ArticleBritish journal of pharmacology2009
Quantitative analysis of the loss of muscarinic receptors in various peripheral tissues in M1-M5 receptor single knockout mice.
Article in British journal of pharmacology, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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Who cites it
13 citing papers in PubMed, 44 citations in OpenAlex.
- Phosphoproteome reveals molecular mechanisms of aberrant rhythm in neurotransmitter-mediated islet hormone secretion in diabetic mice.Clinical and translational medicine · 2022Article
- Multitargeting nature of muscarinic orthosteric agonists and antagonists.Frontiers in physiology · 2022Review
- Social Isolation: How Can the Effects on the Cholinergic System Be Isolated?Frontiers in pharmacology · 2021Review
- The beneficial effects of a muscarinic agonist on pancreatic β-cells.Scientific reports · 2019Article
- Structure-Activity Relationships of Pan-GαACS chemical neuroscience · 2018Article
- Muscarinic receptors 2 and 5 regulate bitter response of urethral brush cells via negative feedback.FASEB journal : official publication of the Federation of American Societies for Experimental Biology · 2018Article
- Article
- Decrease in heart adrenoceptor gene expression and receptor number as compensatory tool for preserved heart function and biological rhythm in M(2) KO animals.Naunyn-Schmiedeberg's archives of pharmacology · 2012Article
- Characterization of bladder selectivity of antimuscarinic agents on the basis of in vivo drug-receptor binding.International neurourology journal · 2012Article
- α1-Adrenoceptors and muscarinic receptors in voiding function - binding characteristics of therapeutic agents in relation to the pharmacokinetics.British journal of clinical pharmacology · 2011Review
- The residual nonadrenergic contractile response to nerve stimulation of the mouse prostate is mediated by acetylcholine but not ATP in a comparison with the mouse vas deferens.The Journal of pharmacology and experimental therapeutics · 2010Article
- The M2-muscarinic receptor inhibits the development of streptozotocin-induced neuropathy in mouse urinary bladder.The Journal of pharmacology and experimental therapeutics · 2010Article
- Immunoglobulins from scleroderma patients inhibit the muscarinic receptor activation in internal anal sphincter smooth muscle cells.American journal of physiology. Gastrointestinal and liver physiology · 2009Article
Corrections and comments
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Authors and funding
6 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
background and purposeTo compare loss in binding to muscarinic receptor (mAChR) subtypes with their known functions, the total density of muscarinic receptors was measured in peripheral tissues from wild type (WT) and mAChR knockout (KO) mice. EXPERIMENTAL APPROACH: Binding parameters of [N-methyl-3H]scopolamine methyl chloride ([3H]NMS) were determined in 10 peripheral tissues of WT and M1-M5 receptor KO mice. Competition between [3H]NMS and darifenacin (selective M3 receptor antagonist) was also measured. KEY
resultsThere was an extensive loss of [3H]NMS-binding sites (maximal number of binding sites, Bmax) in heart and smooth muscle from M2KO mice, compared with WT mice. Smooth muscle from M3KO mice also showed a moderate loss of Bmax. Bmax fell in pancreas and bladder of M4KO mice and in prostate in M1KO and M3KO mice. There was a large loss of Bmax in exocrine and endocrine glands of M3KO mice with a moderate decrease in M2KO mice. Darifenacin inhibited specific [3H]NMS binding in submandibular gland and bladder of WT, M2KO and M3KO mice. Ki (inhibition constant) values for darifenacin in the submandibular gland were the same in WT and M2KO mice but increased in M3KO mice. However, Ki values in bladder were decreased in M2KO mice and increased in M3KO mice. CONCLUSIONS AND IMPLICATIONS: Single mAChR KO mice exhibit a loss of mAChR in peripheral tissues that generally paralleled the reported loss of function. Quantitative analysis of data, however, also suggested that, in some instances, normal expression of a receptor subtype depended on expression of other subtypes.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.