor, and mirtazapine, a noradrenergic and specific serotonergic antidepressant; however, the involvement of 5-HT in acute pruriceptive processing has not yet been elucidated in detail. Scratching events induced by chloroquine (CQ) were attenuated by the administration of milnacipran or mirtazapine, and these effects were reversed ...
Source: European Journal of Pharmacology - September 23, 2021 Category: Drugs & Pharmacology Authors: Yu Miyahara Hideki Funahashi Ayaka Haruta-Tsukamoto Yoichiro Kogoh Anna Kanemaru-Kawazoe Toshikazu Nishimori Yasushi Ishida Source Type: research

β1-adrenergic receptor but not β2 mediates osteogenic differentiation of bone marrow mesenchymal stem cells in normotensive and hypertensive rats
In conclusion, ADRB1, but not ADRB2, could be involved in the osteogenic differentiation of BMSCs from Wistar rats and SHRs.The high ADRB1 expression might suppress the effect of ADRB2 on BMSCs.PMID:34555397 | DOI:10.1016/j.ejphar.2021.174515 (Source: European Journal of Pharmacology)
Source: European Journal of Pharmacology - September 23, 2021 Category: Drugs & Pharmacology Authors: Ayn á Emanuelli Alves Barreto Victor Gustavo Balera Brito Mariana Sousa Patrocinio Beatriz Babeto Ballassoni Sabrina Cruz Tfaile Frasnelli Sandra Helena Penha Oliveira Source Type: research

Cardio-protective effect of tetrahydrocurcumin, the primary hydrogenated metabolite of curcumin in vivo and in vitro: Induction of apoptosis and autophagy via PI3K/AKT/mTOR pathways
In conclusion, THC effectively inhibited H/R-induced autophagy and apoptosis via, at least partially, activating the PI3K/AKT/mTOR pathways. THC might have the potential to be further developed into a potential candidate for the treatment of MI/R injury.PMID:34555398 | DOI:10.1016/j.ejphar.2021.174495 (Source: European Journal of Pharmacology)
Source: European Journal of Pharmacology - September 23, 2021 Category: Drugs & Pharmacology Authors: Xiaoying Chen Qingfeng Xie Ying Zhu Jiamin Xu Guoshu Lin Shujun Liu Ziren Su Xiaoping Lai Qian Li Jianhui Xie Xiaobo Yang Source Type: research

Low-intensity pulsed ultrasound prevents angiotensin II-induced aortic smooth muscle cell phenotypic switch via hampering miR-17-5p and enhancing PPAR- γ
Eur J Pharmacol. 2021 Sep 20;911:174509. doi: 10.1016/j.ejphar.2021.174509. Online ahead of print.ABSTRACTVascular events can trigger a pathological phenotypic switch in vascular smooth muscle cells (VSMCs), decreasing and disrupting the plasticity and diversity of vascular networks. The development of novel therapeutic approaches is necessary to prevent these changes. We aimed to investigate the effects and associated mechanisms of low-intensity pulsed ultrasound (LIPUS) irradiation on the angiotensin II (AngII)-induced phenotypic switch in VSMCs. In vivo, AngII was infused subcutaneously for 4 weeks to stimulate vascular...
Source: European Journal of Pharmacology - September 21, 2021 Category: Drugs & Pharmacology Authors: Kun Zhao Tingting Wu Chuanxi Yang Haotian Pan Tianhua Xu Jing Zhang Xiasheng Guo Juan Tu Dong Zhang Xiangqing Kong Bin Zhou Wei Sun Source Type: research

Nectin cell adhesion molecule-4 (NECTIN-4): A potential target for cancer therapy
Eur J Pharmacol. 2021 Sep 18:174516. doi: 10.1016/j.ejphar.2021.174516. Online ahead of print.ABSTRACTNECTIN-4 [a poliovirus receptor-related-4 (pvrl-4) encoded protein] is a Ca2+ independent immunoglobulin-like protein. Along with other Nectins (Nectin-1, -2 and -3), it is primarily involved in cell-cell adhesion. In contrast to other Nectins, Nectin-4 is specifically enriched in the embryonic and placental tissues but its expression significantly declines in adult life. In recent years, it has been found that Nectin-4 is especially overexpressed and served as a tumor associated inducer in various malignant tumors includi...
Source: European Journal of Pharmacology - September 21, 2021 Category: Drugs & Pharmacology Authors: Subhajit Chatterjee Saptarshi Sinha Chanakya Nath Kundu Source Type: research

Pirfenidone is a renal protective drug: Mechanisms, signalling pathways, and preclinical evidence
Eur J Pharmacol. 2021 Sep 18:174503. doi: 10.1016/j.ejphar.2021.174503. Online ahead of print.ABSTRACTRenal fibrosis, a characteristic of all chronic kidney diseases, lacks effective therapeutic drugs currently. Pirfenidone (PFD), a small molecule drug with good oral bioavailability, is widely used in idiopathic pulmonary fibrosis and exerts anti-fibrotic, anti-inflammatory, antioxidant, and anti-apoptotic effects. These effects have been attributed to the suppression of cell growth factors (in particular, but not exclusively, transforming growth factor-β), matrix metalloproteinases, and the epithelial-mesenchymal tra...
Source: European Journal of Pharmacology - September 21, 2021 Category: Drugs & Pharmacology Authors: Xue Bai Ping Nie Yan Lou Yuexin Zhu Shan Jiang Bing Li Ping Luo Source Type: research

Evaluation of nootropic activity of telmisartan and metformin on diazepam-induced cognitive dysfunction in mice through AMPK pathway and amelioration of hippocampal morphological alterations
This study indicates that diazepam caused a decline in cognitive function depending on hippocampal activity. Telmisartan, a common antihypertensive agent and metformin, a traditional antidiabetic drug improved this cognitive dysfunction through their anti-oxidant and anti-inflammatory effect as they decreased initial and retention transfer latency as well as it increased step down latency. Also they decreased TNF-α, NFκB, and Caspase 3 and upregulated AMPK expression, moreover they ameliorated the hippocampal morphological alterations, GFAP and COX-2 immunoexpression.PMID:34547248 | DOI:10.1016/j.ejphar.2021.17...
Source: European Journal of Pharmacology - September 21, 2021 Category: Drugs & Pharmacology Authors: Eman S Said Asmaa M Elsayed Laila A Rashed Eman H Nadwa Njood A Alsuhaibani Batool S Alfuraih Rania H Mahmoud Source Type: research

Low-intensity pulsed ultrasound prevents angiotensin II-induced aortic smooth muscle cell phenotypic switch via hampering miR-17-5p and enhancing PPAR- γ
Eur J Pharmacol. 2021 Sep 18:174509. doi: 10.1016/j.ejphar.2021.174509. Online ahead of print.ABSTRACTVascular events can trigger a pathological phenotypic switch in vascular smooth muscle cells (VSMCs), decreasing and disrupting the plasticity and diversity of vascular networks. The development of novel therapeutic approaches is necessary to prevent these changes. We aimed to investigate the effects and associated mechanisms of low-intensity pulsed ultrasound (LIPUS) irradiation on the angiotensin II (AngII)-induced phenotypic switch in VSMCs. In vivo, AngII was infused subcutaneously for 4 weeks to stimulate vascular rem...
Source: European Journal of Pharmacology - September 21, 2021 Category: Drugs & Pharmacology Authors: Kun Zhao Tingting Wu Chuanxi Yang Haotian Pan Tianhua Xu Jing Zhang Xiasheng Guo Juan Tu Dong Zhang Xiangqing Kong Bin Zhou Wei Sun Source Type: research

Nectin cell adhesion molecule-4 (NECTIN-4): A potential target for cancer therapy
Eur J Pharmacol. 2021 Sep 18:174516. doi: 10.1016/j.ejphar.2021.174516. Online ahead of print.ABSTRACTNECTIN-4 [a poliovirus receptor-related-4 (pvrl-4) encoded protein] is a Ca2+ independent immunoglobulin-like protein. Along with other Nectins (Nectin-1, -2 and -3), it is primarily involved in cell-cell adhesion. In contrast to other Nectins, Nectin-4 is specifically enriched in the embryonic and placental tissues but its expression significantly declines in adult life. In recent years, it has been found that Nectin-4 is especially overexpressed and served as a tumor associated inducer in various malignant tumors includi...
Source: European Journal of Pharmacology - September 21, 2021 Category: Drugs & Pharmacology Authors: Subhajit Chatterjee Saptarshi Sinha Chanakya Nath Kundu Source Type: research

Pirfenidone is a renal protective drug: Mechanisms, signalling pathways, and preclinical evidence
Eur J Pharmacol. 2021 Sep 18:174503. doi: 10.1016/j.ejphar.2021.174503. Online ahead of print.ABSTRACTRenal fibrosis, a characteristic of all chronic kidney diseases, lacks effective therapeutic drugs currently. Pirfenidone (PFD), a small molecule drug with good oral bioavailability, is widely used in idiopathic pulmonary fibrosis and exerts anti-fibrotic, anti-inflammatory, antioxidant, and anti-apoptotic effects. These effects have been attributed to the suppression of cell growth factors (in particular, but not exclusively, transforming growth factor-β), matrix metalloproteinases, and the epithelial-mesenchymal tra...
Source: European Journal of Pharmacology - September 21, 2021 Category: Drugs & Pharmacology Authors: Xue Bai Ping Nie Yan Lou Yuexin Zhu Shan Jiang Bing Li Ping Luo Source Type: research

Evaluation of nootropic activity of telmisartan and metformin on diazepam-induced cognitive dysfunction in mice through AMPK pathway and amelioration of hippocampal morphological alterations
This study indicates that diazepam caused a decline in cognitive function depending on hippocampal activity. Telmisartan, a common antihypertensive agent and metformin, a traditional antidiabetic drug improved this cognitive dysfunction through their anti-oxidant and anti-inflammatory effect as they decreased initial and retention transfer latency as well as it increased step down latency. Also they decreased TNF-α, NFκB, and Caspase 3 and upregulated AMPK expression, moreover they ameliorated the hippocampal morphological alterations, GFAP and COX-2 immunoexpression.PMID:34547248 | DOI:10.1016/j.ejphar.2021.17...
Source: European Journal of Pharmacology - September 21, 2021 Category: Drugs & Pharmacology Authors: Eman S Said Asmaa M Elsayed Laila A Rashed Eman H Nadwa Njood A Alsuhaibani Batool S Alfuraih Rania H Mahmoud Source Type: research

Y-2 reduces oxidative stress and inflammation and improves neurological function of collagenase-induced intracerebral hemorrhage rats
In conclusion, Y-2 sublingual tablets might be a promising therapeutic agent for the treatment of ICH.PMID:34536364 | DOI:10.1016/j.ejphar.2021.174507 (Source: European Journal of Pharmacology)
Source: European Journal of Pharmacology - September 18, 2021 Category: Drugs & Pharmacology Authors: Yao Hua Limei Zhou Weidong Yang Wenji An Xiaolin Kou Jian Ren Hailang Su Rong Chen Zhengping Zhang Jianjun Zou Zhihong Zhao Source Type: research

Urea transporter and its specific and nonspecific inhibitors: State of the art and pharmacological perspective
Eur J Pharmacol. 2021 Sep 16;911:174508. doi: 10.1016/j.ejphar.2021.174508. Online ahead of print.ABSTRACTHypertension is a major concern for a wide array of patients. The traditional drugs are commonly referred as 'water pills' and these molecules have been successful in alleviating hypertension. However, this comes at the high expense of precious electrolytes in our body. To dissipate this major adverse effect, the urea transporter inhibitors play especially important roles in maintaining the fluid balance by maintaining the concentration of urea in the inner medullary collecting duct. The purpose of this communication i...
Source: European Journal of Pharmacology - September 18, 2021 Category: Drugs & Pharmacology Authors: Sudipta Nandi Saptarshi Sanyal Sk Abdul Amin Sushil Kumar Kashaw Tarun Jha Shovanlal Gayen Source Type: research

LncRNA MEG3 reverses CCl < sub > 4 < /sub > -induced liver fibrosis by targeting NLRC5
Eur J Pharmacol. 2021 Sep 15:174462. doi: 10.1016/j.ejphar.2021.174462. Online ahead of print.ABSTRACTLiver fibrosis is a persistent pathological repair of chronic liver injury, which is characterized by excessive deposition of collagen-dominated extracellular matrix (ECM). It is well known that hepatic fibrosis can be reversed in the absence of etiology. Studies have shown that long non-coding RNA (Lnc RNA) maternally expressed gene3 (MEG3) has strong effects on the activation of hepatic stellata cells (HSCs). However, the function of MEG3 in the reversal of liver fibrosis has not been studied. In this experiment, we stud...
Source: European Journal of Pharmacology - September 18, 2021 Category: Drugs & Pharmacology Authors: Yuan-Yuan Wu Sha Wu Xiao-Feng Li Shuai Luo Wang Ao Su-Qin Yin Cheng Huang Jun Li Source Type: research

Y-2 reduces oxidative stress and inflammation and improves neurological function of collagenase-induced intracerebral hemorrhage rats
In conclusion, Y-2 sublingual tablets might be a promising therapeutic agent for the treatment of ICH.PMID:34536364 | DOI:10.1016/j.ejphar.2021.174507 (Source: European Journal of Pharmacology)
Source: European Journal of Pharmacology - September 18, 2021 Category: Drugs & Pharmacology Authors: Yao Hua Limei Zhou Weidong Yang Wenji An Xiaolin Kou Jian Ren Hailang Su Rong Chen Zhengping Zhang Jianjun Zou Zhihong Zhao Source Type: research

Urea transporter and its specific and nonspecific inhibitors: State of the art and pharmacological perspective
Eur J Pharmacol. 2021 Sep 15:174508. doi: 10.1016/j.ejphar.2021.174508. Online ahead of print.ABSTRACTHypertension is a major concern for a wide array of patients. The traditional drugs are commonly referred as 'water pills' and these molecules have been successful in alleviating hypertension. However, this comes at the high expense of precious electrolytes in our body. To dissipate this major adverse effect, the urea transporter inhibitors play especially important roles in maintaining the fluid balance by maintaining the concentration of urea in the inner medullary collecting duct. The purpose of this communication is to...
Source: European Journal of Pharmacology - September 18, 2021 Category: Drugs & Pharmacology Authors: Sudipta Nandi Saptarshi Sanyal Sk Abdul Amin Sushil Kumar Kashaw Tarun Jha Shovanlal Gayen Source Type: research

LncRNA MEG3 reverses CCl < sub > 4 < /sub > -induced liver fibrosis by targeting NLRC5
Eur J Pharmacol. 2021 Sep 15:174462. doi: 10.1016/j.ejphar.2021.174462. Online ahead of print.ABSTRACTLiver fibrosis is a persistent pathological repair of chronic liver injury, which is characterized by excessive deposition of collagen-dominated extracellular matrix (ECM). It is well known that hepatic fibrosis can be reversed in the absence of etiology. Studies have shown that long non-coding RNA (Lnc RNA) maternally expressed gene3 (MEG3) has strong effects on the activation of hepatic stellata cells (HSCs). However, the function of MEG3 in the reversal of liver fibrosis has not been studied. In this experiment, we stud...
Source: European Journal of Pharmacology - September 18, 2021 Category: Drugs & Pharmacology Authors: Yuan-Yuan Wu Sha Wu Xiao-Feng Li Shuai Luo Wang Ao Su-Qin Yin Cheng Huang Jun Li Source Type: research

7-[[(4-methyl-2-pyridinyl)amino](2-pyridinyl)methyl]-8-quinolinol (compound 30666) inhibits enhancer activity and reduces B-cell lymphoma growth - A question of specificity
We report that both IGH-translocation positive NHL cells as well as IGH-translocation negative B cells and non-B cell controls treated with compound 30666 exhibited consistent growth inhibition. A statistically significant increase in cell percentage in sub-G1 phase of cell cycle was observed, suggesting induction of apoptosis. Compound 30666 downregulated MYC levels in BL cell lines and altered IGH enhancer RNA expression. Moreover, a global decrease of H3K27ac and an increase of H3K4me1 was observed upon 30666 treatment, which suggests switching enhancers to a poised or primed state. Altogether, our findings indicate tha...
Source: European Journal of Pharmacology - September 17, 2021 Category: Drugs & Pharmacology Authors: Marta El żbieta Kasprzyk Wojciech Łosiewski Marta Podralska Marta Kazimierska Weronika Sura Agnieszka Dzikiewicz-Krawczyk Source Type: research

Morin attenuates memory deficits in a rat model of Alzheimer's disease by ameliorating oxidative stress and neuroinflammation
This study aimed to investigate the effect of flavonoid morin on oxidative/nitrosative stress, neuroinflammation, and histological, molecular, and behavioral changes caused by amyloid-beta (Aβ)1-42 in male Wistar rats (Alzheimer's disease model). Rats received morin (20 mg/kg, oral gavage) for 14 consecutive days after intrahippocampal injection of Aβ1-42. Morin decreased the levels of malondialdehyde and nitric oxide, increased glutathione content, and enhanced catalase activity in the hippocampus of animals receiving Aβ1-42. It also reduced the expression of tumor necrosis factor-α, interleukin-1&bet...
Source: European Journal of Pharmacology - September 17, 2021 Category: Drugs & Pharmacology Authors: Negin Mohammadi Masoumeh Asle-Rousta Mehdi Rahnema Rahim Amini Source Type: research

Gypenoside XLIX loaded nanoparticles targeting therapy for renal fibrosis and its mechanism
This study opens a promising way for targeted drug treatment of renal fibrosis.PMID:34529980 | DOI:10.1016/j.ejphar.2021.174501 (Source: European Journal of Pharmacology)
Source: European Journal of Pharmacology - September 16, 2021 Category: Drugs & Pharmacology Authors: Qixia Liu Xiaohui Chen Min Kan Jing Yang Qian Gong Rui Jin Yulong Dai Juan Jin Hongmei Zang Source Type: research

The pharmacological assessment of resveratrol on preclinical models of rheumatoid arthritis through a systematic review and meta-analysis
Eur J Pharmacol. 2021 Sep 11:174504. doi: 10.1016/j.ejphar.2021.174504. Online ahead of print.ABSTRACTResveratrol/RES (3,5,4'-trihydroxy-trans-stilbene) is a natural compound found in many foods and red wine and has pleiotropic biological effects. Several preclinical studies evaluating the efficacy of RES in animal models of rheumatoid arthritis (RA) have been described, but the diversity of experimental conditions and of outcomes preclude definitive conclusions about RES's efficacy. We, therefore, performed a meta-analysis to assess its efficacy in mitigating experimental RA. We searched three databases until January 2021...
Source: European Journal of Pharmacology - September 14, 2021 Category: Drugs & Pharmacology Authors: Monika Mittal Poonam Mehta Swati Rajput Singh Rajender Naibedya Chattopadhyay Source Type: research

The pharmacological assessment of resveratrol on preclinical models of rheumatoid arthritis through a systematic review and meta-analysis
Eur J Pharmacol. 2021 Sep 11:174504. doi: 10.1016/j.ejphar.2021.174504. Online ahead of print.ABSTRACTResveratrol/RES (3,5,4'-trihydroxy-trans-stilbene) is a natural compound found in many foods and red wine and has pleiotropic biological effects. Several preclinical studies evaluating the efficacy of RES in animal models of rheumatoid arthritis (RA) have been described, but the diversity of experimental conditions and of outcomes preclude definitive conclusions about RES's efficacy. We, therefore, performed a meta-analysis to assess its efficacy in mitigating experimental RA. We searched three databases until January 2021...
Source: European Journal of Pharmacology - September 14, 2021 Category: Drugs & Pharmacology Authors: Monika Mittal Poonam Mehta Swati Rajput Singh Rajender Naibedya Chattopadhyay Source Type: research

The pharmacological assessment of resveratrol on preclinical models of rheumatoid arthritis through a systematic review and meta-analysis
Eur J Pharmacol. 2021 Sep 11:174504. doi: 10.1016/j.ejphar.2021.174504. Online ahead of print.ABSTRACTResveratrol/RES (3,5,4'-trihydroxy-trans-stilbene) is a natural compound found in many foods and red wine and has pleiotropic biological effects. Several preclinical studies evaluating the efficacy of RES in animal models of rheumatoid arthritis (RA) have been described, but the diversity of experimental conditions and of outcomes preclude definitive conclusions about RES's efficacy. We, therefore, performed a meta-analysis to assess its efficacy in mitigating experimental RA. We searched three databases until January 2021...
Source: European Journal of Pharmacology - September 14, 2021 Category: Drugs & Pharmacology Authors: Monika Mittal Poonam Mehta Swati Rajput Singh Rajender Naibedya Chattopadhyay Source Type: research

The pharmacological assessment of resveratrol on preclinical models of rheumatoid arthritis through a systematic review and meta-analysis
Eur J Pharmacol. 2021 Sep 11:174504. doi: 10.1016/j.ejphar.2021.174504. Online ahead of print.ABSTRACTResveratrol/RES (3,5,4'-trihydroxy-trans-stilbene) is a natural compound found in many foods and red wine and has pleiotropic biological effects. Several preclinical studies evaluating the efficacy of RES in animal models of rheumatoid arthritis (RA) have been described, but the diversity of experimental conditions and of outcomes preclude definitive conclusions about RES's efficacy. We, therefore, performed a meta-analysis to assess its efficacy in mitigating experimental RA. We searched three databases until January 2021...
Source: European Journal of Pharmacology - September 14, 2021 Category: Drugs & Pharmacology Authors: Monika Mittal Poonam Mehta Swati Rajput Singh Rajender Naibedya Chattopadhyay Source Type: research

The pharmacological assessment of resveratrol on preclinical models of rheumatoid arthritis through a systematic review and meta-analysis
Eur J Pharmacol. 2021 Sep 11:174504. doi: 10.1016/j.ejphar.2021.174504. Online ahead of print.ABSTRACTResveratrol/RES (3,5,4'-trihydroxy-trans-stilbene) is a natural compound found in many foods and red wine and has pleiotropic biological effects. Several preclinical studies evaluating the efficacy of RES in animal models of rheumatoid arthritis (RA) have been described, but the diversity of experimental conditions and of outcomes preclude definitive conclusions about RES's efficacy. We, therefore, performed a meta-analysis to assess its efficacy in mitigating experimental RA. We searched three databases until January 2021...
Source: European Journal of Pharmacology - September 14, 2021 Category: Drugs & Pharmacology Authors: Monika Mittal Poonam Mehta Swati Rajput Singh Rajender Naibedya Chattopadhyay Source Type: research

Metformin abrogates the voiding dysfunction induced by prolonged methylglyoxal intake
Eur J Pharmacol. 2021 Sep 10:174502. doi: 10.1016/j.ejphar.2021.174502. Online ahead of print.ABSTRACTMethylglyoxal (MGO) is a reactive carbonyl species found at high levels in blood of diabetic patients. The anti-hyperglycemic drug metformin can scavenger MGO and reduce the formation of advanced glycation end products (AGEs). Here, we aimed to investigate if MGO-induced bladder dysfunction can be reversed by metformin. Male C57/BL6 mice received 0.5% MGO in drinking water for 12 weeks, and metformin (300 mg/kg, daily gavage) was given in the last two weeks. The bladder functions were evaluated by performing voiding behavi...
Source: European Journal of Pharmacology - September 13, 2021 Category: Drugs & Pharmacology Authors: Akila L Oliveira Mariana G de Oliveira Matheus L Medeiros Fab íola Z Mónica Edson Antunes Source Type: research

Reversal of elastase-induced abdominal aortic aneurysm following the delivery of nanoparticle-based pentagalloyl glucose (PGG) is associated with reduced inflammatory and immune markers
CONCLUSION: Nanoparticles-loaded pentagalloyl glucose therapy can be an effective treatment option against advanced stage aneurysms to reverse the disease by ameliorating inflammation and restoring arterial homeostasis.PMID:34516951 | DOI:10.1016/j.ejphar.2021.174487 (Source: European Journal of Pharmacology)
Source: European Journal of Pharmacology - September 13, 2021 Category: Drugs & Pharmacology Authors: Dhital Saphala Charles D Rice Naren R Vyavahare Source Type: research

Fisetin, potential flavonoid with multifarious targets for treating neurological disorders: An updated review
Eur J Pharmacol. 2021 Sep 10:174492. doi: 10.1016/j.ejphar.2021.174492. Online ahead of print.ABSTRACTNeurodegenerative disorders pose a significant health burden and imprint a debilitative impact on the quality of life. Importantly, aging is intricately intertwined with the progression of these disorders, and their prevalence increases with a rise in the aging population worldwide. In recent times, fisetin emerged as one of the potential miracle molecules to address neurobehavioral and cognitive abnormalities. These effects were attributed to its actions on several macromolecules and multiple molecular mechanisms. Fisetin...
Source: European Journal of Pharmacology - September 13, 2021 Category: Drugs & Pharmacology Authors: Ravula Arun Reddy Teegala Suraj Benerji Kalakotla Shanker Pasangulapati Jagadeesh Prasad Venkatesan Perumal Boyina Hemanth Kumar Source Type: research

Metformin abrogates the voiding dysfunction induced by prolonged methylglyoxal intake
Eur J Pharmacol. 2021 Sep 10:174502. doi: 10.1016/j.ejphar.2021.174502. Online ahead of print.ABSTRACTMethylglyoxal (MGO) is a reactive carbonyl species found at high levels in blood of diabetic patients. The anti-hyperglycemic drug metformin can scavenger MGO and reduce the formation of advanced glycation end products (AGEs). Here, we aimed to investigate if MGO-induced bladder dysfunction can be reversed by metformin. Male C57/BL6 mice received 0.5% MGO in drinking water for 12 weeks, and metformin (300 mg/kg, daily gavage) was given in the last two weeks. The bladder functions were evaluated by performing voiding behavi...
Source: European Journal of Pharmacology - September 13, 2021 Category: Drugs & Pharmacology Authors: Akila L Oliveira Mariana G de Oliveira Matheus L Medeiros Fab íola Z Mónica Edson Antunes Source Type: research

Reversal of elastase-induced abdominal aortic aneurysm following the delivery of nanoparticle-based pentagalloyl glucose (PGG) is associated with reduced inflammatory and immune markers
CONCLUSION: Nanoparticles-loaded pentagalloyl glucose therapy can be an effective treatment option against advanced stage aneurysms to reverse the disease by ameliorating inflammation and restoring arterial homeostasis.PMID:34516951 | DOI:10.1016/j.ejphar.2021.174487 (Source: European Journal of Pharmacology)
Source: European Journal of Pharmacology - September 13, 2021 Category: Drugs & Pharmacology Authors: Dhital Saphala Charles D Rice Naren R Vyavahare Source Type: research

Fisetin, potential flavonoid with multifarious targets for treating neurological disorders: An updated review
Eur J Pharmacol. 2021 Sep 10:174492. doi: 10.1016/j.ejphar.2021.174492. Online ahead of print.ABSTRACTNeurodegenerative disorders pose a significant health burden and imprint a debilitative impact on the quality of life. Importantly, aging is intricately intertwined with the progression of these disorders, and their prevalence increases with a rise in the aging population worldwide. In recent times, fisetin emerged as one of the potential miracle molecules to address neurobehavioral and cognitive abnormalities. These effects were attributed to its actions on several macromolecules and multiple molecular mechanisms. Fisetin...
Source: European Journal of Pharmacology - September 13, 2021 Category: Drugs & Pharmacology Authors: Ravula Arun Reddy Teegala Suraj Benerji Kalakotla Shanker Pasangulapati Jagadeesh Prasad Venkatesan Perumal Boyina Hemanth Kumar Source Type: research

Angiogenesis as a potential treatment strategy for rheumatoid arthritis
Eur J Pharmacol. 2021 Sep 9;910:174500. doi: 10.1016/j.ejphar.2021.174500. Online ahead of print.ABSTRACTAngiogenesis is an early and key event in the pathogenesis of rheumatoid arthritis (RA) and is crucial for the proliferation of synovial tissue and the formation of pannus. This process is regulated by both angiogenesis-stimulating factors and angiogenesis inhibitors, the basis for the "on-off hypothesis of angiogenesis." In RA, inflammation, immune imbalance, and hypoxia can further turn on the switch for blood vessel formation and induce angiogenesis. The new vasculature can recruit white blood cells, induce...
Source: European Journal of Pharmacology - September 12, 2021 Category: Drugs & Pharmacology Authors: Yan Wang Hong Wu Ran Deng Source Type: research

Angiogenesis as a potential treatment strategy for rheumatoid arthritis
Eur J Pharmacol. 2021 Sep 9:174500. doi: 10.1016/j.ejphar.2021.174500. Online ahead of print.ABSTRACTAngiogenesis is an early and key event in the pathogenesis of rheumatoid arthritis (RA) and is crucial for the proliferation of synovial tissue and the formation of pannus. This process is regulated by both angiogenesis-stimulating factors and angiogenesis inhibitors, the basis for the "on-off hypothesis of angiogenesis." In RA, inflammation, immune imbalance, and hypoxia can further turn on the switch for blood vessel formation and induce angiogenesis. The new vasculature can recruit white blood cells, induce imm...
Source: European Journal of Pharmacology - September 12, 2021 Category: Drugs & Pharmacology Authors: Yan Wang Hong Wu Ran Deng Source Type: research

Resveratrol modulates Toxoplasma gondii infection induced liver injury by intervening in the HMGB1/TLR4/NF- κB signaling pathway
This study used the RH strain tachyzoites of T. gondii to infect murine liver line, NCTC-1469 cells to establish an in vitro model and acute infection of mice for the in vivo model to explore the protective effect of RSV on liver injury induced by T. gondii infection. The results showed that RSV inhibited the proliferation of T. gondii in the liver, reduced the alanine aminotransferase/aspartate aminotransferase levels and pathological liver damage. Additionally, RSV inhibited the production of tumor necrosis factor-α, inducible nitric oxide synthase and HMGB1 by interfering with the TLR4/NF-κB signaling pathwa...
Source: European Journal of Pharmacology - September 11, 2021 Category: Drugs & Pharmacology Authors: Jing-Mei Lu Guang-Nan Jin Yu-Nan Lu Xu-Dong Zhao Hui-Wen Lan Shuai-Ru Mu Xin-Yu Shen Guang-Hua Xu Cheng-Hua Jin Juan Ma Xuejun Jin Xiang Xu Lian-Xun Piao Source Type: research

Treprostinil palmitil inhibits the hemodynamic and histopathological changes in the pulmonary vasculature and heart in an animal model of pulmonary arterial hypertension
In this study, TP was delivered by inhalation (treprostinil palmitil inhalation suspension, TPIS) in a rat sugen 5416 (Su)/hypoxia (Hx) model of pulmonary arterial hypertension (PAH) to evaluate its effects on hemodynamics, pulmonary vascular remodeling, and cardiac performance and histopathology. Male Sprague-Dawley rats received Su (20 mg/kg, s.c), three weeks of Hx (10% O2) and 5 or 10 weeks of normoxia (Nx). TPIS was given during the 5-10 week NX period after the Su/Hx challenge. Su/Hx increased the mean pulmonary arterial blood pressure (mPAP) and right heart size (Fulton index), reduced cardiac output (CO), stroke vo...
Source: European Journal of Pharmacology - September 11, 2021 Category: Drugs & Pharmacology Authors: Michel R Corboz Adam J Plaunt Vladimir Malinin Zhili Li Helena Gauani Donald Chun David Cipolla Walter R Perkins Richard W Chapman Source Type: research

Protective effects of octylseleno-xylofuranoside in a streptozotocin-induced mouse model of Alzheimer's disease
Eur J Pharmacol. 2021 Sep 8:174499. doi: 10.1016/j.ejphar.2021.174499. Online ahead of print.ABSTRACTOctylseleno-xylofuranoside (OSX) is an organic selenium compound which has previously shown antioxidant and antidepressant-like activities, trough the modulation of monoaminergic system and synaptic plasticity pathways. Since recent studies have suggested Major Depressive Disorder (MDD) as a potential risk factor or condition that precedes and correlates with Alzheimer's Disease (AD), this study aimed to evaluate the protective effects of OSX in an AD mouse model induced by intracerebroventricular injection of STZ. To addre...
Source: European Journal of Pharmacology - September 11, 2021 Category: Drugs & Pharmacology Authors: Rodolfo Baldinotti Mariana G Fronza Luana Silva Camila Bonemann Bender Diogo Seibert L üdtke Fabiana K Seixas Tiago Collares Diego Alves Lucielli Savegnago Source Type: research

Short-lived sensitization of cardiovascular outcomes of postpartum endotoxemia in preeclamptic rats: Role of medullary solitary tract neuroinflammation
Eur J Pharmacol. 2021 Sep 8;910:174494. doi: 10.1016/j.ejphar.2021.174494. Online ahead of print.ABSTRACTPreeclampsia (PE) is a pregnancy-related disorder with serious maternal complications. Considering the increased importance of postpartum infection in maternal morbidity and mortality, we investigated whether preeclamptic maternal programming alters cardiovascular consequences of endotoxemia in rats and the role of cardiac and brainstem neuroinflammation in this interaction. Preeclampsia was induced by oral administration of L-NAME (50 mg/kg/day) for 7 days starting from day 14 of conception. Changes in blood pressure, ...
Source: European Journal of Pharmacology - September 11, 2021 Category: Drugs & Pharmacology Authors: Salwa A Abuiessa Sahar M El-Gowilly Hanan M El-Gowelli Mai M Helmy Mahmoud M El-Mas Source Type: research

Potent efficacy of Stachybotrys microspora triprenyl phenol-7, a small molecule having anti-inflammatory and antioxidant activities, in a mouse model of acute kidney injury
Eur J Pharmacol. 2021 Sep 7;910:174496. doi: 10.1016/j.ejphar.2021.174496. Online ahead of print.ABSTRACTAcute kidney injury (AKI) increases the risk of chronic kidney disease (CKD), complicates existing CKD, and can lead to the end-stage renal disease. However, there are no approved effective therapeutics for AKI. Recent studies have suggested that inflammation and oxidative stress are the primary causes of AKI. We previously reported the potential anti-inflammatory and antioxidant activities of Stachybotrys microspora triprenyl phenol-7 (SMTP-7). The aim of the present study was to evaluate the efficacy of SMTP-7 in AKI ...
Source: European Journal of Pharmacology - September 10, 2021 Category: Drugs & Pharmacology Authors: Keita Shibata Terumasa Hashimoto Keiji Hasumi Koji Nobe Source Type: research

Dexmedetomidine protects the heart against ischemia reperfusion injury via regulation of the bradykinin receptors
CONCLUSIONS: DEX regulates BK receptor expression and potentiates the protection of BK in cardiac I/R injury, which suggests that modulating endogenous cardioprotective factors may play an important role in DEX-induced cardioprotection.PMID:34506777 | DOI:10.1016/j.ejphar.2021.174493 (Source: European Journal of Pharmacology)
Source: European Journal of Pharmacology - September 10, 2021 Category: Drugs & Pharmacology Authors: Jinchao Song Jiankui Du Xing Tan Zhaotang Wu Jihong Yuan Binhai Cong Source Type: research

Phosphodiesterase-1 inhibitor modulates Ca < sup > 2+ < /sup > regulation in sirtuin 1-deficient mouse cardiomyocytes
CONCLUSIONS: Our results suggest that ITI-214 improves intracellular Ca2+ regulation, which in turn exerts inotropic effects and suppresses arrhythmic events in Sirt1-deficient ventricular myocytes.PMID:34506778 | DOI:10.1016/j.ejphar.2021.174498 (Source: European Journal of Pharmacology)
Source: European Journal of Pharmacology - September 10, 2021 Category: Drugs & Pharmacology Authors: Hui-Wen Yang Chih-Yuan Lin Feng-Zhi Lin Pei-Ling Yu Shih-Ming Huang Yao-Chang Chen Chien-Sung Tsai Hsiang-Yu Yang Source Type: research

Involvement of interstitial cells of Cajal in nicotinic acetylcholine receptor-induced relaxation of the porcine lower esophageal sphincter
In conclusion, membrane hyperpolarization of the ICCs via the activation of anoctamin-1 plays a central role in DMPP-induced relaxation. ATP may be a neurotransmitter for inhibitory enteric neurons, which stimulate the ICCs. The ICCs act as the interface of neurotransmission of nicotinic acetylcholine receptor in order to induce LES relaxation.PMID:34506779 | DOI:10.1016/j.ejphar.2021.174491 (Source: European Journal of Pharmacology)
Source: European Journal of Pharmacology - September 10, 2021 Category: Drugs & Pharmacology Authors: Yoshihiro Otsuka Xiaopeng Bai Yoshimasa Tanaka Eikichi Ihara Takatoshi Chinen Haruei Ogino Yoshihiro Ogawa Source Type: research

Potent efficacy of Stachybotrys microspora triprenyl phenol-7, a small molecule having anti-inflammatory and antioxidant activities, in a mouse model of acute kidney injury
Eur J Pharmacol. 2021 Sep 7:174496. doi: 10.1016/j.ejphar.2021.174496. Online ahead of print.ABSTRACTAcute kidney injury (AKI) increases the risk of chronic kidney disease (CKD), complicates existing CKD, and can lead to the end-stage renal disease. However, there are no approved effective therapeutics for AKI. Recent studies have suggested that inflammation and oxidative stress are the primary causes of AKI. We previously reported the potential anti-inflammatory and antioxidant activities of Stachybotrys microspora triprenyl phenol-7 (SMTP-7). The aim of the present study was to evaluate the efficacy of SMTP-7 in AKI mode...
Source: European Journal of Pharmacology - September 10, 2021 Category: Drugs & Pharmacology Authors: Keita Shibata Terumasa Hashimoto Keiji Hasumi Koji Nobe Source Type: research

Dexmedetomidine protects the heart against ischemia reperfusion injury via regulation of the bradykinin receptors
CONCLUSIONS: DEX regulates BK receptor expression and potentiates the protection of BK in cardiac I/R injury, which suggests that modulating endogenous cardioprotective factors may play an important role in DEX-induced cardioprotection.PMID:34506777 | DOI:10.1016/j.ejphar.2021.174493 (Source: European Journal of Pharmacology)
Source: European Journal of Pharmacology - September 10, 2021 Category: Drugs & Pharmacology Authors: Jinchao Song Jiankui Du Xing Tan Zhaotang Wu Jihong Yuan Binhai Cong Source Type: research

Phosphodiesterase-1 inhibitor modulates Ca < sup > 2+ < /sup > regulation in sirtuin 1-deficient mouse cardiomyocytes
CONCLUSIONS: Our results suggest that ITI-214 improves intracellular Ca2+ regulation, which in turn exerts inotropic effects and suppresses arrhythmic events in Sirt1-deficient ventricular myocytes.PMID:34506778 | DOI:10.1016/j.ejphar.2021.174498 (Source: European Journal of Pharmacology)
Source: European Journal of Pharmacology - September 10, 2021 Category: Drugs & Pharmacology Authors: Hui-Wen Yang Chih-Yuan Lin Feng-Zhi Lin Pei-Ling Yu Shih-Ming Huang Yao-Chang Chen Chien-Sung Tsai Hsiang-Yu Yang Source Type: research

Involvement of interstitial cells of Cajal in nicotinic acetylcholine receptor-induced relaxation of the porcine lower esophageal sphincter
In conclusion, membrane hyperpolarization of the ICCs via the activation of anoctamin-1 plays a central role in DMPP-induced relaxation. ATP may be a neurotransmitter for inhibitory enteric neurons, which stimulate the ICCs. The ICCs act as the interface of neurotransmission of nicotinic acetylcholine receptor in order to induce LES relaxation.PMID:34506779 | DOI:10.1016/j.ejphar.2021.174491 (Source: European Journal of Pharmacology)
Source: European Journal of Pharmacology - September 10, 2021 Category: Drugs & Pharmacology Authors: Yoshihiro Otsuka Xiaopeng Bai Yoshimasa Tanaka Eikichi Ihara Takatoshi Chinen Haruei Ogino Yoshihiro Ogawa Source Type: research

Pharmacological significance of extra-oral taste receptors
Eur J Pharmacol. 2021 Sep 5:174480. doi: 10.1016/j.ejphar.2021.174480. Online ahead of print.ABSTRACTIt has recently been shown that taste receptors, in addition to being present in the oral cavity, exist in various extra-oral organs and tissues such as the thyroid, lungs, skin, stomach, intestines, and pancreas. Although their physiological function is not yet fully understood, it appears that they can help regulate the body's homeostasis and provide an additional defense function against pathogens. Since the vast majority of drugs are bitter, the greatest pharmacological interest is in the bitter taste receptors. In this...
Source: European Journal of Pharmacology - September 8, 2021 Category: Drugs & Pharmacology Authors: Ottavio D'Urso Filippo Drago Source Type: research

Pharmacological significance of extra-oral taste receptors
Eur J Pharmacol. 2021 Sep 5:174480. doi: 10.1016/j.ejphar.2021.174480. Online ahead of print.ABSTRACTIt has recently been shown that taste receptors, in addition to being present in the oral cavity, exist in various extra-oral organs and tissues such as the thyroid, lungs, skin, stomach, intestines, and pancreas. Although their physiological function is not yet fully understood, it appears that they can help regulate the body's homeostasis and provide an additional defense function against pathogens. Since the vast majority of drugs are bitter, the greatest pharmacological interest is in the bitter taste receptors. In this...
Source: European Journal of Pharmacology - September 8, 2021 Category: Drugs & Pharmacology Authors: Ottavio D'Urso Filippo Drago Source Type: research

Candidates for smart cardiovascular medical device coatings: A comparative study with endothelial and smooth muscle cells
Eur J Pharmacol. 2021 Sep 4:174490. doi: 10.1016/j.ejphar.2021.174490. Online ahead of print.ABSTRACTStent-induced vascular injury is manifested by removal of the endothelium and phenotypic changes in the underlying medial smooth muscle cells layer. This results in pathological vascular remodelling primarily contributed to smooth muscle cell proliferation and leads to vessel re-narrowing; neointimal hyperplasia. Current drug-eluting stents release non-selective anti-proliferative drugs such as paclitaxel from the stent surface that not only inhibit growth of smooth muscle cells but also delay endothelial healing, potential...
Source: European Journal of Pharmacology - September 7, 2021 Category: Drugs & Pharmacology Authors: Miriama Ceresnakova David Murray Tewfik Soulimane Sarah P Hudson Source Type: research