CHRM1,3,5 bind CHRM1,3,5 antagonists

Stable Identifier
R-HSA-9704151
Type
Reaction [binding]
Species
Homo sapiens
Compartment
ReviewStatus
5/5
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A muscarinic receptor (CHRM) antagonist is a type of anticholinergic agent that blocks the activity of human muscarinic acetylcholine receptors 1-5 (Caulfield & Birdsall 1998, Dorje et al. 1991, Bolden & Richelson 1992). Muscarinic antagonists reduce the activation of the parasympathetic nervous system. The normal function of the parasympathetic system is often described as "rest-and-digest", and includes slowing of the heart, narrowing of airways, an increased digestion rate, promotion of urination, and sexual arousal. Most muscarinic antagonists are synthetic but two of the most commonly used ones are belladonna alkaloids (from deadly nightshade plants), namely scopolamine and atropine. Scopolamine is used to treat motion sickness (Golding & Gresty 2015) whereas atropine can counter organophosphate poisoning (Bajracharya et al. 2016). Both are used for comsetic purposes to promote pupil dilation (Tran et al. 2018).

Muscarinic antagonists are widely used in the treatment of low heart rate (Harvey 2012), overactive bladder (Nadeau et al. 2014, Franco et al. 2020), peptic and gastric ulcers (Ehlert et al. 2012, Shamburek & Schubert 1993), asthma and COPD (Alagha et al. 2014), and neurological problems such as Parkinson's disease (Ztaou & Amalric 2019) and Alzheimer's disease (Clader & Wang 2005).
Literature References
PubMed ID Title Journal Year
22222706 Muscarinic agonists and antagonists: effects on gastrointestinal function

Pak, KJ, Ehlert, FJ, Griffin, MT

Handb Exp Pharmacol 2012
1994002 Antagonist binding profiles of five cloned human muscarinic receptor subtypes

Brann, MR, Tacke, R, Wess, J, Dörje, F, Lambrecht, G, Mutschler, E

J. Pharmacol. Exp. Ther. 1991
25502048 Pathophysiology and treatment of motion sickness

Gresty, MA, Golding, JF

Curr Opin Neurol 2015
8097411 Pharmacology of gastric acid inhibition

Shamburek, RD, Schubert, ML

Baillieres Clin Gastroenterol 1993
9647869 International Union of Pharmacology. XVII. Classification of muscarinic acetylcholine receptors

Birdsall, NJ, Caulfield, MP

Pharmacol Rev 1998
32007426 Long-term efficacy and safety of solifenacin in pediatric patients aged 6 months to 18 years with neurogenic detrusor overactivity: results from two phase 3 prospective open-label studies

Vande Walle, J, Bosman, B, Dahler, E, Davies, LN, Snijder, R, Hoebeke, P, Franco, I, Bolong, D, Stroosma, O, Verheggen, F, Baka-Ostrowska, M, Newgreen, D

J Pediatr Urol 2020
29715053 A Review of Myopia Control with Atropine

Tran, YH, Jong, M, Tran, TD, Coroneo, M, Sankaridurg, P, Tran, HDM

J Ocul Pharmacol Ther 2018
24839481 Long-term use of solifenacin in pediatric patients with overactive bladder: Extension of a prospective open-label study

Pellerin, E, Lamontagne, P, Nadeau, G, Moore, K, Schröder, A, Genois, L, Hamel, M, Bolduc, S

Can Urol Assoc J 2014
28327676 Management of Organophosphorus Poisoning

Bajracharya, SR, Prasad, PN, Ghimire, R

J Nepal Health Res Counc 2016
1346637 Antagonism by antimuscarinic and neuroleptic compounds at the five cloned human muscarinic cholinergic receptors expressed in Chinese hamster ovary cells

Cusack, B, Bolden, C, Richelson, E

J. Pharmacol. Exp. Ther. 1992
24587893 Long-acting muscarinic receptor antagonists for the treatment of chronic airway diseases

Chanez, P, Martinez, S, Sofalvi, T, Alagha, K, Tummino, C, Pahus, L, Charpin, D, Bourdin, A, Palot, A, Gouitaa, M

Ther Adv Chronic Dis 2014
16250841 Muscarinic receptor agonists and antagonists in the treatment of Alzheimer's disease

Clader, JW, Wang, Y

Curr Pharm Des 2005
30825602 Contribution of cholinergic interneurons to striatal pathophysiology in Parkinson's disease

Amalric, M, Ztaou, S

Neurochem Int 2019
22222704 Muscarinic receptor agonists and antagonists: effects on cardiovascular function

Harvey, RD

Handb Exp Pharmacol 2012
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