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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Citations
  1. Catharanthine sulfate is a vinblastine-type alkaloid precursor with antitumor activity. It inhibits AChR by ion channel blocking and desensitization.
  2. mAChR agonist

    AC260584 is an M1 muscarinic receptor allosteric agonist with a pEC50 of 7.6.
  3. muscarinic M(3) receptor antagonist

    PF-3635659 is a potent muscarinic M(3) receptor antagonist.
  4. mAChR agonist

    Xanomeline oxalate is a potent agonist of muscarinic acetylcholine receptors (EC50 values are 0.3, 92.5, 5, 52, and 42 nM for M1, M2, M3, M4, and M5, respectively).
  5. mAChR antagonist

    AF-DX 384 is a drug which acts as a selective antagonist of the muscarinic acetylcholine receptors.
  6. M1 mAChR agonist

    TBPB is an allosteric M1 mAChR agonist with EC50 value of 89 nM that regulates amyloid processing and produces antipsychotic-like activity in rats.
  7. AchR agonist

    Nitenpyram is a nicotinic acetylcholine receptor (AchR) agonist.
  8. M2/M3 antagonist

    Diphenidol HCl is a potent antagonist of muscarinic M2 and M3 receptor with pKb of 6.72 and 7.02.
  9. mAChR PAM

    BQCA is a highly selective positive allosteric modulator of the M1 muscarinic acetylcholine receptor (mAChR).
  10. Muscarinic receptor agonist

    Methacholine chloride is a synthetic choline ester that acts as a non-selective muscarinic receptor agonist in the parasympathetic nervous system.
  11. muscarinic antagonist

    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.
  12. Muscarinic antagonist

    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.
  13. Carbamoylcholine chloride is used to study responses mediated by nAChR and mAChR, including smooth muscle contraction, gut motility, and neuronal signaling.
  14. Muscarinic antagonist

    Mepenzolate Bromide is a muscarinic antagonist used to treat gastrointestinal disorders. It decreases the severity of elastase-induced airspace enlargement and respiratory dysfunction.
  15. M1 muscarinic receptor antagonist

    Pirenzepine dihydrochloride (LS519) is a selective M1 muscarinic receptor antagonist.
  16. Pirmenol hydrochloride inhibits IK.ACh by blocking muscarinic receptors. The IC50 of Pirmenol for inhibition of Carbachol-induced IK.ACh is 0.1 μM.
  17. mAChR antagonist

    Atropine methyl bromide, a muscarinic receptor (mAChR) antagonist, is a quaternary ammonium salt of atropine and a mydriatic for dilation of the pupil during ophthalmic examination. It is introduced for relieving pyloric spasm in infants for its highly polar nature. It penetrates less readily into the central nervous system than atropine.
  18. mAChR agonist

    Cevimeline (Evoxac) Hcl is a parasympathomimetic and muscarinic agonist, with particular effect on M3 receptors; used in the treatment of dry mouth associated with sjogren's syndrome.
  19. Piperidolate hydrochloride is an antimuscarinic, Also a potential inhibitor of human glutathione transferase P1-1.
  20. alpha-1 adrenergic receptors / mAChRs inhibitor

    Anisodamine is an inhibitor of alpha-1 adrenergic receptors and mAChRs isolated from Chinese solanacea plant.
  21. mAChR inhibitor

    Piperidolate is a tertiary amine antimuscarinic. It is similar to atropine. It is mainly used in the smooth muscle spasm of the gastrointestinal tract and inhibits intestinal cramp induced by acetylcholine in rats and dogs.
  22. mAChR antagonist

    Cimetropium Bromide (DA-3177) is a mAChR antagonist for long-term treatment of irritable bowel syndrome.
  23. M4 modulator

    VU6005806 (AZN-00016130) is a potent muscarnic acethylcholine receptor subtype 4 (M4) positive allosteric modulator (PAM), with EC50s of 94 nM, 28 nM, 87 nM and 68 nM for human, rat, dog and cyno M4, respectively. Used in the research of neuropsychiatric disorders.
  24. muscarinic receptor antagonist

    Revefenacin is potent and selective muscarinic receptor antagonist in development for the treatment of COPD.
  25. 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.
  26. Choline bitartrate is a form of the nutrient choline which is found in foods.
  27. Diphemanil methylsulfate is a quaternary ammonium anticholinergic.
  28. Muscarinic Receptor Antagonist

    Solifenacin is a novel muscarinic receptor antagonist with pKis of 7.6, 6.9 and 8.0 for M1, M2 and M3 receptors, respectively.
  29. hM3Dq agonist.

    DREADD agonist 21 is a potent human muscarinic acetylcholine M3 receptors (hM3Dq) agonist(EC50=1.7 nM).
  30. Sigma-1 receptor agonist/muscarinic M1 agonist

    Blarcamesine, also known as AVex-73 and AE-37, is a muscarinic M1 agonist potentially for the treatment of Alzheimer's disease. It is an ς receptor ligand.
  31. mAChR modulator

    Rapacuronium bromide is an allosteric modulator of muscarinic acetylcholine receptor (mAChR).
  32. mAChR antagonist

    mAChR-IN-1 hydrochloride is a potent muscarinic cholinergic receptor (mAChR) antagonist, with an IC50 of 17 nM.
  33. M3 muscarinic receptor antagonist

    Tarafenacin D-tartrate (SVT-40776 D-tartrate) is a highly selective M3 muscarinic receptor antagonist (Ki= 0.19 nM), ~200 fold selectivity over M2 receptor.
  34. mAChR antagonist

    Elucaine is a muscarinic acetylcholine receptor antagonist with anti-ulcerative activity.
  35. mAChR modulator

    VU0467154 is a positive allosteric modulator of the M4 muscarinic acetylcholine receptor (mAChR), potentiating the response to ACh with pEC50s of 7.75, 6.2 and 6 for rat, human and cynomolgus monkey M4 receptor, respectively.
  36. mAChR M5 positive allosteric modulator

    VU 0365114 is a mAChR M5 positive allosteric modulator, with an EC50 of 2.7 μM.
  37. M3 muscarinic receptor antagonist

    YM-58790 is a potent antagonist of M3 muscarinic receptor, with Ki of 15 nM.
  38. M5 NAM

    VU 6008667 is a selective negative allosteric modulator of M5 NAM with IC50s of 1.2 μM and 1.6 μM for human M5 and rat M5, respectively. High CNS penetration.
  39. muscarinic agonist

    Talsaclidine is a muscarinic agonist with preferential neuron-stimulating properties. Talsaclidine is a full agonist at the M1 subtype, and as a partial agonist at the M2 and M3 subtypes.
  40. M1 modulator

    TAK-071 is a novel, potent and highly selective muscarinic acetylcholine receptor 1 (M1R) positive allosteric modulator. EC50 of TAK-071 M1R agonist activities is 520 nM.
  41. Dexetimide ((+)-Benzetimide) is a high-affinity muscarinic receptor antagonist and a potent and persistent anticholinergic agent used to treat neuroleptic-induced parkinsonism.
  42. partial M1 agonist and M2/M3 antagonist

    Alvameline (Lu25-109) is a partial M1 agonist and M2/M3 antagonist.
  43. Peimisine and peiminine production by endophytic fungus Fusarium sp. isolated from Fritillaria unibracteata var. wabensis.
  44. M1 agonist

    Cevimeline hydrochloride hemihydrate, a novel muscarinic receptor agonist, is a candidate therapeutic drug for xerostomia in Sjogren's syndrome.
  45. Muscarinic receptor antagonist

    Umeclidinium bromide(GSK573719A) is a muscarinic receptor antagonist which is useful in treatment of chronic obstructive pulmonary disease (COPD).
  46. M3 receptors inhibitor

    Imidafenacin is a potent and selective inhibitor of M3 receptors with Kb of 0.317 nM; less potent for M2 receptors(IC50=4.13 nM).
  47. mAChR antagonist

    mAChR-IN-1 is a potent muscarinic cholinergic receptor(mAChR) antagonist with IC50 of 17 nM.
  48. mAChR5 modulator

    VU 0238429 is positive allosteric modulator of muscarinic acetylcholine receptor subtype 5 (mAChR5 or M5), with an EC50 of 1.16 μM.
  49. mAChR M4 potentiator

    VU0152100 is a potent and selective allosteric potentiator of M4 mAChR with an EC50 of 380 ?? 93 nM.
  50. [3H](+)pentazocine binding inhibitor

    Levetimide is a potent and stereoselective inhibitor of [3H](+)pentazocine binding, with a Ki of 2.2 nM.

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