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[PMID]: 29414655
[Au] Autor:Podmolíková L; Mukanyangezi MF; Nieto-Marín P; Giglio D
[Ad] Address:Department of Pharmacology, University of Gothenburg, Gothenburg, Sweden; Faculty of Medicine, Charles University, Hradec Králové, Czech Republic.
[Ti] Title:Cholinergic regulation of proliferation of the urothelium in response to E. coli lipopolysaccharide exposition.
[So] Source:Int Immunopharmacol;56:222-229, 2018 Mar.
[Is] ISSN:1878-1705
[Cp] Country of publication:Netherlands
[La] Language:eng
[Ab] Abstract:How the proliferation of the urothelium is regulated is known to a little degree. E. coli lipopolysaccharide (LPS) activates the innate immune response of the urinary bladder via the Toll-like receptor 4 (TLR4) on the urothelium but induces also urothelial proliferation. We wanted to assess whether muscarinic receptors are involved in the regulation of urothelial proliferation triggered by LPS stimulation. Female Fischer 344 rats were instilled with LPS or saline (control) in the urinary bladder in the absence or presence of muscarinic receptor blockade with atropine and regeneration of the urothelium was assessed 4h and 24h later. In the Fischer 344 bladder, urothelial thinning and urothelial caspase 3 up-regulation occurred at 4h after LPS urinary bladder instillation, which were totally blocked in rats pre-treated with atropine. TLR4 was only expressed in blood vessels in the Fischer 344 bladder, while it was also expressed in umbrella cells in the Sprague-Dawley bladder. Proliferation (Ki67 incorporation) of the human urothelial cell line UROtsa was reduced in the presence of the muscarinic receptor antagonists methoctramine (M2/M4-selective) and pirenzepine (M1/M4-selective), while proliferation instead was enhanced in the presence of atropine. In UROtsa cells exposed to LPS for 24h, 4-DAMP (M3/M1/M5-selective) inhibited instead proliferation. In conclusion, muscarinic receptors regulate urothelial proliferation and LPS may induce urothelial apoptosis via muscarinic receptor-dependent pathways. Our findings also suggest that species differences exist in the expressional pattern of TLR4 in the urothelium.
[Pt] Publication type:JOURNAL ARTICLE
[Em] Entry month:1802
[Cu] Class update date: 180227
[Lr] Last revision date:180227
[St] Status:In-Process

  2 / 5093 MEDLINE  
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[PMID]: 29290419
[Au] Autor:Heijman J; Kirchner D; Kunze F; Chrétien EM; Michel-Reher MB; Voigt N; Knaut M; Michel MC; Ravens U; Dobrev D
[Ad] Address:Institute of Pharmacology, West German Heart and Vascular Center, Faculty of Medicine, University Duisburg-Essen, Essen, Germany; Department of Cardiology, Cardiovascular Research Institute Maastricht, Maastricht University, Maastricht, The Netherlands.
[Ti] Title:Muscarinic type-1 receptors contribute to I in human atrial cardiomyocytes and are upregulated in patients with chronic atrial fibrillation.
[So] Source:Int J Cardiol;255:61-68, 2018 Mar 15.
[Is] ISSN:1874-1754
[Cp] Country of publication:Netherlands
[La] Language:eng
[Ab] Abstract:BACKGROUND: Basal and acetylcholine-gated inward-rectifier K -currents (I and I , respectively) are altered in atrial fibrillation (AF). G -protein-coupled muscarinic (M) receptors type-2 are considered the predominant receptors activating I . Although a role for G -coupled non-M -receptor subtypes has been suggested, the precise regulation of I by multiple M-receptor subtypes in the human atrium is unknown. Here, we investigated M -receptor-mediated I regulation and its remodeling in chronic AF (cAF). METHODS AND RESULTS: M -receptor mRNA and protein abundance were increased in atrial cardiomyocyte fractions and atrial homogenates from cAF patients, whereas M -receptor levels were unchanged. The regulation of I by M -receptors was investigated in right-atrial cardiomyocytes using two applications of the M-receptor agonist carbachol (CCh, 2µM), with pharmacological interventions during the second application. CCh application produced a rapid current increase (Peak-I ), which declined to a quasi-steady-state level (Qss-I ). In sinus rhythm (Ctl) the selective M -receptor antagonists pirenzepine (10nM) and muscarinic toxin-7 (MT-7, 10nM) significantly inhibited CCh-activated Peak-I , whereas in cAF they significantly reduced both Peak- and Qss-I , with no effects on basal inward-rectifier currents in either group. Conversely, the selective M -receptor agonist McN-A-343 (100µM) induced a current similar to the CCh-activated current in Ctl atrial cardiomyocytes pretreated with pertussis toxin to inhibit M -receptor-mediated G -protein signaling, which was abolished by MT-7. Computational modeling indicated that M - and M -receptors redundantly activate I to abbreviate APD, albeit with predominant effects of M -receptors. CONCLUSION: Our data suggest that G -coupled M -receptors also regulate human atrial I and that their relative contribution to I activation is increased in cAF patients. We provide novel insights about the role of non-M -receptors in human atrial cardiomyocytes, which may have important implications for understanding AF pathophysiology.
[Pt] Publication type:JOURNAL ARTICLE
[Em] Entry month:1801
[Cu] Class update date: 180218
[Lr] Last revision date:180218
[St] Status:In-Data-Review

  3 / 5093 MEDLINE  
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[PMID]: 29267212
[Au] Autor:Zhang M; Vrolijk M; Haenen GRMM
[Ad] Address:Department of Pharmacology and Toxicology, Maastricht University, 6200 MD Maastricht, The Netherlands. z.ming@maastrichtuniversity.nl.
[Ti] Title:The Screening of Anticholinergic Accumulation by Traditional Chinese Medicine.
[So] Source:Int J Mol Sci;19(1), 2017 Dec 21.
[Is] ISSN:1422-0067
[Cp] Country of publication:Switzerland
[La] Language:eng
[Ab] Abstract:Many Western drugs can give rise to serious side effects due to their ability to bind to acetylcholine receptors in the brain. This aggravates when they are combined, which is known as anticholinergic accumulation (AA). Some bioactives in Traditional Chinese Medicine (TCM) are known to block acetylcholine receptors and thus potentially cause AA. The AA of TCM was screened by quantifying the displacement of [³H] pirenzepine on acetylcholine receptors in a rat brain homogenate. We used a new unit to express AA, namely the Total Atropine Equivalents (TOAT). The TOAT of various herbs used in TCM was very diverse and even negative for some herbs. This is indicative for the broadness of the pallet of ingredients used in TCM. Three TCM formulas were screened for AA: Ma Huang Decotion (MHD), Antiasthma Simplified Herbal Medicine intervention (ASHMI), and Yu Ping Feng San (YPFS). The TOAT of ASHMI was indicative for an additive effect of herbs used in it. Nevertheless, it can be calculated that one dose of ASHMI is probably too low to cause AA. The TOAT of YPFS was practically zero. This points to a protective interaction of AA. Remarkably, MHD gave a negative TOAT, indicating that the binding to the acetylcholine receptors was increased, which also circumvents AA. In conclusion, our results indicate that TCM is not prone to give AA and support that there is an intricate interaction between the various bioactives in TCM to cure diseases with minimal side effects.
[Pt] Publication type:JOURNAL ARTICLE
[Em] Entry month:1712
[Cu] Class update date: 180213
[Lr] Last revision date:180213
[St] Status:In-Process

  4 / 5093 MEDLINE  
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[PMID]: 29204068
[Au] Autor:Liu Y; Wang Y; Lv H; Jiang X; Zhang M; Li X
[Ad] Address:Department of Ophthalmology, Peking University Third Hospital, Beijing, China.
[Ti] Title:α-adrenergic agonist brimonidine control of experimentally induced myopia in guinea pigs: A pilot study.
[So] Source:Mol Vis;23:785-798, 2017.
[Is] ISSN:1090-0535
[Cp] Country of publication:United States
[La] Language:eng
[Ab] Abstract:Purpose: To investigate the efficacy of α-adrenergic agonist brimonidine either alone or combined with pirenzepine for inhibiting progressing myopia in guinea pig lens-myopia-induced models. Methods: Thirty-six guinea pigs were randomly divided into six groups: Group A received 2% pirenzepine, Group B received 0.2% brimonidine, Group C received 0.1% brimonidine, Group D received 2% pirenzepine + 0.2% brimonidine, Group E received 2% pirenzepine + 0.1% brimonidine, and Group F received the medium. Myopia was induced in the right eyes of all guinea pigs using polymethyl methacrylate (PMMA) lenses for 3 weeks. Eye drops were administered accordingly. Intraocular pressure was measured every day. Refractive error and axial length measurements were performed once a week. The enucleated eyeballs were removed for hematoxylin and eosin (H&E) and Van Gieson (VG) staining at the end of the study. Results: The lens-induced myopia model was established after 3 weeks. Treatment with 0.1% brimonidine alone and 0.2% brimonidine alone was capable of inhibiting progressing myopia, as shown by the better refractive error (p=0.024; p=0.006) and shorter axial length (p=0.005; p=0.0017). Treatment with 0.1% brimonidine and 0.2% brimonidine combined with 2% pirenzepine was also effective in suppressing progressing refractive error (p=0.016; p=0.0006) and axial length (p=0.017; p=0.0004). The thickness of the sclera was kept stable in all groups except group F; the sclera was much thinner in the lens-induced myopia eyes compared to the control eyes. Conclusions: Treatment with 0.1% brimonidine alone and 0.2% brimonidine alone, as well as combined with 2% pirenzepine, was effective in inhibiting progressing myopia. The result indicates that intraocular pressure elevation is possibly a promising mechanism and potential treatment for progressing myopia.
[Pt] Publication type:JOURNAL ARTICLE
[Em] Entry month:1712
[Cu] Class update date: 171220
[Lr] Last revision date:171220
[St] Status:In-Process

  5 / 5093 MEDLINE  
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[PMID]: 29198091
[Au] Autor:Erdinest N; Morad Y
[Ad] Address:Department of Ophthalmology, Hadassah-Hebrew University Medical Center.
[Ti] Title:[TREATMENTS FOR SLOWING THE PROGRESSION OF MYOPIA].
[So] Source:Harefuah;156(11):720-724, 2017 Nov.
[Is] ISSN:0017-7768
[Cp] Country of publication:Israel
[La] Language:heb
[Ab] Abstract:INTRODUCTION: Myopia is the most common refractive error and is now endemic over the entire industrial world, particularly in Asia. High myopia is one of the major causes of blindness in the world. Slowing the progress of myopia is possible, the most effective treatment being atropine ophthalmic drops, given in a dose-dependent fashion. Although high-dose atropine (1% and 0.5%) was found to be highly effective in slowing myopia progression, low-dose atropine (0.01%) was found to have the lowest rebound effect (accelerated myopia progression after treatment cessation) and was therefore, the most effective treatment in the long term. Moderately effective treatments include pirenzepine drops, cyclopentolate drops, orthokeratology, contact lenses which are designed to reduce the peripheral hyperopic blur and distance-center soft multifocal contact lenses. Less effective treatments include multifocal spectacle lenses, bifocal spectacle lenses, bifocal soft contact lenses and outdoor activity in daylight. Visual therapy, biofeedback, full-spectacle correction, under-correction, spectacles designed to reduce the peripheral hyperopic blur, single-vision rigid gas-permeable contact lenses, single-vision soft contact lenses, tropicamide drops and timolol drops were all found to be ineffective.
[Pt] Publication type:ENGLISH ABSTRACT; JOURNAL ARTICLE; REVIEW
[Em] Entry month:1712
[Cu] Class update date: 171203
[Lr] Last revision date:171203
[St] Status:In-Process

  6 / 5093 MEDLINE  
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[PMID]: 29158113
[Au] Autor:Bacanak MS; Aydin B; Cabadak H; Nurten A; Gören MZ; Enginar N
[Ad] Address:Department of Medical Pharmacology, Istanbul Faculty of Medicine, Istanbul University, Turkey.
[Ti] Title:Contribution of M and M muscarinic receptor subtypes to convulsions in fasted mice treated with scopolamine and given food.
[So] Source:Behav Brain Res;, 2017 Nov 17.
[Is] ISSN:1872-7549
[Cp] Country of publication:Netherlands
[La] Language:eng
[Ab] Abstract:Treatment of fasted mice and rats with the nonselective muscarinic antagonist, scopolamine or atropine, causes convulsions after food intake. This study evaluated the effect of fasting on the expression of M and M muscarinic receptors in the brain regions, the relationship between receptor expression and seizure stages, and the muscarinic receptor subtype which plays a role in the occurrence of convulsions. Mice were grouped as allowed to eat ad lib (fed) and deprived of food for 24hours (fasted). Fasted animals developed convulsions after being treated with scopolamine (60%) or the selective M receptor antagonist pirenzepine (10mg/kg; 20% and 60mg/kg; 70%) and given food. Fasting increased expression of M receptors in the frontal cortex and M receptors in the hippocampus, but produced no change in the expression of both receptors in the amygdaloid complex. Food intake after fasting decreased M receptor expression in the frontal cortex and M and M receptor expression in the hippocampus. Seizure severity was uncorrelated with muscarinic receptor expression in the brain regions. Taken together, these findings provide evidence for the role of M muscarinic receptor antagonism and fasting-induced increases in M and M expression possible underlying mechanism in the occurrence of convulsions in fasted animals.
[Pt] Publication type:JOURNAL ARTICLE
[Em] Entry month:1711
[Cu] Class update date: 171121
[Lr] Last revision date:171121
[St] Status:Publisher

  7 / 5093 MEDLINE  
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[PMID]: 29122691
[Au] Autor:Smail MA; Soles JL; Karwoski TE; Rubin RT; Rhodes ME
[Ad] Address:Department of Biology, Saint Vincent College, Latrobe, PA, United States.
[Ti] Title:Sexually diergic hypothalamic-pituitary-adrenal axis responses to selective and non-selective muscarinic antagonists prior to cholinergic stimulation by physostigmine in rats.
[So] Source:Brain Res Bull;137:23-34, 2017 Nov 07.
[Is] ISSN:1873-2747
[Cp] Country of publication:United States
[La] Language:eng
[Ab] Abstract:Central cholinergic systems regulate the hypothalamic-pituitary-adrenal (HPA) axis differentially in males and females (sexual diergism). We previously investigated the role of muscarinic receptors in this regulation by administering physostigmine (PHYSO), an acetylcholinesterase inhibitor, to male and female rats pretreated with scopolamine (SCOP), a nonselective muscarinic antagonist. SCOP pretreatment enhanced adrenocorticotropic hormone (ACTH) and corticosterone (CORT) responses in both sexes; males had greater ACTH responses while females had greater CORT responses. In the present study, we further explored the role of muscarinic receptor subtypes in HPA axis regulation by administering PHYSO to male and female rats following SCOP or various doses of either the M1 or the M2 selective muscarinic receptor antagonists, pirenzepine (PIREN) or methoctramine (METHO), respectively. Blood sampling occurred before and at multiple times after PHYSO. ACTH and CORT were determined by highly specific immunoassays. PIREN+PHYSO resulted in sustained, dose-dependent increases in ACTH and CORT: ACTH responses were similar in both sexes, CORT responses were greater in females, and percent changes from baseline for both hormones were greater in males. METHO+PHYSO resulted in overall decreases in ACTH and CORT: ACTH and CORT responses were higher in females but lower than those caused by PIREN or SCOP in both sexes, and percent changes from baseline were lower in males. Area under the curve analyses further supported these sexually diergic effects. These results suggest that specific muscarinic receptor subtypes differentially influence the HPA axis in a sexually diergic manner.
[Pt] Publication type:JOURNAL ARTICLE
[Em] Entry month:1711
[Cu] Class update date: 171124
[Lr] Last revision date:171124
[St] Status:Publisher

  8 / 5093 MEDLINE  
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[PMID]: 28966237
[Au] Autor:Iwase M; Nishimura Y; Kurata N; Namba H; Hirai T; Kiuchi Y
[Ad] Address:Department of Pharmacology, Showa University School of Medicine.
[Ti] Title:Inhibitory Effects of Gastrointestinal Drugs on CYP Activities in Human Liver Microsomes.
[So] Source:Biol Pharm Bull;40(10):1654-1660, 2017.
[Is] ISSN:1347-5215
[Cp] Country of publication:Japan
[La] Language:eng
[Ab] Abstract:OTC drugs have an important role in self-medication. However, the pharmacokinetic properties of some OTC drugs have not been fully investigated and reports concerning their drug interactions are insufficient. Several gastrointestinal drugs are available as OTC drugs. Because of their pharmacological properties, these drugs are often used concomitantly with other drugs. Therefore, it is important to predict the possible drug interactions among these drugs. In the current study, we investigated the inhibitory effects of five gastrointestinal drugs, namely loperamide, oxethazaine, papaverine, pirenzepine, and trimebutine, on CYP activities in human liver microsomes. Furthermore, we calculated the ratio of the intrinsic clearance of each CYP substrate in the presence or absence of the gastrointestinal drugs. The possibility of drug interactions in vivo was predicted by cut-off criteria. CYP3A4 activity was markedly inhibited by trimebutine, papaverine, and oxethazaine. Their inhibitory properties were competitive and the K values were 6.56, 12.8, and 3.08 µM, respectively. Alternative R values of CYP3A4 exceeded the cut-off level. These results suggested that drug interactions mediated by CYP3A4 may occur during treatment with these gastrointestinal drugs, necessitating the confirmation of the clinical significance of these drug interactions to prevent unexpected adverse effects.
[Pt] Publication type:JOURNAL ARTICLE
[Em] Entry month:1710
[Cu] Class update date: 171002
[Lr] Last revision date:171002
[St] Status:In-Process
[do] DOI:10.1248/bpb.b17-00118

  9 / 5093 MEDLINE  
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[PMID]: 28847570
[Au] Autor:Aydinoglu F; Dalkir FT; Demirbag HO; Ogulener N
[Ad] Address:Department of Pharmacology, Pharmacy Faculty, Cukurova University, Adana, Turkey.
[Ti] Title:The interaction of l-cysteine/H S pathway and muscarinic acetylcholine receptors (mAChRs) in mouse corpus cavernosum.
[So] Source:Nitric Oxide;70:51-58, 2017 Nov 01.
[Is] ISSN:1089-8611
[Cp] Country of publication:United States
[La] Language:eng
[Ab] Abstract:The aim of this study was to investigate the possible interaction of l-cysteine/H S pathway and muscarinic acetylcholine receptors (mAChRs) in the mouse corpus cavernosum (CC). l-cysteine (endogenous H S substrate; 10 -10 M), sodium hydrogen sulfide (NaHS; exogenous H S; 10 -10 M) and acetylcholine (10 -10 M) produced concentration-dependent relaxation in isolated mouse CC tissues. Relaxations to endogenous and exogenous H S were reduced by non-selective mAChR antagonist atropine (5 × 10 M), selective M mAChR antagonist pirenzepine (5 × 10 M) and selective M mAChR antagonist 4-DAMP (10 M) but not by selective M mAChR antagonist AF-DX 116 (10 M). Also, acetylcholine-induced relaxations were reduced by atropine, pirenzepine, 4-DAMP and AF-DX 116, confirming the selective effects of mAChR antagonists. Furthermore, acetylcholine-induced relaxations were attenuated by cystathionine-gamma-lyase (CSE) inhibitor d,l-propargylglycine (PAG, 10 M) and cystathionine-ß-synthase inhibitor (CBS) aminooxyacetic acid (AOAA, 10 M). l-nitroarginine, nitric oxide synthase inhibitor, augmented the inhibitory effects of mAChR antagonists and H S enzyme inhibitors on acetylcholine-induced relaxations. In addition, the existence and localization of CSE, CBS and 3-MST were demonstrated in mouse CC. Furthermore, tissue acetylcholine release was significantly increased by l-cysteine but not by exogenous H S. The increase in acetylcholine level was completely inhibited by AOAA and PAG. These results suggest that M and M mAChRs contributes to relaxant effect mediated by endogenous H S but at same time l-cysteine triggers acetylcholine release from cavernosal tissue. Also, the role of NO in the interaction of l-cysteine/H S pathway and muscarinic acetylcholine receptors (mAChRs) could not be excluded.
[Pt] Publication type:JOURNAL ARTICLE
[Em] Entry month:1708
[Cu] Class update date: 171020
[Lr] Last revision date:171020
[St] Status:In-Process

  10 / 5093 MEDLINE  
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[PMID]: 28711697
[Au] Autor:Menozzi A; Pozzoli C; Poli E; Bontempi G; Serventi P; Meucci V; Intorre L; Bertini S
[Ad] Address:Department of Veterinary Science, University of Parma, Strada del Taglio 10, 43126 Parma, Italy. Electronic address: alessandro.menozzi@unipr.it.
[Ti] Title:Role of muscarinic receptors in the contraction of jejunal smooth muscle in the horse: An in vitro study.
[So] Source:Res Vet Sci;115:387-392, 2017 Dec.
[Is] ISSN:1532-2661
[Cp] Country of publication:England
[La] Language:eng
[Ab] Abstract:Nonselective antimuscarinic drugs are clinically useful in several pathologic conditions of horses, but, blocking all muscarinic receptor (MR) subtypes, may cause several side effects. The availability of selective antimuscarinic drugs could improve therapeutic efficacy and safety. We aimed to enlighten the role of different MR subtypes by evaluating the effects of nonselective, and selective M , M and M MR antagonists on the contractions of horse jejunum. Segments of circular muscle of equine jejunum, were put into organ baths, connected to isotonic transducers, and the effects on ACh concentration-response curves, and on electrical field stimulation (EFS)-evoked contractions of intestinal preparations, induced by nonselective or selective MR antagonists, compared to pre-drug level, were studied. Atropine (nonselective MR antagonist), pirenzepine (selective M antagonist), and p-FHHSiD (selective M antagonist) competitively antagonized ACh (pA =9.78±0.21; 7.14±0.25 and 7.56±0.17, respectively). Methoctramine (selective M antagonist) antagonized ACh in a concentration-unrelated fashion; however, it competitively antagonized carbachol, a nonselective muscarinic agonist (pA =6.42±0.23). Atropine dose-dependently reduced EFS-evoked contractions, reaching a maximal effect of -45.64±6.54%; the simultaneous block of neurokinin receptors, almost completely abolished the atropine-insensitive contractions. p-FHHSiD dose-dependently reduced EFS-induced contractions, while pirenzepine caused a minor decrease. Methoctramine, ineffective up to 10 M, enhanced the contractions at 10 M; the block of neurokinin receptors abolished the increase of contraction. Cholinergic contractions of horse jejunum are mainly mediated by M receptors; M selective antagonists seem to scarcely affect cholinergic, and to enhance neurokininergic contractions of equine jejunum, thus their use entails a lower risk of causing intestinal hypomotility, compared to nonselective drugs.
[Pt] Publication type:JOURNAL ARTICLE
[Em] Entry month:1707
[Cu] Class update date: 171117
[Lr] Last revision date:171117
[St] Status:In-Process


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