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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: Aroxybutynin
(R)-Oxybutynin is a potent muscarinic receptor antagonist employed in the investigation of neurogenic bladder dysfunction. This compound exhibits antispasmodic, antimuscarinic, and anticholinergic properties, effectively inhibiting carbachol-induced contractions. It serves as a valuable tool for studying urinary incontinence and related conditions.
VU6021625 is a selective antagonist of the M4 muscarinic acetylcholine receptor (mAChR), exhibiting an IC50 of 0.44 nM for human M4 and 57 nM for rat M4. This compound is valuable for studies exploring the role of M4 receptors in neurological processes and potential therapeutic targets for neurodegenerative diseases. Its selectivity and potency make it an important tool for researchers investigating cholinergic signaling pathways.
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TD-6301 is a potent antagonist of the M2 and M4 muscarinic receptors, demonstrating high selectivity and strong affinity for the human M2 receptor (Ki = 0.36 nM). This compound effectively inhibits volume-induced bladder contractions (ID50 = 0.075 mg/kg), making it a valuable tool in the study of overactive bladder conditions. Its specificity for bladder tissues presents opportunities for targeted therapeutic research in urology and related fields.
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Synonyms: Daturine sulfate hydrate
L-Hyoscyamine sulfate hydrate is a potent and competitive antagonist of muscarinic acetylcholine receptors (mAChR). As a naturally occurring tropane alkaloid, it exhibits significant biological activity by inhibiting mAChR-mediated signaling pathways. This compound is primarily utilized in pharmacological research and studies related to the modulation of synaptic transmission, making it valuable for investigating various physiological and pathological processes.
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Bibn 140 is a pyridine derivative that acts as a selective antagonist of the M2 muscarinic acetylcholine receptor (mAChR), exhibiting high affinity with a Ki value of 12 nM. This compound is primarily utilized in research exploring cholinergic signaling and its implications in neurological disorders. Its specificity for the M2 subtype over the M1 receptor positions it as a valuable tool for studying M2 receptor-related biological processes.
Synonyms: (S)-FK-176
(S)-Vamicamide is a selective antagonist of the muscarinic acetylcholine receptors (mAChRs). This compound exhibits notable anticholinergic activity, making it useful for studies related to neurotransmission and receptor signaling pathways. Its application extends to research in conditions influenced by cholinergic modulation, such as cognitive disorders and movement disorders.
Synonyms: FK-176
Vamicamide is a competitive antagonist of muscarinic acetylcholine receptors (mAChRs) that functions by inhibiting the binding of mAChR agonists, thereby preventing contractions induced by cholinergic nerve stimulation. It demonstrates significant anti-bladder spasm effects, exhibiting a pA2 value of 6.82 in bladder tissue. Vamicamide is valuable for research in the study of neurological diseases and disorders related to bladder dysfunction.
AZD-9164 bromide is a long-acting antagonist of the muscarinic M3 receptor. It demonstrates significant potential for modulating airway smooth muscle contraction and has applications in the study of respiratory diseases, including chronic obstructive pulmonary disease (COPD) and asthma. Researchers may utilize AZD-9164 bromide to explore mechanisms underlying bronchoconstriction and to develop targeted therapies for these conditions.
Synonyms: Ponalid; UK 738
Ethybenztropine is a muscarinic receptor blocker, functioning primarily as an anticholinergic agent. It inhibits the action of acetylcholine at muscarinic receptors, thereby exerting antihistaminergic effects. This compound is utilized in research applications that explore cholinergic signaling pathways and the role of muscarinic receptors in various biological processes.
Synonyms: L-erythro-Neopterin
L-(-)-Neopterin (L-erythro-Neopterin) is a competitive antagonist of cholinergic receptors, mitigating the inhibitory effects of pteridine diuretics on the growth of Crithidia fasciculata. This compound is valuable in studies investigating nervous system functions and purine metabolism, providing insights into neurochemical pathways and potential therapeutic applications.
Synonyms: Ponalid hydrobromide; UK 738 hydrobromide
Ethybenztropine hydrobromide is a muscarinic receptor blocker with notable antiparkinsonian activity. This anticholinergic agent functions to alleviate symptoms associated with Parkinson's disease, potentially enhancing dopaminergic signaling by acting as a dopamine reuptake inhibitor. It is widely utilized in research exploring therapeutic strategies for managing Parkinson’s disease and related movement disorders.
Muscarinic M3 receptor antagonist-2 is a selective antagonist of the muscarinic M3 receptor, crucial in mediating various physiological responses. This compound demonstrates potency in inhibiting M3 receptor activity, making it valuable for research into disorders related to cholinergic signaling and smooth muscle contraction. Its application is particularly relevant in studies focused on airway diseases, gastrointestinal motility, and other conditions associated with M3 receptor dysregulation.
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YM-58790 free base is a potent antagonist of the muscarinic acetylcholine receptors (mAChR), specifically targeting the M3 subtype with a Ki value of 15 nM, along with M1 and M2 subtypes at 28 nM and 260 nM, respectively. This compound demonstrates significant inhibitory effects on bladder pressure during reflexly-evoked rhythmic contractions in rat studies. YM-58790 free base is used in research focused on neuropharmacology and the modulation of cholinergic signaling pathways, particularly in relation to bladder function and potential therapeutic applications in urological disorders.
Muscarinic M3 receptor antagonist-1 functions as an antagonist of the muscarinic acetylcholine receptor M3. It plays a crucial role in the study of inflammatory and obstructive airway diseases, providing insights into potential therapeutic interventions. This reagent aids in the exploration of M3 receptor-mediated pathways and their implications in respiratory conditions.
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Synonyms: HSR-902
Tiquizium bromide is a nonselective muscarinic antagonist that acts as an atropine-type spasmolytic agent. It effectively inhibits the development of gastric and duodenal lesions, while also inducing mydriasis and reducing salivation induced by pilocarpine. This compound is useful in pharmacological studies aimed at exploring muscarinic receptor modulation and its physiological effects.
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Parapenzolate bromide is an orally active antagonist of muscarinic acetylcholine receptors (mAChRs). As an anticholinergic agent, it demonstrates antispasmodic properties, making it useful for studies related to gastrointestinal motility and smooth muscle relaxation. This compound is valuable in research applications focusing on the modulation of cholinergic signaling and its effects on various physiological processes.
Trihexyphenidyl is a selective M1 muscarinic receptor antagonist, with an IC50 of 3.7 nM for rat cerebral cortex M1 receptors. It modulates cholinergic activity, effectively countering acetylcholine supersensitivity in neural pathways. Trihexyphenidyl is utilized in research for Parkinson's disease and demonstrates efficacy in improving movement disorders, as well as inhibiting vagally-induced bradycardia and vasodilation. Its inhibition of McN-A-343-induced pressor responses highlights its potential in studying neurophysiological effects.
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MK-0969 is an M3 muscarinic acetylcholine receptor antagonist. It exhibits biological activity relevant to the modulation of smooth muscle tone, making it useful in the study of conditions such as chronic obstructive pulmonary disease and urinary incontinence. Researchers can employ MK-0969 to investigate the therapeutic potential of M3 receptor inhibition in respiratory and urological disorders.
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Sintropium bromide is a muscarinic acetylcholine receptor (mAChR) antagonist that exerts notable anticholinergic effects. Its primary biological activity includes alleviating pain and reducing muscle spasms, making it a valuable tool for research in pain management and neuromuscular studies.
J-104129 is a selective antagonist of the M3 muscarinic receptor, exhibiting a Ki value of 4.2 nM. This compound demonstrates significant bronchodilatory effects, making it useful in studying respiratory disorders. Its oral bioactivity supports its application in pharmacological research focusing on muscarinic receptor modulation.
Oxyphencyclimine is an orally active antagonist of muscarinic acetylcholine receptors (mAChR). This compound is demonstrated to reduce ulceration index and enhance pepsin activity in rat models of gastric ulcers. Oxyphencyclimine is suitable for investigation in studies related to peptic ulcer disease and gastrointestinal spasms, providing a valuable tool for understanding these conditions.
Petiline is a steroidal alkaloid that serves as a selective antagonist of M cholinergic receptors. By competitively inhibiting these receptors, Petiline demonstrates significant anticholinergic effects, including a reduction in vagal influence on cardiac function. Additionally, it exhibits central excitatory, cardiotonic, and spasmolytic activities, making it a valuable tool for investigating cholinergic system-related disorders such as arrhythmias and intestinal spasms.
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Synonyms: Tropine tropate hydrobromide; DL-Hyoscyamine hydrobromide
Atropine hydrobromide is a competitive antagonist of muscarinic acetylcholine receptors (mAChRs), demonstrating IC50 values of 0.39 nM and 0.71 nM for human mAChR M4 and chicken mAChR M4, respectively. It effectively inhibits acetylcholine-induced relaxations in human pulmonary veins. This compound is valuable for research applications related to anti-myopia and the treatment of bradycardia.
Synonyms: KL 373 lactate
Biperiden lactate is a non-selective muscarinic receptor antagonist that competitively interacts with M1 muscarinic receptors. This compound inhibits acetylcholine activity, thus enhancing dopamine signaling within the central nervous system. Biperiden lactate is particularly useful for research into Parkinson's disease and related psychiatric disorders, providing insights into therapeutic strategies aimed at managing these conditions.
Synonyms: Parpanil hydrochloride
Caramiphen hydrochloride is a muscarinic antagonist that exhibits anticonvulsant properties. It provides partial protection against seizures and neuropathological effects induced by Soman exposure. This compound is valuable for research focused on exploring therapeutic strategies for seizure disorders and understanding the underlying mechanisms of muscarinic receptor modulation.
