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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.
CONCLUSION: The results of current study suggest that administration of Dezocine 0.1mg/kg may effectively prevent the occurrence and reflex degree of sufentanil-induced irritating cough in general anesthesia induction in patients. PMID: 25560575 [PubMed - in process] (Source: Pharmacological Reports)
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 succ...
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.
CONCLUSIONS: The results of the research indicate that some of the investigated compounds reduced effectively either both phases of the test or were able to attenuate pain during only the acute or late phase of the formalin test. These properties, which are particularly strong in case of the compounds 1-3, 5, 6, 9 and 14, might be relevant for the development of novel analgesic-active compounds and their possible use in neuropathic pain syndromes. PMID: 25560577 [PubMed - in process] (Source: Pharmacological Reports)
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.
CONCLUSION: These results showed a preventive effect of the carvacrol on all measured parameter in COPD guinea pigs which was comparable to the effect of dexamethasone at used concentrations. PMID: 25560588 [PubMed - in process] (Source: Pharmacological Reports)
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.
CONCLUSIONS: The results demonstrate that fospropofol and alfentanil provide synergistic antinociceptive interactions in the formalin, hot-plate, and tail-flick tests. The observed synergistic interaction between fospropofol and alfentanil are indicative of the effectiveness of the combination treatment in pain management and should be explored further in patients undergoing minor surgical procedures. PMID: 25560590 [PubMed - in process] (Source: Pharmacological Reports)
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 mechanism...
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.
CONCLUSIONS: The serum level of pro-inflammatory IL-6 in patients with generalized epilepsy decreased in statistically significant way during VPA therapy, so the anti-inflammatory properties of VPA are also important for the effective control of seizure. Due to the incompatibility of reports on the influence of VPA on cytokine system in patients with generalized epilepsy, this problem needs more investigations, especially in the group of children. PMID: 25443723 [PubMed - in process] (Source: Pharmacological Reports)
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.
CONCLUSION: We conclude that the hypotensive effects of omentin-1 could be driven by stimulated production of NO in the vascular system, possibly related to increased adiponectin and decreased IL-6 mRNA in PAT. PMID: 25443726 [PubMed - in process] (Source: Pharmacological Reports)
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 years it has become ...
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

Ramipril/amlodipine single pill - Effectiveness, tolerance and patient satisfaction with antihypertensive therapy in relation to nutritional status.
CONCLUSIONS: The effectiveness of therapy with ramipril/amlodipine FDC in the study population was high, but slightly lower in overweigh and obese. This FDC was well tolerated and a significant number of patients satisfied with the therapy regardless of nutritional status. Although the perceived tolerance and satisfaction with treatment were lower in obese and overweight than in normal weight patients; the incidence of AE and perceived benefit from the use of a single-pill, compared to multiple tablets, were comparable irrespective of nutritional status. PMID: 25443733 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - December 1, 2014 Category: Drugs & Pharmacology Authors: Olszanecka-Glinianowicz M, Smertka M, Almgren-Rachtan A, Chudek J Tags: Pharmacol Rep Source Type: research

Alleviation of hepatic injury by chrysin in cisplatin administered rats: Probable role of oxidative and inflammatory markers.
CONCLUSION: The results of the present study demonstrate that oxidative stress and inflammation are closely associated with cisplatin-induced toxicity and chrysin shows the protective efficacy against cisplatin-induced hepatotoxicity possibly via attenuating the oxidative stress and inflammatory response. PMID: 25443734 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - December 1, 2014 Category: Drugs & Pharmacology Authors: Rehman MU, Ali N, Rashid S, Jain T, Nafees S, Tahir M, Khan AQ, Lateef A, Khan R, Hamiza OO, Kazim S, Qamar W, Sultana S Tags: Pharmacol Rep Source Type: research

The anti-cancer actions of O6-methylguanine-DNA-methyltransferase in relation to colon polyps.
CONCLUSIONS: We concluded that high frequency of 84F allele in the group of patients may suggest the role of the MGMT variant in colon polyps etiology. PMID: 25443735 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - December 1, 2014 Category: Drugs & Pharmacology Authors: Kycler W, Korski K, Loziński C, Teresiak-Mańczak A, Przybyła A, Mackiewicz A, Cybulski Z, Lamperska K Tags: Pharmacol Rep Source Type: research

Modulating actions of NMDA receptors on pronociceptive effects of locally injected remifentanil in diabetic rats.
CONCLUSIONS: The hyperalgesic and allodynic actions of locally treated remifentanil may decrease in diabetic conditions. Increases in NMDA receptors activation, reactive oxygen species production and NO release may modify the sensitivity to remifentanil in diabetes induced neuropathic pain states. PMID: 25443736 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - December 1, 2014 Category: Drugs & Pharmacology Authors: Mert T, Oksuz H, Tugtag B, Kilinc M, Senoglu N, Bilgin R Tags: Pharmacol Rep Source Type: research

Apoptotic mechanisms of the biotechnologically produced arylnaphtalene lignan justicidin B in the acute myeloid leukemia-derived cell line HL-60.
CONCLUSION: The potent activity at low micromolar concentration and the feasibility of biotechnological production of justicidin B implies that there is enormous scope in its further evaluation as possible antineoplastic drug candidate. PMID: 25443737 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - December 1, 2014 Category: Drugs & Pharmacology Authors: Momekov G, Yossifov D, Guenova M, Michova A, Stoyanov N, Konstantinov S, Ionkov T, Sacheva P, Ionkova I Tags: Pharmacol Rep Source Type: research

Daytime sleepiness and EEG abnormalities in patients treated with second generation antipsychotic agents.
CONCLUSIONS: Although antipsychotics may have profound effects on EEG patients with schizophrenia do not have higher daytime sleepiness than patients with anxiety/personality disorders. Patients with schizophrenia may compensate sedative effects of antipsychotic treatment with sleep duration prolongation and report even less sleepiness than non-psychotic patients. PMID: 25443738 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - December 1, 2014 Category: Drugs & Pharmacology Authors: Okruszek L, Jernajczyk W, Wierzbicka A, Waliniowska E, Jakubczyk T, Jarema M, Wichniak A Tags: Pharmacol Rep Source Type: research

Celecoxib prevents colitis associated colon carcinogenesis: An upregulation of apoptosis.
CONCLUSION: The chemopreventive action of celecoxib in colitis mediated colon carcinogenesis may include the regulation of DNA mismatch repair enzymes, cell cycle check points, cell proliferation and apoptosis. PMID: 25443739 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - December 1, 2014 Category: Drugs & Pharmacology Authors: Setia S, Nehru B, Sanyal SN Tags: Pharmacol Rep Source Type: research

Antithyroid effects of naringin, hesperidin and rutin in l-T4 induced hyperthyroid rats: Possible mediation through 5'DI activity.
CONCLUSION: Rutin, naringin and hesperidin have the potential to inhibit thyroid functions without hepatotoxicity and the effects are possibly mediated through their free radical scavenging action as evidenced by EPR study. From the comparative analyses of the results, rutin appeared to be the most effective one suggesting its better antithyroid and antioxidative potential over other two. PMID: 25443740 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - December 1, 2014 Category: Drugs & Pharmacology Authors: Panda S, Kar A Tags: Pharmacol Rep Source Type: research

Interactions between levetiracetam and cardiovascular drugs against electroconvulsions in mice.
CONCLUSIONS: Although experimental data can be hardly extrapolated to clinical practice, it is suggested that perindopril arginine may positively influence the anticonvulsant action of LEV in epileptic patients. The use of losartan potassium, candesartan cilexetil, captopril, hydrochlorothiazide or ethacrynic acid in patients treated with LEV seems neutral regarding its anticonvulsant activity. PMID: 25443741 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - December 1, 2014 Category: Drugs & Pharmacology Authors: Lukawski K, Raszewski G, Czuczwar SJ Tags: Pharmacol Rep Source Type: research