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Effect of resveratrol on the pharmacokinetics of fexofenadine in rats: Involvement of P-glycoprotein inhibition.
CONCLUSIONS: RSV significantly enhanced the exposure of FEX in rats likely by the inhibition of P-glycoprotein (P-gp) mediated efflux during the intestinal absorption, suggesting that there is a potential pharmacokinetic interaction between RSV and FEX. Therefore, further studies are recommended to evaluate the potential drug-phytochemical interactions in humans. PMID: 26922536 [PubMed - as supplied by publisher] (Source: Pharmacological Reports)
Source: Pharmacological Reports - February 29, 2016 Category: Drugs & Pharmacology Authors: Bedada SK, Yellu NR, Neerati P Tags: Pharmacol Rep Source Type: research

Intensive statin therapy, used alone or in combination with ezetimibe, improves homocysteine level and lipid peroxidation to a similar degree in patients with coronary artery diseases.
Abstract BACKGROUND: Increase in the concentration of homocysteine is one of the risks of cardiovascular diseases. Coronary artery disease accompanied the increase of LDL cholesterol level and hipolipemic drugs are used in such treatments. Also these drugs have pleiotropic effects, which are not greatly known. The aim of that study is to compare the effect of three different hipolipemic therapies (rosuvastatin 15mg/d; atorvastatin 40mg/d; atorvastatin+ezetymibe 10mg/d+10mg/d) depending upon the concentration of homocysteine and lipid peroxidation in plasma of CAD patients with non-target LDL-cholesterol level. ...
Source: Pharmacological Reports - February 29, 2016 Category: Drugs & Pharmacology Authors: Pytel E, Jackowska P, Chwatko G, Olszewska-Banaszczyk M, Koter-Michalak M, Kubalczyk P, Broncel M Tags: Pharmacol Rep Source Type: research

Hesperidin alleviates cisplatin-induced hepatotoxicity in rats without inhibiting its antitumor activity.
CONCLUSION: Hesperidin decreased cisplatin-induced functional and histopathological liver damage in a dose-dependent manner without affecting its potential cytotoxic effect. PMID: 26922538 [PubMed - as supplied by publisher] (Source: Pharmacological Reports)
Source: Pharmacological Reports - February 29, 2016 Category: Drugs & Pharmacology Authors: Omar HA, Mohamed WR, Arafa EA, Shehata BA, Sherbiny GA, Arab HH, Elgendy AN Tags: Pharmacol Rep Source Type: research

Ifenprodil for prolonged spinal blockades of motor function and nociception in rats.
Abstract BACKGROUND: The aim of the study was to compare the proposed spinal anesthetic effect of ifenprodil, an a1 adrenergic receptor antagonist, with that of the long-acting local anesthetic bupivacaine. METHODS: After intrathecally injecting the rats with five different doses of each drug, the dose-response curves of ifenprodil and bupivacaine were constructed to obtain the 50% effective dose (ED50). The spinal blockades of motor function and nociception of ifenprodil were compared with that of bupivacaine. RESULTS: We showed that either ifenprodil or bupivacaine produced spinal blockades of motor fu...
Source: Pharmacological Reports - February 29, 2016 Category: Drugs & Pharmacology Authors: Chen YW, Chiu CC, Wang JN, Hung CH, Wang JJ Tags: Pharmacol Rep Source Type: research

Age-specific influences of chronic administration of the fatty acid amide hydrolase inhibitor URB597 on cardiovascular parameters and organ hypertrophy in DOCA-salt hypertensive rats.
CONCLUSION: Two weeks of URB597 administration to DOCA-salt hypertensive rats caused an age-specific reduction in BP, HR and cardiac and renal hypertrophy and did not affect the body weight, and water and food intake. Thus, caution should be taken during studies of FAAH inhibitors because of their potential age-specific effects. PMID: 26922540 [PubMed - as supplied by publisher] (Source: Pharmacological Reports)
Source: Pharmacological Reports - February 29, 2016 Category: Drugs & Pharmacology Authors: Toczek M, Baranowska-Kuczko M, Grzęda E, Pędzińska-Betiuk A, Weresa J, Malinowska B Tags: Pharmacol Rep Source Type: research

Renoprotective effect of diosgenin in streptozotocin induced diabetic rats.
CONCLUSION: The above study justifies diosgenin as a promising candidate in diabetes associated complication through its antioxidant and anti-inflammatory activity. PMID: 26922541 [PubMed - as supplied by publisher] (Source: Pharmacological Reports)
Source: Pharmacological Reports - February 29, 2016 Category: Drugs & Pharmacology Authors: Kanchan DM, Somani GS, Peshattiwar VV, Kaikini AA, Sathaye S Tags: Pharmacol Rep Source Type: research

The preventive role of levosimendan against bleomycin-induced pulmonary fibrosis in rats.
In this study, the effects of levosimendan used in the treatment of acute congestive heart failure upon pulmonary fibrosis in rats induced with bleomycin (BL) were analyzed. METHODS: A total of 33 male Sprague-Dawley type rats were categorized into five groups randomly. About 2.5U/kg BL was intratracheally administered to the rats in the BL, BL+L1, BL+L2, and BL+L3 groups, and 0.9% saline was intratracheally administered at the same rate to the control group. 0.3, 1, and 3mg/kg levosimendan was intraperitoneally administered to the BL+L1, BL+L2, and BL+L3 groups, respectively. Blood and tissue samples were taken from ...
Source: Pharmacological Reports - February 29, 2016 Category: Drugs & Pharmacology Authors: Gürbüzel M, Sayar I, Cankaya M, Gürbüzel A, Demirtas L, Bakirci EM, Capoglu I Tags: Pharmacol Rep Source Type: research

The molecular basis of chloroethylclonidine block of inward rectifier (Kir2.1 and Kir4.1) K(+) channels.
CONCLUSIONS: Overall, our results suggest that differences in the cavity of Kir channels are determinants in its interactions with chloroethylclonidine. PMID: 26922543 [PubMed - as supplied by publisher] (Source: Pharmacological Reports)
Source: Pharmacological Reports - February 29, 2016 Category: Drugs & Pharmacology Authors: Rodríguez-Menchaca AA, Aréchiga-Figueroa IA, Sánchez-Chapula JA Tags: Pharmacol Rep Source Type: research

Odors identification differences in deficit and nondeficit schizophrenia.
CONCLUSIONS: No overall differences between DS and NDS regarding odors identification have been found. The results seem to indicate some specific deficits in the identification of markers of rose, pineapple, orange and cinnamon. PMID: 26922544 [PubMed - as supplied by publisher] (Source: Pharmacological Reports)
Source: Pharmacological Reports - February 29, 2016 Category: Drugs & Pharmacology Authors: Pełka-Wysiecka J, Wroński M, Bieńkowski P, Murawiec S, Samochowiec A, Samochowiec J Tags: Pharmacol Rep Source Type: research

Augmentation of effect of venlafaxine by folic acid in behavioral paradigms of depression in mice: Evidence of serotonergic and pro-inflammatory cytokine pathways.
CONCLUSIONS: Combining low dose venlafaxine with an augmenting agent like folic acid, thus, appears to be an optimum strategy to increase its therapeutic efficacy and to reduce its dose. PMID: 26922545 [PubMed - as supplied by publisher] (Source: Pharmacological Reports)
Source: Pharmacological Reports - February 29, 2016 Category: Drugs & Pharmacology Authors: Thomas J, Khanam R, Vohora D Tags: Pharmacol Rep Source Type: research

Recent advances in the biomedical applications of fumaric acid and its ester derivatives: The multifaceted alternative therapeutics.
Abstract Several lines of evidence have demonstrated the potential biomedical applications of fumaric acid (FA) and its ester derivatives against many human disease conditions. Fumaric acid esters (FAEs) have been licensed for the systemic treatment of the immune-mediated disease psoriasis. Biogen Idec Inc. announced about the safety and efficacy of the formulation FAE (BG-12) for treating RRMS (relapsing-remitting multiple sclerosis). Another FAE formulation DMF (dimethyl fumarate) was found to be capable of reduction in inflammatory cardiac conditions, such as autoimmune myocarditis and ischemia and reperfusion....
Source: Pharmacological Reports - February 29, 2016 Category: Drugs & Pharmacology Authors: Das RK, Brar SK, Verma M Tags: Pharmacol Rep Source Type: research

The influence of aripiprazole and olanzapine on the anxiolytic-like effect observed in prenatally stressed rats (animal model of schizophrenia) exposed to the ethyl alcohol.
CONCLUSION: ARI and OLA can reduce the level of anxiety which proves drugs effectiveness in course anxiety-like behavior. On the other hand only ARI generated anxiolytic effect in exposure to ethyl alcohol conditions. PMID: 26922547 [PubMed - as supplied by publisher] (Source: Pharmacological Reports)
Source: Pharmacological Reports - February 29, 2016 Category: Drugs & Pharmacology Authors: Ratajczak P, Kus K, Giermaziak W, Nowakowska E Tags: Pharmacol Rep Source Type: research

A novel synthetic novobiocin analog, FM-Nov17, induces DNA damage in CML cells through generation of reactive oxygen species.
CONCLUSIONS: FM-Nov17-induces DNA damage and mitochondria-dependent cellular apoptosis in CML cells. The process is mediated by the generation of ROS. PMID: 26922548 [PubMed - as supplied by publisher] (Source: Pharmacological Reports)
Source: Pharmacological Reports - February 29, 2016 Category: Drugs & Pharmacology Authors: Zhang N, Huang L, Tian J, Chen X, Ke F, Zheng M, Xu J, Wu L Tags: Pharmacol Rep Source Type: research

The effect of statin therapy on thyroid autoimmunity in patients with Hashimoto's thyroiditis: A pilot study.
CONCLUSIONS: Although 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitors are able to reduce thyroid autoimmunity in women with Hashimoto's thyroiditis, intensive statin therapy is required to produce this effect. PMID: 26922549 [PubMed - as supplied by publisher] (Source: Pharmacological Reports)
Source: Pharmacological Reports - February 29, 2016 Category: Drugs & Pharmacology Authors: Krysiak R, Kowalcze K, Okopień B Tags: Pharmacol Rep Source Type: research

Role of spinal 5-HT2 receptors subtypes in formalin-induced long-lasting hypersensitivity.
CONCLUSION: Data suggest that spinal 5-HT2A/2B/2C receptors have pronociceptive effects and participate in the development and maintenance of formalin-induced long-lasting hypersensitivity. These receptors are expressed in DRG and their expression is modulated by formalin. PMID: 26922550 [PubMed - as supplied by publisher] (Source: Pharmacological Reports)
Source: Pharmacological Reports - February 29, 2016 Category: Drugs & Pharmacology Authors: Cervantes-Durán C, Vidal-Cantú GC, Godínez-Chaparro B, Granados-Soto V Tags: Pharmacol Rep Source Type: research

The role of glutamatergic, GABA-ergic, and cholinergic receptors in depression and antidepressant-like effect.
Abstract Depression is one of the most common mental disorders and social issue worldwide. Although there are many antidepressants available, the effectiveness of the therapy is still a serious issue. Moreover, there are many limitations of currently used antidepressants, including slow onset of action, numerous side effects, or the fact that many patients do not respond adequately to the treatment. Therefore, scientists are searching for new compounds with different mechanisms of action. Numerous data indicate the important role of glutamatergic, GABA-ergic, and cholinergic receptors in the pathomechanism of majo...
Source: Pharmacological Reports - February 29, 2016 Category: Drugs & Pharmacology Authors: Pytka K, Dziubina A, Młyniec K, Dziedziczak A, Żmudzka E, Furgała A, Olczyk A, Sapa J, Filipek B Tags: Pharmacol Rep Source Type: research

Coadministration of tramadol with aripiprazole and venlafaxine-The effect on spatial memory functions in male rats.
CONCLUSION: It can be assumed that chronic treatment with combinations of TRM+VEN or TRM+ARI is unlikely to cause memory impairment and interfere with either any antidepressant effect of VEN or any antipsychotic effect of ARI in patients suffering from chronic pain using TRM. PMID: 26922552 [PubMed - as supplied by publisher] (Source: Pharmacological Reports)
Source: Pharmacological Reports - February 29, 2016 Category: Drugs & Pharmacology Authors: Szkutnik-Fiedler D, Kus K, Ratajczak P, Antoniów M, Nowakowska E, Grześkowiak E Tags: Pharmacol Rep Source Type: research

Modulation of the voltage-gated potassium channel Kv2.1 by the anti-tumor alkylphospholipid perifosine.
CONCLUSIONS: Taken together, these results show that perifosine modified the Kv2.1 inactivation gating resulting in a decrease of the current amplitude. These data will help to elucidate the mechanism of action of this promising anti-cancer drug on ion channels and their possible implications. PMID: 26922553 [PubMed - as supplied by publisher] (Source: Pharmacological Reports)
Source: Pharmacological Reports - February 29, 2016 Category: Drugs & Pharmacology Authors: Delgado-Ramírez M, Morán-Zendejas R, Aréchiga-Figueroa IA, Toro-Castillo C, Ramírez-Martínez JF, Rodríguez-Menchaca AA Tags: Pharmacol Rep Source Type: research

Reactive oxygen species and synthetic antioxidants as angiogenesis modulators: Clinical implications.
oszewska A Abstract Angiogenesis is important for normal functioning of organism and its disturbances are observed in many diseases, called angiogenesis-related states. Reactive oxygen species (ROSs) play an important role in physiology, but high level of cellular ROSs is cytotoxic and mutagenic for the cells, i.e. it can lead to oxidative stress. In this review we discuss close relationship between ROSs and angiogenesis process. Substances counteracting free radicals or their action and oxidative stress are known as antioxidants. We postulate that antioxidants, by affecting angiogenesis, may modulate therapy res...
Source: Pharmacological Reports - February 29, 2016 Category: Drugs & Pharmacology Authors: Radomska-Leśniewska DM, Hevelke A, Skopiński P, Bałan B, Jóźwiak J, Rokicki D, Skopińska-Różewska E, Białoszewska A Tags: Pharmacol Rep Source Type: research

Potential role of spinal TRPA1 channels in antinociceptive tolerance to spinally administered morphine.
CONCLUSIONS: Antinociceptive morphine tolerance and up-regulation of spinal DAAO were attenuated in morphine-treated animals by blocking the spinal TRPA1. This finding suggests that spinal TRPA1 may contribute, at least partly, to facilitation of morphine antinociceptive tolerance through mechanisms that possibly involve TRPA1-mediated up-regulation of the astroglial DAAO, a generator of hydrogen peroxide, a pronociceptive compound acting also on TRPA1. PMID: 26922555 [PubMed - as supplied by publisher] (Source: Pharmacological Reports)
Source: Pharmacological Reports - February 29, 2016 Category: Drugs & Pharmacology Authors: Wei H, Wu HY, Fan H, Li TF, Ma AN, Li XY, Wang YX, Pertovaara A Tags: Pharmacol Rep Source Type: research

Common ABCB1 polymorphisms in Greek patients with chronic hepatitis C infection: A comparison with hyperlipidemic patients and the general population.
CONCLUSION: Our findings imply an influence of ABCB1 polymorphisms on HCV infectivity, possibly through an effect on lipid homeostasis. PMID: 26922556 [PubMed - as supplied by publisher] (Source: Pharmacological Reports)
Source: Pharmacological Reports - February 29, 2016 Category: Drugs & Pharmacology Authors: Gbandi E, Goulas A, Sevastianos V, Hadziyannis S, Panderi A, Koskinas J, Papatheodoridis G, Vasiliadis T, Agapakis D, Protopapas A, Ioannidou P, Zacharakis G, Sinakos E, Koutsounas S, Germanidis G Tags: Pharmacol Rep Source Type: research

Epicutaneous (EC) immunization with type II collagen (COLL II) induces CD4(+) CD8(+) T suppressor cells that protect from collagen-induced arthritis (CIA).
CONCLUSION: Maneuver of EC immunization with a protein antigen that induces suppressor cells to inhibit inflammatory responses may become an attractive, noninvasive, needle-free therapeutic method for different clinical situations. PMID: 26922557 [PubMed - as supplied by publisher] (Source: Pharmacological Reports)
Source: Pharmacological Reports - February 29, 2016 Category: Drugs & Pharmacology Authors: Marcińska K, Majewska-Szczepanik M, Lazar A, Kowalczyk P, Biała D, Woźniak D, Szczepanik M Tags: Pharmacol Rep Source Type: research

The effect of metformin on the hypothalamic-pituitary-thyroid axis in patients with type 2 diabetes and amiodarone-induced hypothyroidism.
CONCLUSIONS: The obtained results indicate that the effect of metformin on hypothalamic-pituitary-thyroid axis activity is partially related to thyroid function. Metformin treatment may bring clinical benefits to patients with amiodarone-induced hypothyroidism and poor tolerance of exogenous l-thyroxine. PMID: 26922558 [PubMed - as supplied by publisher] (Source: Pharmacological Reports)
Source: Pharmacological Reports - February 29, 2016 Category: Drugs & Pharmacology Authors: Krysiak R, Gilowska M, Szkróbka W, Okopień B Tags: Pharmacol Rep Source Type: research

The 28-day exposure to fenpropathrin decreases locomotor activity and reduces activity of antioxidant enzymes in mice brains.
CONCLUSIONS: The decrease of SOD activity in mice brains results from direct inhibition of the enzyme by Fen and/or increased utilization due to excessive free radical formation in conditions of Fen-induced oxidative stress. The reduction in GPx activity is probably due to limited glutathione availability. The reduced locomotor activity is a behavioral demonstration of Fen-induced damage in the dopaminergic system. PMID: 26922559 [PubMed - as supplied by publisher] (Source: Pharmacological Reports)
Source: Pharmacological Reports - February 29, 2016 Category: Drugs & Pharmacology Authors: Nieradko-Iwanicka B, Borzęcki A Tags: Pharmacol Rep Source Type: research

Anticancer agent 3-bromopyruvic acid forms a conjugate with glutathione.
CONCLUSIONS: 3-BP reacts with GSH in the absence of cells and intracellularly. This reaction appears to be the main cause of GSH loss in 3-BP treated cells. PMID: 26922560 [PubMed - as supplied by publisher] (Source: Pharmacological Reports)
Source: Pharmacological Reports - February 29, 2016 Category: Drugs & Pharmacology Authors: Sadowska-Bartosz I, Szewczyk R, Jaremko L, Jaremko M, Bartosz G Tags: Pharmacol Rep Source Type: research

Imatinib reduces cholesterol uptake and matrix metalloproteinase activity in human THP-1 macrophages.
säter D Abstract BACKGROUND: Imatinib mesylate (Glivec(®), formerly STI-571) is a selective tyrosine kinase inhibitor used for the treatment of chronic myeloid leukemia and gastrointestinal stromal tumors. However, there are reports suggesting that imatinib could be atheroprotective by lowering plasma low-density lipoprotein (LDL). AIM: To investigate the potential inhibitory effect of imatinib on cholesterol uptake in human macrophages as well as its effect on matrix metalloproteinase (MMP) activity. METHODS AND RESULTS: Uptake of fluorescence-labeled LDL was analyzed using flow cytometry. Macr...
Source: Pharmacological Reports - January 13, 2016 Category: Drugs & Pharmacology Authors: Gacic J, Vorkapic E, Olsen RS, Söderberg D, Gustafsson T, Geffers R, Skoglund K, Matussek A, Wågsäter D Tags: Pharmacol Rep Source Type: research

β-Elemene induces apoptosis of human rheumatoid arthritis fibroblast-like synoviocytes via reactive oxygen species-dependent activation of p38 mitogen-activated protein kinase.
CONCLUSIONS: Taken together, β-elemene is effective in inducing mitochondrial apoptosis of RA-FLS, which is mediated through induction of ROS formation and p38 MAPK activation. β-Elemene may thus have therapeutic benefits for RA. PMID: 26721344 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - January 13, 2016 Category: Drugs & Pharmacology Authors: Zou S, Wang C, Cui Z, Guo P, Meng Q, Shi X, Gao Y, Yang G, Han Z Tags: Pharmacol Rep Source Type: research

Enhanced pretreatment CD25 expression on peripheral blood CD4+ T cell predicts shortened survival in acute myeloid leukemia patients receiving induction chemotherapy.
CONCLUSIONS: Our data indicate that quantification of CD25 expression on peripheral blood CD4+ T cells could become a novel, easily accessible method of shortened survival prognostication of AML patients subjected to standard cytotoxic therapy. PMID: 26721345 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - January 13, 2016 Category: Drugs & Pharmacology Authors: Bołkun Ł, Rusak M, Eljaszewicz A, Pilz L, Radzikowska U, Łapuć I, Łuksza E, Dąbrowska M, Bodzenta-Łukaszyk A, Kłoczko J, Moniuszko M Tags: Pharmacol Rep Source Type: research

TBBPA causes neurotoxic and the apoptotic responses in cultured mouse hippocampal neurons in vitro.
CONCLUSION: We suggest that the H2DCFDA assay cannot be used to measure TBBPA-stimulated cell-mediated ROS production. PMID: 26721346 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - January 13, 2016 Category: Drugs & Pharmacology Authors: Szychowski KA, Wójtowicz AK Tags: Pharmacol Rep Source Type: research

β-Lapachone enhances Mre11-Rad50-Nbs1 complex expression in cisplatin-induced nephrotoxicity.
CONCLUSION: Although, it remains unclear how β-lapachone induces MRN complex expression, our findings suggest that β-lapachone might affect MRN complex expression and participate in DNA damage recovery in cisplatin-induced nephrotoxicity. PMID: 26721347 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - January 13, 2016 Category: Drugs & Pharmacology Authors: Kim TW, Kim YJ, Kim HT, Park SR, Jung JY Tags: Pharmacol Rep Source Type: research

Mixed MOP/DOP agonist biphalin elicits anti-transit effect in mouse models mimicking diarrhea-predominant irritable bowel syndrome symptoms.
CONCLUSION: Biphalin is an interesting template for novel opioid-based agents to be used in therapy of functional GI diseases. PMID: 26721348 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - January 13, 2016 Category: Drugs & Pharmacology Authors: Zielińska M, Jarmuż A, Sałaga M, Lipkowski AW, Fichna J Tags: Pharmacol Rep Source Type: research

Hydrogen sulfide inhibits endothelial nitric oxide formation and receptor ligand-mediated Ca(2+) release in endothelial and smooth muscle cells.
CONCLUSIONS: H2S antagonized Ca(2+) mobilization by receptor agonists and store-operated Ca(2+) entry thereby limiting eNOS activation and NO formation. The effect of H2S on Ca(2+) stores was not restricted to endothelial cells but was also observed in vascular and tracheal smooth muscle cells. PMID: 26721349 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - January 13, 2016 Category: Drugs & Pharmacology Authors: Kloesch B, Steiner G, Mayer B, Schmidt K Tags: Pharmacol Rep Source Type: research

Oral treatment with enrofloxacin early in life promotes Th2-mediated immune response in mice.
CONCLUSION: Our results clearly indicate that the immune system is more vulnerable to decreased bacterial exposure early in life that may promote development of allergy. PMID: 26721350 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - January 13, 2016 Category: Drugs & Pharmacology Authors: Strzępa A, Majewska-Szczepanik M, Kowalczyk P, Woźniak D, Motyl S, Szczepanik M Tags: Pharmacol Rep Source Type: research

An antihypertensive opioid: Biphalin, a synthetic non-addictive enkephalin analog decreases blood pressure in spontaneously hypertensive rats.
We examined cardiovascular effects of biphalin, a potentially non-addictive dimeric enkephalin analog, an agonist of opioid μ and δ receptors. METHODS: Biphalin was infused iv at 150μg/kg/h to anesthetized spontaneously hypertensive rats (SHR) and normotensive Wistar-Kyoto rats (WKY). Along with MAP and heart rate (HR), renal blood flow (RBF) and iliac blood flow (IBF, a measure of hind limb perfusion) were measured using Transonic probes on renal and iliac artery, respectively. The effects of biphalin were compared with those of intravenous morphine (1.5mg/kg/h). RESULTS: In two SHR groups biphalin d...
Source: Pharmacological Reports - January 13, 2016 Category: Drugs & Pharmacology Authors: Bądzyńska B, Lipkowski AW, Sadowski J Tags: Pharmacol Rep Source Type: research

Caffeine augments the antidepressant-like activity of mianserin and agomelatine in forced swim and tail suspension tests in mice.
CONCLUSION: The synergistic effect of caffeine and the tested drugs may be associated with their summative actions on monoaminergic neurotransmission. Caffeine-mianserin and caffeine-agomelatine interactions might have been of pharmacodynamic origin. PMID: 26721352 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - January 13, 2016 Category: Drugs & Pharmacology Authors: Poleszak E, Szopa A, Wyska E, Kukuła-Koch W, Serefko A, Wośko S, Bogatko K, Wróbel A, Wlaź P Tags: Pharmacol Rep Source Type: research

The anxiolytic-like activity of a novel N-cycloalkyl-N-benzoylpiperazine derivative.
Abstract BACKGROUND: Anxiety-related disorders are among the most common mental illnesses in the world for which benzodiazepines, buspirone and antidepressant drugs remain the first-line treatment. These drugs have good efficacy but they have numerous disadvantages, such as drug abuse potential, delayed onset of action or tolerance. A literature review reveals that a variety of piperazine derivatives may exhibit interesting pharmacological properties, including anxiolytic-like, antidepressant, nootropic and antinociceptive activities demonstrated in animal models, as well as an antioxidant capacity shown in some i...
Source: Pharmacological Reports - January 13, 2016 Category: Drugs & Pharmacology Authors: Strub DJ, Sałat K, Librowski T, Lochyński S, Gaweł M, Podkowa A Tags: Pharmacol Rep Source Type: research

Epileptogenic effects of G protein-coupled estrogen receptor 1 in the rat pentylenetetrazole kindling model of epilepsy.
In this study, 30 adult male Wistar albino rats were used. Due to intraperitoneal (ip) injections of a subconvulsant dose of PTZ (35mg/kg) which was repeated 12 times every 48h, chemical kindling occurred and kindling seizure was recorded for 30min. The rats were injected with 17β-estradiol (5μg/kg, ip) or G-1 (5μg/kg, ip), G-15 (5μg/kg, ip), Saline, Ethanol and Dimethyl sulfoxide (DMSO) 30min before each dose of PTZ. Observed seizures were classified between the phase 0-5. Thirty minutes later when the last 12. PTZ administration, all rats were sacrificed and the brain cortex, hippocampus sections were remov...
Source: Pharmacological Reports - January 13, 2016 Category: Drugs & Pharmacology Authors: Kurt AH, Bosnak M, Inan SY, Celik A, Uremis MM Tags: Pharmacol Rep Source Type: research

Renal vasculature reactivity to agonist of P2X7 receptor is increased in streptozotocin-induced diabetes.
CONCLUSIONS: It is possible that increased P2X7 receptor reactivity may be involved in the pathogenesis of diabetic nephropathy. PMID: 26721355 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - January 13, 2016 Category: Drugs & Pharmacology Authors: Kreft E, Kowalski R, Jankowski M, Szczepańska-Konkel M Tags: Pharmacol Rep Source Type: research

The effect of testosterone on cardiovascular risk factors in men with type 2 diabetes and late-onset hypogonadism treated with metformin or glimepiride.
CONCLUSIONS: Our results suggest that testosterone may bring more clinical benefits to metformin- than sulfonylurea-treated men with diabetes and LOH. PMID: 26721356 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - January 13, 2016 Category: Drugs & Pharmacology Authors: Krysiak R, Gilowski W, Okopień B Tags: Pharmacol Rep Source Type: research

Stimulation of the metabotropic glutamate (mGlu) 2 receptor attenuates the MK-801-induced increase in the immobility time in the forced swimming test in rats.
CONCLUSIONS: The present results suggest that stimulation of the mGlu2 receptor attenuates the increase in the immobility time in the forced swimming test elicited by subchronic administration of MK-801, and may be potentially useful for treatment of the negative symptoms of schizophrenia. PMID: 26721357 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - January 13, 2016 Category: Drugs & Pharmacology Authors: Kawaura K, Karasawa J, Hikichi H Tags: Pharmacol Rep Source Type: research

Ameliorative potential of pioglitazone and ceftriaxone alone and in combination in rat model of neuropathic pain: Targeting PPARγ and GLT-1 pathways.
CONCLUSION: Based on these results we propose that possible interplay between the neuroprotective effects of pioglitazone and ceftriaxone exists in suppressing the behavioral, biochemical, mitochondrial, neuroinflammatory and apoptotic cascades in spinal nerve ligation induced neuropathic pain in rats. PMID: 26721358 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - January 13, 2016 Category: Drugs & Pharmacology Authors: Pottabathini R, Kumar A, Bhatnagar A, Garg S, Ekavali E Tags: Pharmacol Rep Source Type: research

In vivo protective effect of betulinic acid on dexamethasone induced thymocyte apoptosis by reducing oxidative stress.
CONCLUSIONS: These findings reveal a protective capability of BA against Dex-induced cell death by reducing oxidative stress via mitochondrial mediated signal pathway which could be the potential mechanism underlying BA-elicited immunomodulation. PMID: 26721359 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - January 13, 2016 Category: Drugs & Pharmacology Authors: Yi J, Zhu R, Wu J, Wu J, Xia W, Zhu L, Jiang W, Xiang S, Tan Z Tags: Pharmacol Rep Source Type: research

Nuclear factor E2-related factor-2 (Nrf2) expression and regulation in male reproductive tract.
CONCLUSIONS: Components of the Nrf2/NRF2 system along with coordinated genes are expressed in testis and epididymis. Moreover, some interspecies differences between rat and human were observed, which may impact extrapolation of experimental data into clinical findings. Studies on animal model showed that corpus of epididymis is the most responsive part of the male reproductive tract to oltipraz exposure at the gene expression level. PMID: 26721360 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - January 13, 2016 Category: Drugs & Pharmacology Authors: Wajda A, Łapczuk J, Grabowska M, Słojewski M, Laszczyńska M, Urasińska E, Droździk M Tags: Pharmacol Rep Source Type: research

Hypoestrogenism alters mood: Ketamine reverses depressive-like behavior induced by ovariectomy in rats.
CONCLUSION: Similar to the literature, we showed the antidepressant effect of ketamine in depressive female rats which was induced by ovariectomy; including in female rats submitted to sham surgery that interestingly presented a premature menopausal. PMID: 26721361 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - January 13, 2016 Category: Drugs & Pharmacology Authors: da Silva Moreira SF, Nunes EA, Kuo J, de Macedo IC, Muchale A, de Oliveira C, Scarabelot VL, Marques Filho PR, Medeiros LF, Caumo W, Torres IL Tags: Pharmacol Rep Source Type: research

The effect of combined treatment with escitalopram and risperidone on the MK-801-induced changes in the object recognition test in mice.
CONCLUSIONS: The obtained results suggest that escitalopram may enhance the antipsychotic-like effect of risperidone in the animal tests used for evaluation of some cognitive symptoms of schizophrenia. PMID: 26721362 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - January 13, 2016 Category: Drugs & Pharmacology Authors: Rogóż Z, Kamińska K Tags: Pharmacol Rep Source Type: research

ET-1 mediates the release of reactive oxygen species and TNF-α in lung tissue by protein kinase C α and β1.
CONCLUSION: Endothelin-1 induces ROS generation, increases TNF-α level and lung edema via activation of PKC αβ1. PMID: 26721363 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - January 13, 2016 Category: Drugs & Pharmacology Authors: Gorąca A, Kleniewska P, Skibska B Tags: Pharmacol Rep Source Type: research

Therapeutic strategies for Alzheimer's disease in clinical trials.
This article presents current directions in the search for novel, potentially effective agents for the treatment of AD, as well as selected promising treatment strategies. These include agents acting upon the beta-amyloid, such as vaccines, antibodies and inhibitors or modulators of γ- and β-secretase; agents directed against the tau protein as well as compounds acting as antagonists of neurotransmitter systems (serotoninergic 5-HT6 and histaminergic H3). Ongoing clinical trials with Aβ antibodies (solanezumab, gantenerumab, crenezumab) seem to be promising, while vaccines against the tau protein (AADvac1 a...
Source: Pharmacological Reports - January 13, 2016 Category: Drugs & Pharmacology Authors: Godyń J, Jończyk J, Panek D, Malawska B Tags: Pharmacol Rep Source Type: research

A neutral effect of testosterone therapy on macroprolactin content in men with macroprolactinemia and late-onset hypogonadism.
CONCLUSIONS: Our results suggest a negligible effect of testosterone replacement on macroprolactin levels in macroprolactinemic men with late-onset hypogonadism. PMID: 26721365 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - January 13, 2016 Category: Drugs & Pharmacology Authors: Krysiak R, Kowalska B, Szkróbka W, Okopień B Tags: Pharmacol Rep Source Type: research

Pioglitazone, an anti-diabetic drug requires sustained MAPK activation for its anti-tumor activity in MCF7 breast cancer cells, independent of PPAR-γ pathway.
CONCLUSIONS: Pio suppresses the proliferation of MCF7 cells, at least partly by a PPAR-γ-independent mechanism involving the induction of p21 which in turn requires sustained activation of MAPK. These findings implicate the utility of Pio in the treatment of PPAR positive or negative human cancers and the development of a new class of compounds to enhance the effectiveness of Pio. PMID: 26721366 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - January 13, 2016 Category: Drugs & Pharmacology Authors: Kole L, Sarkar M, Deb A, Giri B Tags: Pharmacol Rep Source Type: research

Alzheimer-associated presenilin 2 gene is dysregulated in rat medial temporal lobe cortex after complete brain ischemia due to cardiac arrest.
CONCLUSIONS: Thus, presented changes suggest that the significant dysregulation of presenilin 2 gene may be connected with a response of neuronal cells to transient global brain ischemia due to cardiac arrest. Finally, the ischemia-induced gene dysregulation may play a key role in the late onset of Alzheimer's-type dementia. PMID: 26721367 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - January 13, 2016 Category: Drugs & Pharmacology Authors: Pluta R, Kocki J, Ułamek-Kozioł M, Bogucka-Kocka A, Gil-Kulik P, Januszewski S, Jabłoński M, Petniak A, Brzozowska J, Bogucki J, Furmaga-Jabłońska W, Czuczwar SJ Tags: Pharmacol Rep Source Type: research