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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: LY 246708 tartrate
Xanomeline tartrate is a potent agonist of the muscarinic M1 and M4 receptors, exhibiting antipsychotic-like activity. This compound enhances neuronal excitability and is primarily utilized in research focused on schizophrenia. Its mechanism provides valuable insights into potential therapeutic approaches for neuropsychiatric conditions.
DREADD agonist 21 dihydrochloride is a highly potent agonist of the human muscarinic acetylcholine M3 receptor (hM3Dq), with an EC50 value of 1.7 nM. This compound selectively activates hM3Dq, facilitating the study of neuronal signaling pathways in various research applications. Its utility in chemogenetics allows for precise modulation of cellular activity, making it an invaluable tool for investigating the roles of specific neuronal circuits in behavior and disease models.
Pilocarpine nitrate is a potent agonist of the M3 muscarinic acetylcholine receptor. It effectively stimulates muscarinic receptors, leading to increased salivation and glandular secretions. This compound is widely utilized in pharmacological research related to the treatment of dry mouth and glaucoma, as well as in studies of neurodegenerative diseases.
Oxotremorine sesquifumarate is an agonist of muscarinic acetylcholine receptors (mAChRs), primarily activating the M2 subtype. This compound is instrumental in neurological research, facilitating the study of cholinergic signaling and its implications in various neurological disorders. Its ability to modulate M2 receptor activity makes it valuable for investigating the physiological and pathophysiological roles of these receptors in the nervous system.
JHU37160 is a potent DREADD agonist that selectively targets hM3Dq and hM4Di receptors with EC50 values of 18.5 nM and 0.2 nM, respectively, in HEK-293 cells. This compound exhibits significant brain penetration and selectively displaces [3H]Clozapine from DREADD sites without affecting other Clozapine-binding sites in murine brain tissue. JHU37160 is valuable for research applications involving chemogenetics, neurobiology, and the exploration of neural circuits.
GSK1034702 is an allosteric agonist of the M1 muscarinic acetylcholine receptor (mAChR) with a pEC50 of 8.1 and the capability to cross the blood-brain barrier. It activates the Gq/11 protein-mediated signaling pathway, promoting neuronal firing and enhancing long-term potentiation (LTP) in the hippocampal CA1 region. This compound is valuable for investigating cognitive impairment mechanisms, including those related to Alzheimer's disease, and has demonstrated pro-cognitive effects in models of nicotine withdrawal cognitive dysfunction. Additionally, GSK1034702 may elicit certain side effects associated with peripheral M receptor activation, including gastrointestinal reactions.
Synonyms: CID-25010775
VU0357017 hydrochloride is a selective allosteric agonist of the M1 muscarinic acetylcholine receptor, demonstrating a potent efficacy with an EC50 of 477 nM. This compound exhibits high selectivity for the M1 receptor, showing no activity at M2-M5 subtypes even at concentrations up to 30 μM. VU0357017 hydrochloride is valuable for research applications related to Alzheimer's disease and schizophrenia.
M4 mAChR agonist-1 is a selective agonist targeting the M4 muscarinic acetylcholine receptor. This compound exhibits potent activation of the M4 receptor with an EC50 greater than 10 μM in human cell systems. It is valuable for research applications focused on studying cholinergic signaling and neuropharmacology.
Synonyms: Carbetapentane
Pentoxyverine is an orally active sigma-1 receptor agonist, exhibiting affinity with Kis of 41 nM for σ1, 894 nM for σ2, and 75 nM for guinea-pig brain membran σ1. This compound acts as a muscarinic antagonist and demonstrates significant biological activities, including antitussive, anticonvulsant, and spasmolytic effects. Pentoxyverine is utilized in research for its potential to inhibit bronchial interceptors, diminish the cough reflex, induce relaxation of bronchial smooth muscle, and reduce airway resistance in various pulmonary conditions.
LY593093 is a selective agonist of the muscarinic M1 receptor, demonstrating an EC50 of 22.8 nM. This compound is orally active and effectively penetrates the blood-brain barrier, making it a valuable tool for investigating mechanisms underlying Alzheimer's disease. Its selectivity for the muscarinic M1 receptor positions LY593093 as a promising reagent for research in neurodegenerative disorders.
Synonyms: ABET
Arecaidine but-2-ynyl ester tosylate is a selective agonist of the mAChR M2 receptor, known to induce dose-dependent reductions in mean arterial pressure and heart rate in rodent models. This compound serves as a valuable tool in cardiovascular disease research, elucidating the role of mAChR M2 in cardiac function. Additionally, as a click chemistry reagent, Arecaidine but-2-ynyl ester tosylate contains an alkyne functional group, enabling its application in copper-catalyzed azide-alkyne cycloaddition reactions with azide-containing molecules for further synthetic applications.
Synonyms: (+)-Muscarine iodide
Muscarine iodide is a potent agonist of the muscarinic acetylcholine receptors (mAChR). It actively stimulates the parasympathetic nervous system, making it a valuable tool in studying cholinergic signaling pathways. This compound is commonly utilized in research focused on neuropharmacology and the physiological effects of muscarinic receptor activation.
LASSBio-873 is a potent muscarinic acetylcholine receptor (mAChR) agonist that effectively crosses the blood-brain barrier. It exhibits significant analgesic properties in models of acute and inflammatory pain. Research indicates that the analgesic effects of LASSBio-873 can be antagonized by the M2 receptor inhibitor methoctramine, making it a valuable tool for studying pain mechanisms and mAChR signaling pathways.
JHU37152 is a potent agonist for Designer Receptors Exclusively Activated by Designer Drugs (DREADDs), specifically targeting the hM3Dq and hM4Di receptors with EC50 values of 5 nM and 0.5 nM, respectively, in HEK-293 cells. This compound demonstrates selective displacement of [3H]Clozapine from DREADD sites without affecting other Clozapine-binding sites in mouse brain tissue. JHU37152 is valuable for research applications involving neural circuit manipulation and the study of neuropharmacology.
Synonyms: AF-267B
NGX-267 is a selective agonist of the actin M1 receptor, demonstrating high selectivity among the five actin receptor subtypes, particularly favoring M1 over M3. This compound exhibits distinct affinity profiles for dopamine D2 and 5-HT2B receptors, highlighting its unique pharmacological properties. NGX-267 is valuable for research applications focused on actin receptor modulation and its implications in cellular dynamics and neurobiology.
Synonyms: WEB 1881 FU hydrochloride
Nebracetam hydrochloride is an orally active agonist of the M1 muscarinic receptor. It facilitates an increase in intracellular Ca2+ concentration, characterized by an EC50 value of 1.59 mM. This compound demonstrates neuroprotective properties and has potential to enhance cognitive function, making it relevant for research focused on neurological disorders, including Alzheimer's disease.
Synonyms: Carbamyl-β-methylcholine
Bethanechol is a selective agonist for muscarinic acetylcholine receptors (mAChRs), specifically targeting subtypes M1, M2, M3, M4, and M5. This parasympathomimetic compound promotes various parasympathetic responses, making it valuable in studies related to gastrointestinal motility, urinary retention, and other conditions influenced by parasympathetic activation. Research applications include evaluating the physiological effects of mAChR stimulation and investigating therapeutic strategies for disorders involving cholinergic transmission.
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M1/M4 Muscarinic Agonist 3 is a selective agonist for the M1 and M4 muscarinic acetylcholine receptors (mAChRs), exhibiting EC50 values of 31 nM and 9.3 nM, respectively. This compound is instrumental in the investigation of cholinergic signaling pathways and has potential applications in neurological research, particularly in the study of cognitive function and memory modulation. Its efficacy in activating M1/M4 receptors makes it a valuable tool for studying muscarinic receptor pharmacology.
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HTL-9936 is a selective agonist of the M1 muscarinic acetylcholine receptor (M1-mAChR), which plays a crucial role in cognitive function and memory. This compound demonstrates potential therapeutic effects in the context of neurodegenerative disorders, particularly Alzheimer's disease. HTL-9936 is a valuable tool for researchers investigating cholinergic signaling pathways and developing novel treatments for cognitive decline.
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Synonyms: (Rac)-SB-202026; (Rac)-Memric
(Rac)-Sabcomeline is a selective agonist for M1 and M4 muscarinic acetylcholine receptors (mAChRs), providing a valuable resource for investigating neurological disorders, particularly schizophrenia. Its activation of mAChRs can facilitate insights into cholinergic signaling pathways and their implications in neuropsychiatric conditions. This compound supports research into the development of therapeutic strategies targeting muscarinic receptors in the treatment of various cognitive and mood disorders.
Lu AE51090 is a selective agonist of the muscarinic M1 receptor, designed to penetrate the blood-brain barrier. This compound activates the human M1 receptor with an EC50 of 61 nM and demonstrates minimal activity at M2 to M5 receptors. Lu AE51090 has been shown to produce procognitive effects in murine models and is relevant for research into Alzheimer’s disease and cognitive impairments associated with schizophrenia.
Arecaidine-propargyl ester tosylate acts as a potent agonist of muscarinic acetylcholine receptors (mAChR). Its primary biological activity includes stimulation of mAChR, which is critical for neuropharmacological research and studies related to the central nervous system. This compound is useful for exploring the role of muscarinic signaling in various physiological processes and developing potential therapeutic strategies targeting mAChR pathways.
Synonyms: (Rac)-SB-202026 hydrochloride; (Rac)-Memric hydrochloride
(Rac)-Sabcomeline hydrochloride is a selective agonist of the M1 muscarinic acetylcholine receptor (mAChR). It exhibits potential neuroprotective effects and is of significant interest in research related to Alzheimer's disease and cognitive disorders. This compound is utilized in studies aimed at understanding the role of muscarinic receptors in synaptic plasticity and memory function.
Tazomeline is a selective agonist of the M1 muscarinic receptor, demonstrating significant inhibitory effects on twitch height in the rabbit vas deferens with an IC50 of 0.001 nM. This compound is primarily utilized in research focused on neuropsychiatric disorders, offering insights into the modulation of cholinergic signaling and potential therapeutic applications.
(Rac)-AF710B is a potent allosteric agonist targeting M1 muscarinic and σ1 receptors. This compound exhibits selective interactions that are valuable for elucidating the role of these receptors in neurological pathways. Its application in research focuses primarily on Alzheimer's disease, making it a significant reagent for studying potential therapeutic strategies.
