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Therapeutic effect of aripiprazole in chronic schizophrenia is accompanied by anti-inflammatory activity.
Abstract BACKGROUND: Weight gain and metabolic abnormalities occur in chronic schizophrenia patients treated with atypical antipsychotics. The purpose of the study was to evaluate changes in serum levels of C-reactive protein (CRP), insulin and cytokines (IL-6, TNF-α, IL-1β, IFN-γ, sTNF-R1, IL-12, IL-23, IL-1Ra, TGF-β1, IL-4, and IL-10) after switching to aripiprazole. METHODS: Cytokine, hsCRP and insulin measurements were performed in patients (n=17) on day 0 and day 28 of the study using standard ELISA assays. The psychopathological status was assessed using PANSS. WC and BMI were meas...
Source: Pharmacological Reports - February 26, 2015 Category: Drugs & Pharmacology Authors: Sobiś J, Rykaczewska-Czerwińska M, Świętochowska E, Gorczyca P Tags: Pharmacol Rep Source Type: research

Ergotamine and nicergoline - Facts and myths.
Abstract Ergotamine, being a representative of naturally occurring ergoline alkaloids, derived from d-lysergic acid, and nicergoline, a d-lumilysergic acid derivative belonging to semi-synthetic ergot-derived alkaloids, display diversified affinity for adrenergic, serotoninergic, and dopamine receptors. Although introduction of triptans marginalized use of ergotamine, nicergoline is used in cerebral metabolic-vascular disorders, and dementia. Additionally, nicergoline exhibits a safety profile comparable to that of placebo, and none of the reviewed studies reported any incidence of fibrosis or ergotism with nicerg...
Source: Pharmacological Reports - February 26, 2015 Category: Drugs & Pharmacology Authors: Zajdel P, Bednarski M, Sapa J, Nowak G Tags: Pharmacol Rep Source Type: research

Thioflavin T effect in diabetic Wistar rats: Reporting the antihyperglycemic property of an amyloid probing dye.
CONCLUSION: ThT is suggested to be a potentially useful compound in treatment and prevention of diabetes and associated complications. PMID: 25712665 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - February 26, 2015 Category: Drugs & Pharmacology Authors: Najafian M, Amini S, Dehestani B, Parivar K, Ebrahim-Habibi A Tags: Pharmacol Rep Source Type: research

Omega-3 fatty acids prevent LPS-induced passive avoidance learning and memory and CaMKII-α gene expression impairments in hippocampus of rat.
CONCLUSION: Taken together, these data suggest that dietary omega-3 may improve cognitive function and provide a potential therapy for memory impairment due to neuroinflammation. PMID: 25712666 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - February 26, 2015 Category: Drugs & Pharmacology Authors: Dehkordi NG, Noorbakhshnia M, Ghaedi K, Esmaeili A, Dabaghi M Tags: Pharmacol Rep Source Type: research

The effect of interleukin-35 on the integrity, ICAM-1 expression and apoptosis of human aortic smooth muscle cells.
CONCLUSION: Our data suggest that IL-35 may be an agent affecting the inflammatory properties of AoSMCs and thus it may regulate immune homeostasis of the vascular wall. Hence, IL-35 may be a novel player affecting Ao-SMC-controlled arterial wall immune homeostasis. PMID: 25712667 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - February 26, 2015 Category: Drugs & Pharmacology Authors: Skowron W, Zemanek K, Wojdan K, Gorzelak P, Borowiec M, Broncel M, Chalubinski M Tags: Pharmacol Rep Source Type: research

Tectorigenin ablates the inflammation-induced epithelial-mesenchymal transition in a co-culture model of human lung carcinoma.
CONCLUSION: These results clearly demonstrate the therapeutic potential of tectorigenin to prevent lung cancer elicited inflammatory and pro-metastatic response in monocytes and warrants further investigations to elucidate its mechanism of action. PMID: 25712668 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - February 26, 2015 Category: Drugs & Pharmacology Authors: Amin A, Mokhdomi TA, Bukhari S, Wani SH, Wafai AH, Lone GN, Qadri A, Qadri RA Tags: Pharmacol Rep Source Type: research

Matrine suppresses proliferation and induces apoptosis in human cholangiocarcinoma cells through suppression of JAK2/STAT3 signaling.
CONCLUSION: Matrine can trigger mitochondrial apoptotic death of cholangiocarcinoma cells largely through inhibition of JAK2/STAT3 signaling. Therefore, matrine represents a potentially effective anticancer agent for cholangiocarcinoma. PMID: 25712669 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - February 26, 2015 Category: Drugs & Pharmacology Authors: Yang N, Han F, Cui H, Huang J, Wang T, Zhou Y, Zhou J Tags: Pharmacol Rep Source Type: research

The effects of vasoactive peptide urocortin 2 on hemodynamics in spontaneous hypertensive rat and the role of L-type calcium channel and CRFR2.
CONCLUSION: UCN2 can modulate electrical remodeling of the myocardium and hemodynamics in an experimental model of SHR via inhibition of L-type calcium channel and CRFR2 in cardiomyocytes. PMID: 25712670 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - February 26, 2015 Category: Drugs & Pharmacology Authors: Liu C, Liu X, Yang J, Duan Y, Yao H, Li F, Zhang X Tags: Pharmacol Rep Source Type: research

Involvement of nitridergic and opioidergic pathways in the antinociception of gabapentin in the orofacial formalin test in mice.
CONCLUSIONS: These results suggest that gabapentin produce antinociception partly via the activation nitridergic pathways and opioid system. PMID: 25712671 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - February 26, 2015 Category: Drugs & Pharmacology Authors: Miranda HF, Sierralta F, Lux S, Troncoso R, Ciudad N, Zepeda R, Zanetta P, Noriega V, Prieto JC Tags: Pharmacol Rep Source Type: research

Selenitetriglycerides-Redox-active agents.
CONCLUSIONS: The anticancer activity of Selol involves perturbation of the redox regulation in the androgen dependent hPCa (LNCaP) cells, but not in healthy cells. After Selol treatment, intracellular Eh has increased in tumors from -223mV to -175mV, while in serum it has decreased (-82mV vs -113mV). It shows significant changes Eh in the extra- and intracellular environment. The difference decreases from 141mV to 62mV. The changes suggest that a tumor cell was probably directed toward apoptosis. This is exemplified in a significant decrease in cancer tumor mass by approx. 17% after the three weeks of Selol administration....
Source: Pharmacological Reports - January 11, 2015 Category: Drugs & Pharmacology Authors: Flis A, Suchocki P, Królikowska MA, Suchocka Z, Remiszewska M, Śliwka L, Książek I, Sitarz K, Sochacka M, Hoser G, Anuszewska E, Wroczyński P, Jastrzębski Z Tags: Pharmacol Rep Source Type: research

Analgesic activity of new 8-methoxy-1,3-dimethyl-2,6-dioxo-purin-7-yl derivatives with carboxylic, ester or amide moieties.
CONCLUSION: The present study revealed that the presented compounds are new class of analgesic and anti-inflammatory agents and are worthy of the further evaluation regarding to their pharmacological properties. PMID: 25560569 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - January 11, 2015 Category: Drugs & Pharmacology Authors: Zygmunt M, Chłoń-Rzepa G, Sapa J, Pawłowski M Tags: Pharmacol Rep Source Type: research

H2S donors attenuate diabetic nephropathy in rats: Modulation of oxidant status and polyol pathway.
CONCLUSION: This study suggests a novel therapeutic approach for diabetic nephropathy using H2S donors. PMID: 25560570 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - January 11, 2015 Category: Drugs & Pharmacology Authors: Safar MM, Abdelsalam RM Tags: Pharmacol Rep Source Type: research

Multifactorial effects of vildagliptin added to ongoing metformin therapy in patients with type 2 diabetes mellitus.
CONCLUSIONS: Vildagliptin added to an ongoing metformin therapy allows to achieve better metabolic control parameters in comparison with a metformin monotherapy and the combination treatment is well tolerated and has a low risk of serious adverse effects. PMID: 25560571 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - January 11, 2015 Category: Drugs & Pharmacology Authors: Strózik A, Stęposz A, Basiak M, Drożdż M, Okopień B Tags: Pharmacol Rep Source Type: research

HMG-COA reductase inhibitors: An opportunity for the improvement of imatinib safety. An experimental study in rat pulmonary hypertension.
CONCLUSIONS: Statins may intensify the beneficial effects of imatinib in PAH, which may be due to the additional influence of statin on the decrease of platelet-derived growth factor (PDGF)-induced effects. These properties allow the dose of imatinib used in PAH treatment to be reduced and thereby might improve its safety profile. PMID: 25560572 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - January 11, 2015 Category: Drugs & Pharmacology Authors: Jasińska-Stroschein M, Owczarek J, Surowiecka A, Kącikowska J, Orszulak-Michalak D Tags: Pharmacol Rep Source Type: research

Impact of sparfloxacin on melanogenesis and antioxidant defense system in normal human melanocytes HEMa-LP - An in vitro study.
CONCLUSIONS: The observed sparfloxacin-dependent inhibition of melanogenesis and changes of antioxidant enzymes activities in human melanocytes give a new insight into the mechanism of fluoroquinolones toxicity directed to pigmented tissues. PMID: 25560573 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - January 11, 2015 Category: Drugs & Pharmacology Authors: Beberok A, Wrześniok D, Otręba M, Buszman E Tags: Pharmacol Rep Source Type: research

Effects of HMG-CoA reductase inhibitors on the pharmacokinetics of nifedipine in rats: Possible role of P-gp and CYP3A4 inhibition by HMG-CoA reductase inhibitors.
CONCLUSION: The increased bioavailability of nifedipine may be mainly due to inhibition of both P-gp in the small intestine and CYP3A subfamily-mediated metabolism of nifedipine in the small intestine and/or in the liver and to the reduction of the CL/F of nifedipine by fluvastatin and simvastatin. PMID: 25560574 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - January 11, 2015 Category: Drugs & Pharmacology Authors: Lee CK, Choi JS, Choi DH Tags: Pharmacol Rep Source Type: research

Dezocine prevents sufentanil-induced cough during general anesthesia induction: A randomized controlled trial.
Abstract BACKGROUND: Opioid-induced cough during induction of general anesthesia is a common phenomenon. Dezocine, a partial μ-receptors agonist and κ-receptors antagonist, has been documented effectively suppressing fentanyl-induced cough in general anesthesia induction. However, the effect of dezocine on sufentanil-induced cough is still unknown. METHODS: A total of 370 patients (American Society of Anesthesiologists physical status I-II), aged 18-70 years, undergoing elective surgery, were randomly divided into a control group (group C) and a dezocine group (group D) (n=185 in each group). Patient...
Source: Pharmacological Reports - January 11, 2015 Category: Drugs & Pharmacology Authors: Liu XS, Xu GH, Shen QY, Zhao Q, Cheng XQ, Zhang J, Gu EW Tags: Pharmacol Rep Source Type: research

Taking aim at a dynamic target: Noscapinoids as microtubule-targeted cancer therapeutics.
Abstract Noscapine and its synthetic derivatives called noscapinoids have been shown to possess potential anticancer properties. These alkaloids target microtubules and inhibit cell proliferation. Noscapinoids are microtubule poisons that induce minor alterations in the innate dynamic instability of microtubules leading to mitotic arrest and cell death. Over the past decade, a number of noscapine derivatives have been synthesized that, compared to the parent compound, show superior anticancer potential, enhanced tumor specificity and tumor regression, and little or no toxicity to normal tissues. Based on their suc...
Source: Pharmacological Reports - January 11, 2015 Category: Drugs & Pharmacology Authors: Lopus M, Naik PK Tags: Pharmacol Rep Source Type: research

Antinociceptive properties of N-Mannich bases derived from 3-substituted pyrrolidine-2,5-dione in the formalin model of persistent pain in mice.
Abstract BACKGROUND: Accumulated data indicate that anticonvulsants possess antinociceptive properties in rodent pain models. In view of the anticonvulsant activity demonstrated previously among N-Mannich bases derived from 3-mono- (1-6) and 3,3-disubstituted pyrrolidine-2,5-diones (7-14) their analgesic activity has been investigated in the formalin model of tonic pain in mice. METHODS: The compounds 1-14 were tested at doses equal to the respective ED50 values obtained earlier in the MES test. 0.5% formalin solution was given as intraplantar injections into the hind paw of the mouse and the duration of the ...
Source: Pharmacological Reports - January 11, 2015 Category: Drugs & Pharmacology Authors: Obniska J, Sałat K, Librowski T, Kamiński K, Lipkowska A, Wiklik B, Rybka S, Rapacz A Tags: Pharmacol Rep Source Type: research

Effects of incretin agonists on endothelial nitric oxide synthase expression and nitric oxide synthesis in human coronary artery endothelial cells exposed to TNFα and glycated albumin.
CONCLUSIONS: TNFα and GA decrease production of NO in HCAEC, presumably by inducing reactive oxygen species or eNOS uncoupling. Incretin agonists in tested concentrations in the presence of l-arginine were not able to reverse this effect and instead led to a further reduction in NO production. PMID: 25560578 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - January 11, 2015 Category: Drugs & Pharmacology Authors: Garczorz W, Francuz T, Siemianowicz K, Kosowska A, Kłych A, Aghdam MR, Jagoda K Tags: Pharmacol Rep Source Type: research

Pioglitazone prevents morphine antinociceptive tolerance via ameliorating neuroinflammation in rat cerebral cortex.
CONCLUSION: It is concluded that oral administration of pioglitazone attenuates morphine-induced tolerance. This effect of pioglitazone may be, at least in part, due to its anti-inflammatory property which suppressed the cortical pro-inflammatory cytokine and inhibited of nuclear factor-kappa B activity. PMID: 25560579 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - January 11, 2015 Category: Drugs & Pharmacology Authors: Ghavimi H, Charkhpour M, Ghasemi S, Mesgari M, Hamishehkar H, Hassanzadeh K, Arami S, Hassanzadeh K Tags: Pharmacol Rep Source Type: research

The MCP-1, CCL-5 and SDF-1 chemokines as pro-inflammatory markers in generalized anxiety disorder and personality disorders.
CONCLUSIONS: Our study has shown the need for determination of proinflammatory interleukins which are considered as biomarkers of personality disorders and generalized anxiety disorders. PMID: 25560580 [PubMed - as supplied by publisher] (Source: Pharmacological Reports)
Source: Pharmacological Reports - January 11, 2015 Category: Drugs & Pharmacology Authors: Ogłodek EA, Szota AM, Just MJ, Moś DM, Araszkiewicz A Tags: Pharmacol Rep Source Type: research

Mechanisms of morphine-venlafaxine interactions in diabetic neuropathic pain model.
CONCLUSIONS: The results of our study show that single administration of VFX potentiates antinociceptive action of morphine in DNPM. This effect is probably mediated by both, noradrenergic and serotonergic systems. On the other hand, 21-days administration of VFX significantly decreases analgesic action of MRF. Moreover, there is a possibility that VFX acts as an antagonist of N-methyl-d-aspartate receptors. PMID: 25560581 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - January 11, 2015 Category: Drugs & Pharmacology Authors: Cegielska-Perun K, Tatarkiewicz J, Siwek A, Dybała M, Bujalska-Zadrożny M Tags: Pharmacol Rep Source Type: research

Association of CYP2C8, CYP2C9 and CYP2J2 gene polymorphisms with myocardial infarction in South Indian population.
CONCLUSION: Our results suggest that individuals with any conventional risk factor for MI along with CYP2J2*7 variant allele may be predisposed to risk of MI in South Indian population. PMID: 25560582 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - January 11, 2015 Category: Drugs & Pharmacology Authors: Arun Kumar AS, Kumar SS, Umamaheswaran G, Kesavan R, Balachandar J, Adithan C Tags: Pharmacol Rep Source Type: research

Myelosuppressive and hepatotoxic potential of leflunomide and methotrexate combination in a rat model of rheumatoid arthritis.
CONCLUSIONS: In rats with AIA, current drug combinations provided higher therapeutic benefit compared to monotherapies, however, greater toxicities were observed. Therefore, continuous monitoring of hematologic parameters and liver function will be recommended in clinical settings. PMID: 25560583 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - January 11, 2015 Category: Drugs & Pharmacology Authors: Bilasy SE, Essawy SS, Mandour MF, Ali EA, Zaitone SA Tags: Pharmacol Rep Source Type: research

Pinocembrin attenuates hippocampal inflammation, oxidative perturbations and apoptosis in a rat model of global cerebral ischemia reperfusion.
CONCLUSIONS: Pinocembrin showed a neuroprotective effects through antioxidant, anti-inflammatory and antiapoptotic mechanisms. PMID: 25560584 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - January 11, 2015 Category: Drugs & Pharmacology Authors: Saad MA, Abdel Salam RM, Kenawy SA, Attia AS Tags: Pharmacol Rep Source Type: research

Anti-interleukin-1β antibody prevents the occurrence of repeated restraint stress-induced alterations in synaptic transmission and long-term potentiation in the rat frontal cortex.
CONCLUSIONS: These data point to an involvement of peripherally produced IL-1β in mediating the influence of repeated restraint stress on the functions of the frontal cortex. PMID: 25560585 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - January 11, 2015 Category: Drugs & Pharmacology Authors: Bobula B, Sowa J, Hess G Tags: Pharmacol Rep Source Type: research

The antinociceptive effect and mechanisms of action of pregabalin in mice.
CONCLUSIONS: We suggest that pregabalin (30 and 100mg/kg) presents central spinal but not central supraspinal antinociceptive effect and pregabalin 100mg/kg shows peripheral antinociceptive effect. The opioidergic pathway seems to mediate the central spinal antinociceptive effect of pregabalin while nitrergic and serotonergic pathways are not involved. PMID: 25560586 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - January 11, 2015 Category: Drugs & Pharmacology Authors: Kaygisiz B, Kilic FS, Senguleroglu N, Baydemir C, Erol K Tags: Pharmacol Rep Source Type: research

Inhibitory effects of imperatorin on voltage-gated K(+) channels and ATP-sensitive K(+) channels.
CONCLUSION: Our results suggest that imperatorin inhibited both Kv and KATP channels. PMID: 25560587 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - January 11, 2015 Category: Drugs & Pharmacology Authors: Wang YW, Yang CT, Chen YH, Gong CL, Chen YF, Kuo YH, Leung YM Tags: Pharmacol Rep Source Type: research

The effect of carvacrol on systemic inflammation in guinea pigs model of COPD induced by cigarette smoke exposure.
Abstract BACKGROUND: Chronic obstructive pulmonary disease (COPD) is a epidemic disease which is mainly due to cigarette smoking. The effect of carvacrol on systemic inflammation in guinea pig model of COPD was examined in the present study. METHODS: Guinea pigs of both sexes were divided into 6 groups, including: control, COPD, COPD+drinking water containing three concentrations of carvacrol and COPD+dexamethasone. Animals were exposed to cigarette smoke for 3 months in order to induce animal model of COPD. Weight changes, serum levels of IL-8 and malondialdehyde (MDA) as well as total and differential white...
Source: Pharmacological Reports - January 11, 2015 Category: Drugs & Pharmacology Authors: Mahtaj LG, Feizpour A, Kianmehr M, Soukhtanloo M, Boskabady MH Tags: Pharmacol Rep Source Type: research

The effect of central noradrenergic system lesion on dopamine (DA) and serotonin (5-HT) synthesis rate following administration of 5-HT3 receptor ligands in chosen parts of the rat brain.
CONCLUSION: Damage to the central noradrenergic system in rat newborns, through altered reactivity of central 5-HT3 receptors, results in permanent disorders in serotoninergic transmission in hippocampus and cerebellum as well as dopaminergic transmission in hippocampus, which may attenuate the activity of the descending pathways that derive from these structures. PMID: 25560589 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - January 11, 2015 Category: Drugs & Pharmacology Authors: Roczniak W, Babuśka-Roczniak M, Kwapuliński J, Brodziak-Dopierała B, Widuchowski W, Cipora E, Nowak P, Oświęcimska JM Tags: Pharmacol Rep Source Type: research

Synergistic antinociceptive interactions between fospropofol and alfentanil in mice.
Abstract BACKGROUND: Combination therapy, which provides the opportunity to achieve optimal analgesia with reduced side effects at lower drug doses, is a valid approach for the treatment of pain. The analgesic interaction between fospropofol and alfentanil has not been investigated till date. We sought to determine the nature of the interaction between fospropofol and alfentanil in mice models of the formalin test, hot-plate test and the tail-flick test. METHODS: The effects of fospropofol, alfentanil and their combinations were examined in the formalin-induced paw inflammatory hyperalgesia, the hot-plate tes...
Source: Pharmacological Reports - January 11, 2015 Category: Drugs & Pharmacology Authors: Zhao C, Jia N, Wang C, Li Y, Li R, Cui J, Cao S, Wang L, Wu Y, Wen A Tags: Pharmacol Rep Source Type: research

Antidepressant-like activity of a new piperazine derivative of xanthone in the forced swim test in mice: The involvement of serotonergic system.
CONCLUSIONS: We demonstrated that HBK-6 has a potent antidepressant-like activity in FST, stronger than that of FX and RX, and seems to mediate its effect through serotonergic system. Moreover, at antidepressant-like doses it does not show neurotoxic properties. Given the promising results, HBK-6 may have potential in the treatment of depression, but this needs extended studies. PMID: 25560591 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - January 11, 2015 Category: Drugs & Pharmacology Authors: Pytka K, Rapacz A, Zygmunt M, Olczyk A, Waszkielewicz A, Sapa J, Filipek B Tags: Pharmacol Rep Source Type: research

Crystal structure of 1-methyl-4-methyl-sulfanyl-1H-pyrazolo-[3,4-d]pyrimidine.
Abstract In the title compound, C7H8N4S, the non-H atoms of the pyrazolo-[3,4-d]pyrimidine ring system and the methyl-sulfanyl group lie on a crystallographic mirror plane. In the crystal, mol-ecules are linked via a number of π-π inter-actions [centroid-centroid distances vary from 3.452 (7) to 3.6062 (8) Å], forming a three-dimensional structure. PMID: 25553046 [PubMed] (Source: Pharmacological Reports)
Source: Pharmacological Reports - December 1, 2014 Category: Drugs & Pharmacology Authors: El Fal M, Ramli Y, Essassi el M, Saadi M, El Ammari L Tags: Acta Crystallogr Sect E Struct Rep Online Source Type: research

CP55,940 attenuates spatial memory retrieval in mice.
CONCLUSION: Since the attenuated psychomotor activity after a dose of 0.125mg/kg did not interfere with memory retrieval, we assume that the impairment of spatial memory observed after the highest dose of CP55,940 (0.25mg/kg) was exerted by its influence on cognitive processes, however, the impact on locomotion could not be excluded. PMID: 25443717 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - December 1, 2014 Category: Drugs & Pharmacology Authors: Bialuk I, Dobosz K, Potrzebowski B, Winnicka MM Tags: Pharmacol Rep Source Type: research

Antiproliferative effect induced by novel imidazoline S43126 in PC12 cells is mediated by ROS, stress activated MAPKs and caspases.
CONCLUSION: Our data showed that the effects of S43126 on PC12 cell death were partly mediated by ROS production, MAPK and caspase activation. These results further indicate an emerging role for I1R in apoptotic processes. PMID: 25443718 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - December 1, 2014 Category: Drugs & Pharmacology Authors: McLean LS, Crane L, Baziard-Mouysset G, Edwards LP Tags: Pharmacol Rep Source Type: research

Chronic administration of phenytoin induces efflux transporter overexpression in rats.
CONCLUSIONS: Overexpression of efflux transporters can be mediated by inducer agents like PHT in a local-concentration dependent manner, and it is reversible once the substance is removed from the body. The recovery of basal Pgp expression could allow the design of dosing schedules that optimize anticonvulsant therapy. PMID: 25443719 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - December 1, 2014 Category: Drugs & Pharmacology Authors: Alvariza S, Fagiolino P, Vázquez M, Feria-Romero I, Orozco-Suárez S Tags: Pharmacol Rep Source Type: research

Rupatadine effectively prevents the histamine-induced up regulation of histamine H1R and bradykinin B2R receptor gene expression in the rat paw.
CONCLUSION: Rupatadine has a suppressing effect on H1R and B2R gene expression which could add to its efficacy towards allergy and allergy-like conditions. PMID: 25443720 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - December 1, 2014 Category: Drugs & Pharmacology Authors: Molyva D, Kalokasidis K, Poulios C, Dedi H, Karkavelas G, Mirtsou V, Goulas A Tags: Pharmacol Rep Source Type: research

Potential of metabolomics in preclinical and clinical drug development.
Abstract Metabolomics is an upcoming technology system which involves detailed experimental analysis of metabolic profiles. Due to its diverse applications in preclinical and clinical research, it became an useful tool for the drug discovery and drug development process. This review covers the brief outline about the instrumentation and interpretation of metabolic profiles. The applications of metabolomics have a considerable scope in the pharmaceutical industry, almost at each step from drug discovery to clinical development. These include finding drug target, potential safety and efficacy biomarkers and mechanis...
Source: Pharmacological Reports - December 1, 2014 Category: Drugs & Pharmacology Authors: Kumar B, Prakash A, Ruhela RK, Medhi B Tags: Pharmacol Rep Source Type: research

Role of TRPV1 and ASIC3 in formalin-induced secondary allodynia and hyperalgesia.
CONCLUSIONS: Data suggest that TRPV1 and ASIC3 participate in the development and maintenance of long-lasting secondary allodynia and hyperalgesia induced by formalin in rats. The use of TRPV1 and ASIC3 antagonists by peripheral administration could prove useful to treat chronic pain. PMID: 25443722 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - December 1, 2014 Category: Drugs & Pharmacology Authors: Martínez-Rojas VA, Barragán-Iglesias P, Rocha-González HI, Murbartián J, Granados-Soto V Tags: Pharmacol Rep Source Type: research

Concentration of Il-1β, Il-2, Il-6, TNFα in the blood serum in children with generalized epilepsy treated by valproate.
Concentration of Il-1β, Il-2, Il-6, TNFα in the blood serum in children with generalized epilepsy treated by valproate. Pharmacol Rep. 2014 Dec;66(6):972-5 Authors: Steinborn B, Zarowski M, Winczewska-Wiktor A, Wójcicka M, Młodzikowska-Albrecht J, Losy J Abstract BACKGROUND: The aim of the study was the comparison of concentrations of IL-1β, IL-2, IL-6 and TNFα before and after valproate (VPA) treatment in blood serum in patients with generalized seizures diagnosed and treated in the Department of Developmental Neurology, Poznan University of Medical Sciences from January...
Source: Pharmacological Reports - December 1, 2014 Category: Drugs & Pharmacology Authors: Steinborn B, Zarowski M, Winczewska-Wiktor A, Wójcicka M, Młodzikowska-Albrecht J, Losy J Tags: Pharmacol Rep Source Type: research

Evaluation of l-arginine on kidney function and vascular reactivity following ischemic injury in rats: Protective effects and potential interactions.
CONCLUSIONS: The protective effect of l-arginine may result from the interaction between NO and ROS and increased NO bioavailability. The protective effects of combined celecoxib and l-arginine against IRI could be attributed to their antioxidant activity which exceeded that of ascorbic acid. PMID: 25443724 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - December 1, 2014 Category: Drugs & Pharmacology Authors: Senbel AM, Omar AG, Abdel-Moneim LM, Mohamed HF, Daabees TT Tags: Pharmacol Rep Source Type: research

The effect of risperidone on the mirtazapine-induced changes in extracellular monoamines in the rat frontal cortex.
CONCLUSIONS: Our data indicate that the increase of cortical extracellular levels of DA and NA by combined administration of mirtazapine and risperidone may be of crucial importance to the pharmacotherapy of drug resistant depression, and that, among other mechanisms, 5-HT1A, 5-HT2A, α2-adrenergic and histamine H1 receptors may play some role in this effect. PMID: 25443725 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - December 1, 2014 Category: Drugs & Pharmacology Authors: Kamińska K, Gołembiowska K, Rogóż Z Tags: Pharmacol Rep Source Type: research

Hypotensive effects of omentin-1 related to increased adiponectin and decreased interleukin-6 in intra-thoracic pericardial adipose tissue.
Abstract BACKGROUND: Omentin is an adipokine expressed in visceral adipose tissue (VAT). In vitro studies demonstrated that omentin induces vasorelaxation in isolated rat mesenteric arteries, and in vivo studies showed inhibition of agonist-induced increases in blood pressure, possibly mediated by nitric oxide (NO)-dependent mechanisms. METHODS: We investigated, in normotensive rats, the effects of subacute omentin-1 administration [8μg/kg, intraperitoneally (ip), once daily for 14 days] on cardiac activity, blood pressure, plasma concentration of l-citrulline (as a marker of NO production from l-arginine)...
Source: Pharmacological Reports - December 1, 2014 Category: Drugs & Pharmacology Authors: Brunetti L, Leone S, Orlando G, Ferrante C, Recinella L, Chiavaroli A, Di Nisio C, Shohreh R, Manippa F, Ricciuti A, Vacca M Tags: Pharmacol Rep Source Type: research

Analgesic and anti-inflammatory activity of 7-substituted purine-2,6-diones.
CONCLUSION: Active compounds (1-6) inhibited the PDE activity, while compound 1 significantly inhibited the PDE4B activity, what may suggest that this mechanism may be involved in their analgesic/anti-inflammatory properties. PMID: 25443727 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - December 1, 2014 Category: Drugs & Pharmacology Authors: Zygmunt M, Chłoń-Rzepa G, Sapa J Tags: Pharmacol Rep Source Type: research

Integrated workflow for quantitative phosphoproteomic analysis of the selected brain structures in development of morphine dependence.
CONCLUSIONS: The proposed MS-based workflow with following data analysis is efficient method for quantitative phosphoproteomic analysis: PMID: 25443728 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - December 1, 2014 Category: Drugs & Pharmacology Authors: Sucharski F, Noga MJ, Suder P, Kotlińska J, Silberring J Tags: Pharmacol Rep Source Type: research

Ligand-directed trafficking of receptor stimulus.
Abstract GPCRs are seven transmembrane-spanning receptors that convey specific extracellular stimuli to intracellular signalling. They represent the largest family of cell surface proteins that are therapeutically targeted. According to the traditional two-state model of receptor theory, GPCRs were considered as operating in equilibrium between two functional conformations, an active (R*) and inactive (R) state. Thus, it was assumed that a GPCR can exist either in an "off" or "on" conformation causing either no activation or equal activation of all its signalling pathways. Over the past several...
Source: Pharmacological Reports - December 1, 2014 Category: Drugs & Pharmacology Authors: Chilmonczyk Z, Bojarski AJ, Sylte I Tags: Pharmacol Rep Source Type: research

Antiarrhythmic efficacy of CPUY102122, a multiple ion channel blocker, on rabbits with ischemia/reperfusion injury.
CONCLUSIONS: These results indicated that CY22 has both antiarrhythmic and cardiovascular protective effects partly by blocking IKr, the production of antioxidants and protection of Cx43. PMID: 25443730 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - December 1, 2014 Category: Drugs & Pharmacology Authors: Wang M, Shan J, Yang Q, Ma X, Jin S, Guo X, You Q, Tang Y Tags: Pharmacol Rep Source Type: research

The effects of ifenprodil on the activity of antidepressant drugs in the forced swim test in mice.
CONCLUSION: The concomitant administration of certain commonly prescribed antidepressant drugs that affect the serotonergic neurotransmission (i.e., typical tricyclic antidepressants and selective serotonin reuptake inhibitors) with a negative modulator selectively binding to the GluN1/N2B subunits of the NMDA receptor complex (i.e., ifenprodil) may induce a more pronounced antidepressant-like effect than monotherapy. However, these findings still need to be confirmed in further experiments. PMID: 25443731 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - December 1, 2014 Category: Drugs & Pharmacology Authors: Poleszak E, Wośko S, Serefko A, Wlaź A, Kasperek R, Dudka J, Wróbel A, Nowak G, Wlaź P Tags: Pharmacol Rep Source Type: research

Chronotherapeutic effect of fisetin on expression of urea cycle enzymes and inflammatory markers in hyperammonaemic rats.
CONCLUSIONS: Fisetin could exhibit anti-hyperammonaemic effect owing to its anti-oxidant and cytoprotective influences. The temporal variation in the effect of fisetin could be due to the (i) chronopharmacological, chronopharmacokinetic properties of fisetin and (ii) modulations in the endogenous circadian rhythms of urea cycle enzymes, brain markers, redox enzymes and renal clearance during hyperammonaemia by fisetin. However, future studies in these lines are necessitated. PMID: 25443732 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - December 1, 2014 Category: Drugs & Pharmacology Authors: Subramanian P, Jayakumar M, Jayapalan JJ, Hashim OH Tags: Pharmacol Rep Source Type: research