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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: UK-112166
Revatropate is a potent muscarinic antagonist primarily targeting M1 and M3 receptors with significantly greater inhibitory effects compared to the M2 subtype. This compound is valuable in the investigation of urge urinary incontinence and functional bowel disorders, facilitating research into the modulation of cholinergic signaling in these conditions.
Desiodomethyl 4-DAMP is a selective antagonist of muscarinic receptors, inhibiting acetylcholine-mediated signaling. This compound is utilized in various pharmacological studies to investigate the role of muscarinic receptors in physiological processes and disease models. Its application extends to research involving neurotransmission, cognitive function, and potential therapeutic interventions for conditions linked to cholinergic dysregulation.
Synonyms: Atropine oxidation hydrochloride
Atropine oxide hydrochloride is a competitive antagonist of muscarinic acetylcholine receptors, including M1, M2, M3, M4, and M5. It demonstrates key biological activity in antagonizing acetylcholine's effects, making it valuable in research focused on neurotransmission and receptor signaling. This reagent is particularly significant for studies involving the therapeutic applications in specific nerve agent and pesticide poisonings.
DAC 5945 is a potent muscarinic antagonist primarily targeting M1 and M2 receptors, exhibiting pKi values of 8.3 and 7.52, respectively. Its selectivity for the airways over cardiac tissue makes it a valuable compound for research related to respiratory disorders. DAC 5945 can be employed in investigations of airway smooth muscle modulation and in studies aimed at understanding the role of muscarinic receptors in various physiological and pathological processes.
(Rac)-5-Carboxy tolterodine is an inactive metabolite of the muscarinic acetylcholine receptor antagonist Tolterodine. It serves as a valuable control in studies involving muscarinic receptors, particularly in the context of acetylcholine modulation. This compound is useful for researchers investigating the pharmacokinetics and metabolic pathways of Tolterodine and related drugs.
LG50643 is a selective antagonist of the M3 muscarinic receptor, exhibiting a high binding affinity with a pKi of 8.64. This compound plays a significant role in research related to neuropharmacology and the modulation of cholinergic signaling pathways. Its ability to inhibit M3 receptor activity makes it valuable for studying various physiological processes and the potential therapeutic effects related to muscarinic receptor dysfunction.
Synonyms: PNU-200577 formic
5-Hydroxymethyl tolterodine formate is a potent antagonist of muscarinic acetylcholine receptors (mAChR). This active metabolite, derived from tolterodine and fesoterodine through the action of CYP2D6 and plasma esterases respectively, has significant implications in the study of urinary disorders. Researchers can utilize 5-Hydroxymethyl tolterodine formate in pharmacological investigations of cholinergic signaling and its effects on smooth muscle activity, contributing to the understanding of treatment options for overactive bladder and related conditions.
Synonyms: Lu 25-109 maleate
Alvameline maleate is a muscarinic acetylcholine receptor (mAChR) antagonist with selective activity at the M2 and M3 subtypes, while acting as a partial agonist for the M1 subtype. This compound has demonstrated the ability to competitively inhibit contractions in human detrusor muscle induced by ammonium chloride and electrical field stimulation, highlighting its potential for applications in bladder function regulation. Furthermore, alvameline maleate has shown promise in enhancing cognitive function following traumatic brain injury in rodent models, making it a valuable tool for research in both urology and neuropharmacology.
Temiverine hydrochloride is a mAChR antagonist exhibiting anticholinergic activity. This compound is also a versatile click chemistry reagent, featuring an alkyne group that enables the copper-catalyzed azide-alkyne cycloaddition (CuAAC) with azide-containing molecules. Its applications extend to chemical biology, facilitating the development of novel therapeutics and biochemical probes.
Synonyms: BL700
Ambutonium bromide is a selective antagonist of the muscarinic acetylcholine receptors (mAChRs). By inhibiting the action of acetylcholine, it plays a significant role in modulating cholinergic signaling pathways. This compound is primarily utilized in research applications aimed at studying the effects of mAChR inhibition in various physiological and pathological contexts.
WIN 62,577 is a selective antagonist of muscarinic acetylcholine receptors (mAChRs), specifically targeting M1 to M4 subtypes. This compound acts as an allosteric enhancer of acetylcholine affinity at the M3 receptor, making it a valuable tool for studying cholinergic signaling. Its unique properties allow for exploration of mAChR-related pathways and their implications in various physiological and pathological conditions. Suitable for research applications in neurobiology and pharmacology, WIN 62,577 facilitates investigations into receptor functions and potential therapeutic targets.
Cyclodrine hydrochloride is a potent antagonist of muscarinic acetylcholine receptors (mAChRs). It is primarily utilized in research to investigate cholinergic signaling pathways and the role of mAChR in various physiological and pathological processes. This compound may aid in the exploration of potential therapeutic targets for disorders influenced by cholinergic activity.
YM-46303 is an antagonist of muscarinic acetylcholine receptors (mAChR), demonstrating high affinity for both M1 and M3 subtypes, with notable selectivity for the M3 receptor over the M2 receptor. This compound is valuable in the study of receptor signaling pathways and can be utilized in research involving neurological disorders, smooth muscle contraction, and other cholinergic system-related investigations. Its specificity makes it a useful tool for elucidating the roles of mAChR subtypes in various biological processes.
Synonyms: Tricyclamol; (±)-Procyclidine
Procyclidine is a muscarinic receptor antagonist with additional NMDA antagonist properties. It is primarily utilized in research related to Parkinson's disease and associated psychiatric disorders, including Soman-induced epilepsy. Procyclidine’s mechanism of action facilitates investigations into cholinergic dysfunction and therapeutic strategies for movement disorders.
Homatropine is a muscarinic acetylcholine receptor (mAChR) antagonist with significant anticholinergic properties. This compound exhibits capacity to modulate activities mediated by the mAChR pathway, making it useful in various pharmacological studies. Homatropine is commonly employed in research applications focused on neurology and pharmacology to investigate cholinergic signaling and its implications for therapeutic approaches.
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Synonyms: DL-Cyclopentolate
Cyclopentolate is a muscarinic receptors antagonist that inhibits acetylcholine-mediated responses through its action on the ciliary muscle, with a pKB value of 7.8. This anti-muscarinic agent is primarily utilized in ophthalmology for inducing mydriasis and facilitating ocular examinations. Its efficacy in temporarily paralyzing the ciliary muscle makes it an essential tool in various eye care procedures.
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Synonyms: (-)-Scopolamine hydrochloride; Hyoscine hydrochloride
Scopolamine hydrochloride is a high-affinity muscarinic antagonist known for its ability to penetrate the blood-brain barrier. This compound effectively inhibits 5-HT3 receptors, exhibiting an IC50 value of 2.09 μM. Scopolamine hydrochloride is utilized in research settings to explore cognitive and memory impairment in animal models, as well as applications related to the prevention of postoperative nausea and vomiting, motion sickness, and various disorders of the nervous system.
