mAChR

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:

  • M1 Receptors: Predominantly found in the central nervous system, particularly in regions associated with cognitive functions. Activation of M1 receptors is linked to memory and learning.
  • M2 Receptors: Found in the heart, where they play a crucial role in regulating heart rate and cardiac contractility. Activation of M2 receptors slows heart rate and reduces the force of cardiac contractions.
  • M3 Receptors: Present in smooth muscle tissues, such as those in the gastrointestinal tract, urinary bladder, and bronchial airways. Activation of M3 receptors leads to smooth muscle contraction.
  • M4 Receptors: Distributed mainly in the central nervous system and involved in modulating neurotransmitter release. Their role in cognition and neuropsychiatric disorders is of interest.
  • M5 Receptors: Located in certain areas of the brain and implicated in the modulation of dopamine release. Research suggests they may be relevant to Parkinson's disease and addiction.

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.

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  1. mAChR Agonist

    CDD0102 Hydrochloride is a potent agonist of the M1 muscarinic acetylcholine receptor (mAChR). This compound exhibits significant biological activity in modulating cholinergic signaling, making it valuable for research into neurological disorders and cognitive function. Its application extends to studying M1 receptor-related pathways and developing potential treatments for conditions such as Alzheimer's disease and schizophrenia.
  2. mAChR Antagonist

    4,4-Difluorobenzhydrol serves as a precursor for a muscarinic acetylcholine receptor (mAChR) antagonist, with potential applications in neuroscience research. Its derivative, 4,4-Difluorobenzhydrol Carbamate, can selectively target the M1 receptor subtype. This specificity makes 4,4-Difluorobenzhydrol an important compound for studying the physiological roles of mAChRs and developing therapeutics for related disorders.
  3. Anticholinergic Agent

    Pridinol is a muscarinic acetylcholine receptor (mAChR)-directed anticholinergic agent that demonstrates muscle relaxant properties. This compound effectively reduces impulse conduction to spinal motor neurons, resulting in decreased muscle contractures associated with various musculoskeletal disorders. Pridinol is valuable for research applications focused on both central and peripheral origins of muscle dysfunction, making it a significant tool for the study of neuromuscular conditions.
  4. mAChR M1 Modulator

    VU0366369 is a selective positive allosteric modulator (PAM) of the muscarinic acetylcholine receptor subtype M1, exhibiting an EC50 value of 830 nM. This compound has demonstrated potential for enhancing M1 receptor function, making it a valuable tool in the study of central nervous system disorders. Researchers may utilize VU0366369 to explore therapeutic strategies for conditions such as Alzheimer's disease and schizophrenia, focusing on cholinergic signaling pathways.
  5. Prolyl Endopeptidase (PREP) Inhibitor

    ONO 1603 is a selective inhibitor of prolyl endopeptidase (PREP), investigated for its potential in antidementia therapy. This compound has demonstrated neuroprotective properties and neurotrophic effects in cerebellar granule cells, enhancing neuronal survival and promoting neurite outgrowth at a concentration of 0.03 µM. Additionally, ONO 1603 increases m3-muscarinic acetylcholine receptor (mAChR) mRNA levels and stimulates mAChR-mediated signaling pathways. These pharmacological properties suggest that ONO 1603 could be a promising therapeutic agent for Alzheimer's disease by enhancing cholinergic neurotransmission and supporting neuronal function.
  6. Intermediate

    4-Bromo-2-hydroxypyridine serves as an important intermediate in organic synthesis, specifically for the development of positive allosteric modulators of the M1 muscarinic acetylcholine receptor (M1 mAChR). Its biological activity makes it a valuable compound in research related to neurodegenerative disorders such as Alzheimer's disease and psychiatric conditions like schizophrenia. This reagent is essential for advancing studies aimed at understanding and targeting cholinergic dysfunction in these diseases.
  7. ML375 Enantiomer

    (R)-ML375 is an enantiomer of ML375, primarily targeting the muscarinic acetylcholine receptor subtype M5 (hM5). This compound is characterized by its lack of significant activity on M5 mAChR, exhibiting an IC50 greater than 30 μM. (R)-ML375 is suitable for studies exploring the role of muscarinic receptors in physiological and pathological processes, providing a valuable tool for chemical research in neuronal signaling and related fields.
  8. nAChR/mAChR Agonist

    Arecoline hydrobromide is a partial agonist of nicotinic (nAChR) and muscarinic acetylcholine receptors (mAChR). This naturally occurring psychoactive alkaloid possesses brain-penetrant properties and is known for its stimulation, alertness enhancement, anxiolytic effects, and anti-parasitic activity. Additionally, Arecoline hydrobromide can induce oxidative stress, making it valuable for research in neuropharmacology and related fields.
  9. mAChR Antagonist

    Oxybutynin chloride is a competitive antagonist of muscarinic acetylcholine receptors (mAChRs), exhibiting binding affinities with Ki values of 14.3 nM and 5.55 nM for [3H]NMS in mouse bladder and cerebral cortex, respectively. It effectively inhibits vascular Kv channels with an IC50 of 11.51 μM, independent of its anticholinergic effects. Oxybutynin chloride is primarily utilized for the management of overactive bladder syndrome (OAB) and alleviating bladder and urinary tract muscle spasms. Additionally, it serves as a click chemistry reagent due to its alkyne functionality, enabling copper-catalyzed azide-alkyne cycloaddition (CuAAc) reactions with azide-containing molecules.
  10. mAChR Antagonist

    Atropine methyl nitrate is a muscarinic acetylcholine receptor (mAChR) antagonist, primarily utilized for its ability to induce pupil dilation (mydriasis) during ophthalmic examinations. This quaternary ammonium derivative is specifically formulated for the treatment of pyloric spasms in infants due to its high polarity, which limits its central nervous system penetration compared to its parent compound, atropine. Research applications include studying cholinergic signaling pathways and exploring therapeutic strategies for gastrointestinal disorders.
  11. mAChR Antagonist

    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.
  12. mAChR Inhibitor

    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.
  13. mAChR Antagonist

    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.
  14. mAChR Antagonist

    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.
  15. mAChR Inhibitor

    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.
  16. mAChR Modulator

    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.
  17. mAChR Inhibitor

    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.
  18. mAChR Antagonist

    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.
  19. mAChR Antagonist

    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.
  20. mAChR Antagonist

    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.
  21. mAChR Inhibitor

    Tolterodine is an mAChR inhibitor that competitively binds to acetylcholine, leading to a reduction in sympathetic excitation and inhibition of involuntary bladder muscle contractions. It is known to restore the Nrf2/NF-κB signaling pathway, providing protection against inflammatory responses and ferroptosis. Additionally, Tolterodine mitigates LPS-induced reactive oxygen species production and lipid oxidation, making it valuable for research in urinary tract infections and overactive bladder conditions.
  22. Muscarinic Receptor Antagonist

    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.
  23. Anticholinergic Agent

    Pridinol mesylate is an anticholinergic agent that targets muscarinic acetylcholine receptors (mAChRs) to provide muscle relaxation. It effectively reduces impulse conduction to spinal motor neurons, exhibiting significant muscle relaxant properties. Pridinol mesylate is useful in research related to musculoskeletal diseases, particularly for investigating skeletal muscle contractures arising from both central and peripheral origins. Its blood-brain permeability facilitates its application in studies involving central nervous system effects.
  24. mAChR Inhibitor

    Trospium chloride is a selective and competitive antagonist of muscarinic acetylcholine receptors (mAChRs). It exhibits potent antimuscarinic activity by binding with high affinity to M1, M2, and M3 receptor subtypes, while showing no interaction with nicotinic cholinergic receptors. This compound is primarily utilized in research related to neurological conditions and to explore the pharmacological modulation of cholinergic signaling.
  25. mAChR Antagonist

    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.
  26. mAChR Agonist

    Muscarine is a selective agonist of muscarinic acetylcholine receptors (mAChRs), predominantly affecting the parasympathetic nervous system. This compound is recognized for its ability to stimulate various biological responses such as increased glandular secretions and smooth muscle contraction. Muscarine is utilized in research applications to investigate cholinergic signaling pathways and the physiological effects of parasympathetic activation.
  27. Central Cholinoreceptor Modulator

    Eucatropine hydrochloride is a potent inhibitor of muscarinic acetylcholine receptors (mAChRs), exhibiting an IC50 value of 0.583 μM. As an anticholinergic agent, it modifies cholinergic signaling, leading to significant behavioral effects. This compound is particularly relevant for research applications focused on central cholinoreceptor modulation and its effects on physiological and behavioral outcomes in animal models.
  28. mAChR Agonist

    Muscarine chloride is a potent agonist of muscarinic acetylcholine receptors (mAChRs). As a biologically active compound, it simulates the parasympathetic nervous system, making it a valuable tool in neuropharmacological research. Muscarine chloride is utilized in studies examining neurotransmission, receptor signaling pathways, and the effects of cholinergic modulation in various biological systems.

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