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Potential benefits of muscarinic M-3 receptor selectivity

Andersson, Karl-Erik LU (2002) In European Urology. Supplement 1(4). p.23-28
Abstract
Detrusor smooth muscle contains muscarinic receptors of the M-2 (approximate to2/3) and M-3 (approximate to1/3) subtypes. M-3 receptors are mainly responsible for normal micturition contraction, whereas, the role Of M-2 receptors has not yet been clarified. In certain disease states, M-2 receptors may also contribute to bladder contraction. Different muscarinic receptor subtypes can contribute to processes of cellular activation or inhibition. For example, in salivary glands, both M-1 and M-3 receptor subtypes may control secretion. In the cardiovascular system, the M-2 receptor subtype can mediate parasympathetically-driven bradycardia and a decrease in cardiac output. In the brain, where the role of cortical M, receptors in cognition is... (More)
Detrusor smooth muscle contains muscarinic receptors of the M-2 (approximate to2/3) and M-3 (approximate to1/3) subtypes. M-3 receptors are mainly responsible for normal micturition contraction, whereas, the role Of M-2 receptors has not yet been clarified. In certain disease states, M-2 receptors may also contribute to bladder contraction. Different muscarinic receptor subtypes can contribute to processes of cellular activation or inhibition. For example, in salivary glands, both M-1 and M-3 receptor subtypes may control secretion. In the cardiovascular system, the M-2 receptor subtype can mediate parasympathetically-driven bradycardia and a decrease in cardiac output. In the brain, where the role of cortical M, receptors in cognition is well documented, M-1 receptor blockade would be expected to compromise central nervous system function. Muscarinic receptors that mediate contraction of human ciliary muscle are most probably M-3 and M-5. Drugs selective for the M-3 receptor might be expected to have clinical efficacy in detrusor overactivity with a reduction in adverse events related to the blockade of other receptor subtypes. However, the clinical effectiveness of a drug depends not only on its receptor affinity, but also on its pharmacokinetics and the importance of specific muscarinic receptors for a given organ function. (C) 2002 Elsevier Science B.V. All rights reserved. (Less)
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author
organization
publishing date
type
Contribution to journal
publication status
published
subject
keywords
overactive bladder (OAB), muscarinic M-3 receptor, selective muscarinic M3 antagonists
in
European Urology. Supplement
volume
1
issue
4
pages
23 - 28
publisher
Elsevier
external identifiers
  • wos:000179320600005
  • scopus:0036664806
ISSN
1569-9056
DOI
10.1016/S1569-9056(02)00045-3
language
English
LU publication?
yes
id
e374d2a6-8af9-4f65-90cf-8d2dd1705b85 (old id 323535)
date added to LUP
2007-08-07 09:20:52
date last changed
2017-12-17 03:49:39
@article{e374d2a6-8af9-4f65-90cf-8d2dd1705b85,
  abstract     = {Detrusor smooth muscle contains muscarinic receptors of the M-2 (approximate to2/3) and M-3 (approximate to1/3) subtypes. M-3 receptors are mainly responsible for normal micturition contraction, whereas, the role Of M-2 receptors has not yet been clarified. In certain disease states, M-2 receptors may also contribute to bladder contraction. Different muscarinic receptor subtypes can contribute to processes of cellular activation or inhibition. For example, in salivary glands, both M-1 and M-3 receptor subtypes may control secretion. In the cardiovascular system, the M-2 receptor subtype can mediate parasympathetically-driven bradycardia and a decrease in cardiac output. In the brain, where the role of cortical M, receptors in cognition is well documented, M-1 receptor blockade would be expected to compromise central nervous system function. Muscarinic receptors that mediate contraction of human ciliary muscle are most probably M-3 and M-5. Drugs selective for the M-3 receptor might be expected to have clinical efficacy in detrusor overactivity with a reduction in adverse events related to the blockade of other receptor subtypes. However, the clinical effectiveness of a drug depends not only on its receptor affinity, but also on its pharmacokinetics and the importance of specific muscarinic receptors for a given organ function. (C) 2002 Elsevier Science B.V. All rights reserved.},
  author       = {Andersson, Karl-Erik},
  issn         = {1569-9056},
  keyword      = {overactive bladder (OAB),muscarinic M-3 receptor,selective muscarinic M3 antagonists},
  language     = {eng},
  number       = {4},
  pages        = {23--28},
  publisher    = {Elsevier},
  series       = {European Urology. Supplement},
  title        = {Potential benefits of muscarinic M-3 receptor selectivity},
  url          = {http://dx.doi.org/10.1016/S1569-9056(02)00045-3},
  volume       = {1},
  year         = {2002},
}