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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: Hyoscyamine
L-Hyoscyamine is a potent and competitive antagonist of muscarinic acetylcholine receptors (mAChRs). As a natural tropane alkaloid, it exerts significant biological activity that makes it valuable in pharmacological research. L-Hyoscyamine is utilized in studies investigating the modulation of cholinergic signaling and related therapeutic applications.
Synonyms: TD4208; GSK1160724
Revefenacin is potent and selective muscarinic receptor antagonist in development for the treatment of COPD.
Homatropine Bromide is a muscarinic acetylcholine receptor (mAChR) antagonist. This compound exhibits anticholinergic properties, making it valuable in various pharmacological applications, particularly for its effects on smooth muscle relaxation and secretion inhibition. It is commonly used in research focused on neuropharmacology and the modulation of cholinergic signaling pathways.
Synonyms: Homatropine methobromide
Homatropine methylbromide is a muscarinic acetylcholine receptor (mAChR) antagonist that demonstrates significant inhibitory activity on endothelial and smooth muscle muscarinic receptors, with an IC50 of 162 nM in WKY-E and SHR-E models. This compound is utilized in research applications focused on studying the effects of mAChR modulation in various physiological and pathological conditions. It serves as a valuable tool for investigating the role of muscarinic signaling in smooth muscle contraction and vascular function.
Trihexyphenidyl hydrochloride is a selective antagonist of the M1 muscarinic receptor, exhibiting an IC50 of 3.7 nM in rat cerebral cortex M1 muscarinic receptors. This compound modulates cholinergic activity, effectively countering acetylcholine supersensitivity and providing therapeutic benefits in movement disorders. Additionally, Trihexyphenidyl hydrochloride has been shown to inhibit vagally-induced bradycardia, vasodilatation, and pressor responses stimulated by McN-A-343. It is a valuable tool for research applications related to Parkinson's disease and other cholinergic dysfunctions.
Synonyms: YM905
Solifenacin is a novel muscarinic receptor antagonist with pKis of 7.6, 6.9 and 8.0 for M1, M2 and M3 receptors, respectively.
Synonyms: Endovalpin; Lytispasm; Valpin; Methyloctatropine bromide; Anisotropine methobromide; Octatropine methylbromide; CB-154
Anisotropine methylbromide is a muscarinic antagonist and antispasmodic. Anisotropine methylbromide is a quaternary ammonium compound. Its use as treatment adjunct in peptic ulcer has been replaced by the use of more effective agents.
Synonyms: Procyclidine Hydrochloride; Tricyclamol hydrochloride; (-)-Tricyclamol iodide; C19H29NO.HCl; Rosemont Brand of Procyclidine Hydrochloride; Tricyclamol; Wellcome Brand of Procyclidine Hydrochloride
Procyclidine hydrochloride is a muscarinic antagonist that crosses the blood-brain barrier and is used in the treatment of drug-induced extrapyramidal disorders and in Parkinsonism.
Synonyms: Cantil; Gastropidil; Cantilaque; Cantilon; mepenzolate iodide; mepenzolic acid
Mepenzolate Bromide is a muscarinic antagonist used to treat gastrointestinal disorders. It decreases the severity of elastase-induced airspace enlargement and respiratory dysfunction.
Propantheline bromide is a selective antagonist of muscarinic acetylcholine receptors (mAChRs). It exhibits notable effects in the management of smooth muscle dysfunction, including conditions such as excessive sweating, abdominal cramps, and involuntary urination. With limited ability to cross the blood-brain barrier, propantheline bromide is valuable in studies that require peripheral mAChR modulation without central nervous system effects.
Synonyms: Tropine tropate sulfate; DL-Hyoscyamine sulfate; Sulfatropinol
Atropine sulfate is a competitive antagonist of the muscarinic acetylcholine receptors (mAChR), exhibiting IC50 values of 0.39 nM for human mAChR M4 and 0.71 nM for chicken mAChR M4. This compound effectively inhibits acetylcholine-induced relaxations in human pulmonary veins. Atropine sulfate is utilized in research related to anti-myopia and the management of bradycardia.
Racanisodamine is a non-selective muscarinic antagonist that modulates the activity of muscarinic acetylcholine receptors (mAChR). It exhibits pharmacological effects similar to its parent compound, anisodamine, and is primarily utilized in formulations for myopic control in ophthalmic applications. This compound is valuable for research into the mechanisms of muscarinic receptor modulation and its implications in vision science.
Synonyms: Hyoscine hydrobromide trihydrate
Scopolamine hydrobromide trihydrate is a potent muscarinic antagonist known for its ability to penetrate the blood-brain barrier. It competitively inhibits 5-HT3 receptors, exhibiting an IC50 of 2.09 μM. This compound is frequently utilized in research related to cognitive and memory impairments, as well as in studies of postoperative nausea, vomiting, and motion sickness. Additionally, Scopolamine hydrobromide trihydrate is relevant in investigating various nervous system disorders.
Synonyms: 6-Hydroxyhyoscyamine hydrobromide
Anisodamine hydrobromide is a non-subtype-selective antagonist of muscarinic and nicotinic acetylcholine receptors. This compound exhibits significant antioxidant and anti-inflammatory properties, making it a valuable tool in research related to these biological activities. Its diverse pharmacological profile supports investigations into neurological disorders and inflammatory conditions.
Synonyms: LS519
Pirenzepine dihydrochloride (LS519) is a selective M1 muscarinic receptor antagonist.
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: 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: Alginor; Cimetropii bromidum; UNII-0C7M5WE60Q
Cimetropium Bromide (DA-3177) is a mAChR antagonist for long-term treatment of irritable bowel syndrome.
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.
Elucaine is a muscarinic acetylcholine receptor antagonist with anti-ulcerative activity.
YM-58790 is a potent antagonist of M3 muscarinic receptor, with Ki of 15 nM.
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.
mAChR-IN-1 is a potent muscarinic cholinergic receptor(mAChR) antagonist with IC50 of 17 nM.
Synonyms: LAS 34273; LAS-W 330
Aclidinium Bromide(LAS 34273; LAS-W 330) is a long-acting, inhaled muscarinic antagonist as a maintenance treatment for chronic obstructive pulmonary disease (COPD).
