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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: Acetylcolina
Acetylcholine iodide is a neurotransmitter found at neuromuscular junctions, autonomic ganglia, parasympathetic effector junctions, a subset of sympathetic effector junctions, and at many sites in the central nervous system.
Choline bitartrate is a form of the nutrient choline which is found in foods.
Methylbenactyzium Bromide is a selective inhibitor of muscarinic acetylcholine receptors (mAChR). This compound effectively modulates cholinergic signaling pathways and is utilized in research focused on neuropharmacology, cardiovascular physiology, and respiratory function. Its ability to inhibit mAChR activity makes it a valuable tool in studies investigating the role of acetylcholine in various physiological processes and disease states.
Synonyms: Diphemanil mesylate
Diphemanil methylsulfate is a quaternary ammonium anticholinergic.
Synonyms: Rec-7-0040; DW61
Flavoxate hydrochloride is a competitive inhibitor of phosphodiesterase (PDE), providing significant antispasmodic effects through its action as a muscarinic acetylcholine receptor (mAChR) antagonist. In addition to its PDE inhibition, it exhibits moderate calcium antagonistic properties and local anesthetic effects. Flavoxate hydrochloride is utilized in research focused on overactive bladder (OAB) and related lower urinary tract infections, contributing to a better understanding of these conditions and potential therapeutic approaches.
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.
Synonyms: Octylonium bromide; SP63
Otilonium bromide is a selective inhibitor of muscarinic acetylcholine receptors (mAChR) with pronounced smooth muscle relaxant properties. This compound primarily functions by modulating calcium mobilization in intestinal smooth muscle, making it a valuable tool in the study of gastrointestinal disorders. Otilonium bromide is widely utilized in research related to irritable bowel syndrome and other smooth muscle-related conditions.
Synonyms: Pilocarpine HCl; NSC 5746 HCl; (+)-Pilocarpine hydrochloride
Pilocarpine Hydrochloride is a selective agonist for the M3 muscarinic acetylcholine receptor (mAChR). It plays a significant role in stimulating glandular secretion, particularly in the treatment of dry mouth and glaucoma. This compound is valuable in research focused on neuropharmacology, as well as studies investigating cholinergic signaling and its implications in various physiological processes.
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.
BQCA is a highly selective positive allosteric modulator of the M1 muscarinic acetylcholine receptor (mAChR).
Synonyms: Acetyl-beta-methylcholine chloride; Provocholine; Mecholyl chloride; Amechol; Methapharma Brand of Methacholine Chloride; Provokit; Roche Brand of Methacholine Chloride
Methacholine chloride is a synthetic choline ester that acts as a non-selective muscarinic receptor agonist in the parasympathetic nervous system.
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: Carbastat; Carboptic; Isopto Carbachol; Miostat; Carbamylcholine
Carbamoylcholine chloride is used to study responses mediated by nAChR and mAChR, including smooth muscle contraction, gut motility, and neuronal signaling.
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.
Synonyms: Quinuclidin-3-yl acetate hydrochloride
Aceclidine hydrochloride is a selective modulator of the M3 muscarinic acetylcholine receptor and an agonist of the M1 receptor (EC50: 40 μM). This compound exhibits cycloplegic properties, functioning as a surfactant and tonicity adjustor while optionally enhancing viscosity and providing antioxidant effects. Aceclidine hydrochloride is valuable in research pertaining to ocular disorders, including refractive errors, glaucoma, xerostomia, conjunctivitis, Sjogren's syndrome, lacrimal gland diseases, and esotropia.
Camylofine is an antimuscarinic compound that selectively inhibits muscarinic acetylcholine receptors (mAChRs). It functions as a smooth muscle relaxant, making it useful in various research applications related to muscle contraction and neurotransmission. This compound is valuable for studying the physiological effects of cholinergic signaling and exploring potential therapeutic interventions for conditions related to smooth muscle hyperactivity.
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.
