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Muscarinic acetylcholine receptors (mAChRs) are a class of G protein-coupled receptors (GPCRs) found in the central and peripheral nervous systems, as well as in various other tissues and organs throughout the body. These receptors are named after muscarine, a natural alkaloid compound found in certain mushrooms, which was one of the first substances discovered to activate them.
There are five subtypes of muscarinic receptors, designated as M1 through M5, each with distinct tissue distribution and functions. Here's an overview of their roles:
Muscarinic receptors are activated by the neurotransmitter acetylcholine and play a vital role in regulating a wide range of physiological processes, including heart rate, smooth muscle contraction, glandular secretion, and neurotransmitter release. They are targets for various drugs, including anticholinergic agents, which block their activity, and drugs used to treat conditions like bradycardia and neurodegenerative disorders.
Understanding the functions and regulation of muscarinic acetylcholine receptors is essential for developing therapies that modulate their activity and for advancing our knowledge of how they contribute to various physiological and pathological processes in the body.
Synonyms: Cl-845
Pirmenol hydrochloride inhibits IK.ACh by blocking muscarinic receptors. The IC50 of Pirmenol for inhibition of Carbachol-induced IK.ACh is 0.1 μM.
Atropine methyl bromide, a muscarinic receptor (mAChR) antagonist, is a quaternary ammonium salt of atropine and a mydriatic for dilation of the pupil during ophthalmic examination. It is introduced for relieving pyloric spasm in infants for its highly polar nature. It penetrates less readily into the central nervous system than atropine.
Synonyms: Evoxac; Cevimeline HCl
Cevimeline (Evoxac) Hcl is a parasympathomimetic and muscarinic agonist, with particular effect on M3 receptors; used in the treatment of dry mouth associated with sjogren's syndrome.
Synonyms: (R)-(+)-Tolterodine; (+)-Tolterodine; (R)-Tolterodine; PNU-200583
Tolterodine is an mAChR inhibitor that competitively binds to acetylcholine, leading to a reduction in sympathetic excitation and inhibition of involuntary bladder muscle contractions. It is known to restore the Nrf2/NF-κB signaling pathway, providing protection against inflammatory responses and ferroptosis. Additionally, Tolterodine mitigates LPS-induced reactive oxygen species production and lipid oxidation, making it valuable for research in urinary tract infections and overactive bladder conditions.
Synonyms: Dactil; Crapinon; NSC 4349; Piperidolate HCl
Piperidolate hydrochloride is an antimuscarinic, Also a potential inhibitor of human glutathione transferase P1-1.
Synonyms: YM905 hydrochloride
Solifenacin hydrochloride is a muscarinic receptor antagonist that selectively inhibits the activity of M1, M2, and M3 muscarinic receptors, displaying pKis of 7.6, 6.9, and 8.0, respectively. This compound is primarily utilized in research to study the modulation of cholinergic signaling and its implications in urological conditions. Its antagonistic properties make it a valuable tool for investigating the pharmacology of bladder overactivity and other related disorders.
Synonyms: 6-Hydroxy hyoscyamine; 654-II
Anisodamine is an inhibitor of alpha-1 adrenergic receptors and mAChRs isolated from Chinese solanacea plant.
Synonyms: 1087 A.N.; BRN 0031110; Dactil; JB 305; Piperidolatum
Piperidolate is a tertiary amine antimuscarinic. It is similar to atropine. It is mainly used in the smooth muscle spasm of the gastrointestinal tract and inhibits intestinal cramp induced by acetylcholine in rats and dogs.
Synonyms: Alginor; Cimetropii bromidum; UNII-0C7M5WE60Q
Cimetropium Bromide (DA-3177) is a mAChR antagonist for long-term treatment of irritable bowel syndrome.
Pridinol mesylate is an anticholinergic agent that targets muscarinic acetylcholine receptors (mAChRs) to provide muscle relaxation. It effectively reduces impulse conduction to spinal motor neurons, exhibiting significant muscle relaxant properties. Pridinol mesylate is useful in research related to musculoskeletal diseases, particularly for investigating skeletal muscle contractures arising from both central and peripheral origins. Its blood-brain permeability facilitates its application in studies involving central nervous system effects.
Synonyms: AZN00016130
VU6005806 (AZN-00016130) is a potent muscarnic acethylcholine receptor subtype 4 (M4) positive allosteric modulator (PAM), with EC50s of 94 nM, 28 nM, 87 nM and 68 nM for human, rat, dog and cyno M4, respectively. Used in the research of neuropsychiatric disorders.
Talsaclidine is a muscarinic agonist with preferential neuron-stimulating properties. Talsaclidine is a full agonist at the M1 subtype, and as a partial agonist at the M2 and M3 subtypes.
TAK-071 is a novel, potent and highly selective muscarinic acetylcholine receptor 1 (M1R) positive allosteric modulator. EC50 of TAK-071 M1R agonist activities is 520 nM.
Synonyms: (+)-Benzetimide; (S)-(+)-Dexetimide; Dexbenzetimide
Dexetimide ((+)-Benzetimide) is a high-affinity muscarinic receptor antagonist and a potent and persistent anticholinergic agent used to treat neuroleptic-induced parkinsonism.
Synonyms: Lu 25-109
Alvameline (Lu25-109) is a partial M1 agonist and M2/M3 antagonist.
Elucaine is a muscarinic acetylcholine receptor antagonist with anti-ulcerative activity.
VU0467154 is a positive allosteric modulator of the M4 muscarinic acetylcholine receptor (mAChR), potentiating the response to ACh with pEC50s of 7.75, 6.2 and 6 for rat, human and cynomolgus monkey M4 receptor, respectively.
VU 0365114 is a mAChR M5 positive allosteric modulator, with an EC50 of 2.7 μM.
YM-58790 is a potent antagonist of M3 muscarinic receptor, with Ki of 15 nM.
VU 6008667 is a selective negative allosteric modulator of M5 NAM with IC50s of 1.2 μM and 1.6 μM for human M5 and rat M5, respectively. High CNS penetration.
DREADD agonist 21 is a potent human muscarinic acetylcholine M3 receptors (hM3Dq) agonist(EC50=1.7 nM).
Synonyms: AE-37; AVex-73; Anavex-2-73
Blarcamesine, also known as AVex-73 and AE-37, is a muscarinic M1 agonist potentially for the treatment of Alzheimer's disease. It is an ς receptor ligand.
Synonyms: Org 9487
Rapacuronium bromide is an allosteric modulator of muscarinic acetylcholine receptor (mAChR).
mAChR-IN-1 hydrochloride is a potent muscarinic cholinergic receptor (mAChR) antagonist, with an IC50 of 17 nM.
Synonyms: SVT-40776 D-tartrate; SVT40776
Tarafenacin D-tartrate (SVT-40776 D-tartrate) is a highly selective M3 muscarinic receptor antagonist (Ki= 0.19 nM), ~200 fold selectivity over M2 receptor.
