ArticleBritish journal of pharmacology2000
The role of M(2)-muscarinic receptors in mediating contraction of the pig urinary bladder in vitro.
Article in British journal of pharmacology, 2000. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers.
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Who cites it
21 citing papers in PubMed, 76 citations in OpenAlex.
- Adreno-Muscarinic Synergy of Contractile Responses From Human Hyperplastic Prostate.International neurourology journal · 2024Article
- Expression of components of the urothelial cholinergic system in bladder and cultivated primary urothelial cells of the pig.BMC urology · 2019Article
- cAMP-dependent regulation of RhoA/Rho-kinase attenuates detrusor overactivity in a novel mouse experimental model.BJU international · 2017Article
- Octodon degus, a new model to study the agonist and plexus-induced response in the urinary bladder.Journal of physiology and biochemistry · 2017Article
- Urinary Retention, Incontinence, and Dysregulation of Muscarinic Receptors in Male Mice Lacking Mras.PloS one · 2015Article
- Rationale for the use of anticholinergic agents in overactive bladder with regard to central nervous system and cardiovascular system side effects.Korean journal of urology · 2013Review
- Inhibition of leptin regulation of parasympathetic signaling as a cause of extreme body weight-associated asthma.Cell metabolism · 2013Article
- The validation of a functional, isolated pig bladder model for physiological experimentation.Frontiers in pharmacology · 2012Article
- Nerve-evoked purinergic signalling suppresses action potentials, Ca2+ flashes and contractility evoked by muscarinic receptor activation in mouse urinary bladder smooth muscle.The Journal of physiology · 2009Article
- Muscarinic receptor expression and receptor-mediated detrusor contraction: comparison of juvenile and adult porcine tissue.Pflugers Archiv : European journal of physiology · 2008Article
- M2 mediated contractions of human bladder from organ donors is associated with an increase in urothelial muscarinic receptors.Neurourology and urodynamics · 2007Article
- Propiverine and metabolites: differences in binding to muscarinic receptors and in functional models of detrusor contraction.Naunyn-Schmiedeberg's archives of pharmacology · 2006Article
- Muscarinic regulation of neonatal rat bladder spontaneous contractions.American journal of physiology. Regulatory, integrative and comparative physiology · 2006Article
- Muscarinic receptors in the bladder: from basic research to therapeutics.British journal of pharmacology · 2006Review
- Pharmacodynamics of propiverine and three of its main metabolites on detrusor contraction.British journal of pharmacology · 2005Article
- Muscarinic receptors: what we know.Current urology reports · 2003Review
- Gender comparison of muscarinic receptor expression and function in rat and human urinary bladder: differential regulation of M2 and M3 receptors?Naunyn-Schmiedeberg's archives of pharmacology · 2003Article
- The intracellular pathway of the acetylcholine-induced contraction in cat detrusor muscle cells.British journal of pharmacology · 2002Article
- M(3) muscarinic receptors mediate contraction of human urinary bladder.British journal of pharmacology · 2002Article
- A benefit-risk assessment of extended-release oxybutynin.Drug safety · 2002Review
Corrections and comments
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Authors and funding
4 authors at 3 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
1. In urinary bladder, M(2)-muscarinic receptors predominate, but it is the smaller population of M(3)-receptors which mediate detrusor contraction. This study examines the M(2) : M(3) ratio and the role of M(2)-receptors in contraction of pig urinary bladder. 2. Competition experiments with [(3)H]-QNB determined the ratio of M(2) : M(3). In functional studies, affinity values (pK(B)) for 4-DAMP, darifenacin and methoctramine were calculated. Similar experiments were performed on tissues following selective M(3)-inactivation (incubation with 40 nM 4-DAMP mustard in the presence of 1 microM methoctramine to protect M(2)-receptors), precontraction with 50 mM KCl and relaxation with isoprenaline (30 microM) or forskolin (1 microM). 3. In competition binding, displacement of [(3)H]-QNB by 4-DAMP, darifenacin and methoctramine best fitted a two-site model suggesting a predominant (70 - 80%) population of M(2)-receptors. 4. On normal detrusor in vitro, 4-DAMP and methoctramine caused surmountable antagonism of responses to carbachol with pK(B) values of 9.37+/-0.07 and 6.05+/-0.05 respectively. Darifenacin caused unsurmountable antagonism, the apparent pK(B) value being 8.61+/-0.10. 5. In tissues where the M(3)-receptors had been inactivated and cyclic AMP levels elevated, 4-DAMP and darifenacin were less potent, with apparent pK(B) values of 8.72+/-0.08 and 6.74+/-0.07. In contrast, methoctramine was more potent, the apparent pK(B) value increasing significantly to 6.86+/-0.06. 6. se data suggest that the pig bladder possesses a similar muscarinic receptor population to the human bladder and that the M(3)-receptor subtype mediates contraction of the normal detrusor muscle. However an involvement of M(2)-receptors in contraction can be observed following pharmacological manipulation of the receptor population.
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