Muscarinic agonist

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Muscarinic agonist
Drug class
Skeletal structure formula of muscarine
Class identifiers
ATC codeN07
Biological targetmuscarinic acetylcholine receptor
External links
MeSHD018721
Legal status
In Wikidata

A muscarinic agonist[1] is an agent that activates the activity of the muscarinic acetylcholine receptor. The muscarinic receptor has different subtypes, labelled M1-M5, allowing for further differentiation.

Clinical significance

M1

M1-type muscarinic

Alzheimer disease (AD), amyloid formation may decrease the ability of these receptors to transmit signals, leading to decreased cholinergic activity. As these receptors themselves appear relatively unchanged in the disease process, they have become a potential therapeutic target when trying to improve cognitive function in patients with AD.[2][3][4]

A number of muscarinic agonists have been developed and are under investigation to treat AD. These agents show promise as they are neurotrophic, decrease amyloid depositions, and improve damage due to oxidative stress. Tau-phosphorylation is decreased and cholinergic function enhanced. Notably several agents of the AF series of muscarinic agonists have become the focus of such research:. AF102B, AF150(S), AF267B. In animal models that are mimicking the damage of AD, these agents appear promising.

The agent xanomeline has been proposed as a potential treatment for schizophrenia.[5][6]

M3

In the form of pilocarpine, muscarinic receptor agonists have been used medically for a short time.

  • M3 agonists
    • Aceclidine, for glaucoma
    • Betel nut
    • Pilocarpine is a drug that acts as a muscarinic receptor agonist that is used to treat glaucoma
    • Sjögren's syndrome

Muscarinic versus nicotinic activity

Comparison of cholinergic agonists [7]
Substance Receptor specificity Hydrolysis by acetylcholinesterase Comments
Muscarinic Nicotinic
Acetylcholine +++ +++ +++ Endogenous ligand
Carbachol ++ +++ - Used in the treatment of glaucoma
Methacholine +++ + ++ Used to diagnose
COPD
.
Bethanechol +++ - - Used in bladder and gastrointestinal hypotonia.
Muscarine +++ - - Natural alkaloid found in certain mushrooms.

Cause of one form of mushroom poisoning

Nicotine - +++ - Natural alkaloid found in the
tobacco plant
.
Pilocarpine ++ - - Used in glaucoma.
Oxotremorine ++ +[9] - Used in research to induce

symptoms of Parkinson's disease.

Muscarinic acetylcholine receptor subtypes

The targets for muscarinic agonists are the muscarinic receptors:

Gq subunits
.

See also

References

  1. PMC 6236374
    .
  2. S2CID 21773972
    .
  3. S2CID 85100519
    .
  4. PMID 18625455
    .
  5. S2CID 24308125
    .
  6. S2CID 12642499
    .
  7. ISBN 978-0-443-06911-6
    .
  8. PMID 17565027
    .
  9. PMID 10602325
    .

External links