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)
Please use this url to cite or link to this publication:
https://lup.lub.lu.se/record/323535
- author
- Andersson, Karl-Erik
LU
- organization
- publishing date
- 2002
- 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
- 2016-04-01 15:25:55
- date last changed
- 2022-03-22 04:28:32
@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}},
keywords = {{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}},
doi = {{10.1016/S1569-9056(02)00045-3}},
volume = {{1}},
year = {{2002}},
}