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 antagonist

    Atropine is a competitive antagonist for the muscarinic acetylcholine receptor types M1, M2, M3, M4 and M5.
  2. muscarinic receptor antagonist

    Biperiden hydrochloride is a muscarinic receptor antagonist that displays some selectivity for the M1 subtype
  3. Muscarinic receptor agonist

    Bethanechol is a parasympathomimetic choline carbamate that selectively stimulates muscarinic receptors without any effect on nicotinic receptors.
  4. AChR antagonist

    Fesoterodine fumarate is a medicine which is used in urinary urgency, reducing the frequency of passing urine and urge urinary incontinence
  5. mAChR M2 antagonist

    Gallamine Triethiodide is a mAChR M2 antagonist with pronounced cardioselectivity.
  6. Ipratropium bromide is a muscarinic antagonist, bronchodilator, N-Isopropyl salt of atropine.
  7. Rsogladine is an anti-gastric ulcer agent that facilitates gap-junctional intercellular communication through M1 muscarininc acetylcholine receptor binding.
  8. Methscopolamine bromide is a competitive antimuscarinic agent that blocks the binding of acetylcholine at muscarinic acetylcholine receptors (mAChR M).
  9. Oxybutynin(Ditropan) is an anticholinergic medication used to relieve urinary and bladder difficulties.
  10. AchR antagonist

    Rocuronium Bromide is a competitive AchR antagonist, used in modern anaesthesia.
  11. muscarinic receptor antagonist

    SVT-40776 is a novel M3 muscarinic receptor antagonist, for the treatment of overactive bladder.
  12. muscarinic acetylcholine receptor (mAChR) antagonist

    Tiotropium Bromide (BA679 BR) is a muscarinic acetylcholine receptor (mAChR) antagonist that blocks the binding of the acetylcholine ligand and subsequent opening of the ligand-gated ion channel.
  13. muscarinic receptor antagonist

    Tolterodine tartrate (Detrol LA) is a muscarinic receptor antagonist which is used for the treatment of urinary incontinence.
  14. muscarinic receptor antagonist

    5-hydroxymethyl tolterodine is a metabolite of Tolterodine, a muscarinic receptor antagonist used in the treatment of urinary incontinence.

  15. muscarinic M3 receptor antagoinst

    Solifenacin-succinate is a muscarinic M3 receptor antagoinst, used in treatment of urinary incontinence.
  16. M1/M3 receptor agonist

    Cevimeline (AF-102B) is a parasympathomimetic and muscarinic agonist, with particular effect on M3 receptors; used in the treatment of dry mouth associated with sjogren's syndrome.
  17. Nicotinic receptor agonist

    Metanicotine is a neuronal nicotinic receptor agonist, showing high selectivity for the ??4??2 subtype (Ki=26 nM); > 1,000 fold selectivity than ??7 receptors(Ki= 36000 nM).
  18. Tropicamide is an anticholinergic used as a mydriatic.
  19. NMDA receptor antagonist

    Orphenadrine citrate is a NMDA receptor antagonist with Ki of 6.0 +/- 0.7 μM, HERG potassium channel blocker.
  20. Methoctramine hydrate is a selective M2 muscarinic receptor antagonist at nM concentrations
  21. Darifenacin works by blocking the M3 muscarinic acetylcholine receptor, which is primarily responsible for bladder muscle contractions.
  22. Catharanthine sulfate is a vinblastine-type alkaloid precursor with antitumor activity. It inhibits AChR by ion channel blocking and desensitization.
  23. mAChR agonist

    AC260584 is an M1 muscarinic receptor allosteric agonist with a pEC50 of 7.6.
  24. muscarinic receptor inhibitor

    Darenzepine is a muscarinic receptor inhibitor extracted from patent US 20170095465 A1.
  25. acetylcholine receptor antagonist

    Beperidium iodide shows a competitive antagonistic effect against acetylcholine receptor with a pA2 of 7.93.
  26. Smilagenin (SMI) is a lipid-soluble small-molecule steroidal sapogenin from Rhizoma anemarrhenae and Radix asparagi widely used in traditional Chinese medicine for treating chronic neurodegeneration diseases.
  27. muscarinic antagonist

    Glycopyrrolate is a muscarinic competitive antagonist used as an antispasmodic.
  28. M1 receptor modulator

    MK7622 is a muscarinic M1 receptor positive allosteric modulator.
  29. muscarinic AChR antagonist

    Flavoxate binds and inhibits muscarinic receptors, thereby suppressing the micturition reflex and increases urinary bladder capacity by modifying the micturition center in the brain stem.
  30. Arecoline is a cholinergic alkaloid from seeds of the betel nut palm Areca catechu.
  31. muscarinic M(3) receptor antagonist

    PF-3635659 is a potent muscarinic M(3) receptor antagonist.
  32. 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).
  33. (-)-Nicotine ditartrate is a potent agonist of AChR (nicotinic acetylcholine recepto).
  34. mAChR antagonist

    AF-DX 384 is a drug which acts as a selective antagonist of the muscarinic acetylcholine receptors.
  35. 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.
  36. M2/M4 AChR agonist

    LY2119620 is a specific, and allosteric agonist of human M2 and M4 muscarinic acetylcholine receptors.
  37. AchR agonist

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

    Diphenidol HCl is a potent antagonist of muscarinic M2 and M3 receptor with pKb of 6.72 and 7.02.
  39. Peimisine and peiminine production by endophytic fungus Fusarium sp. isolated from Fritillaria unibracteata var. wabensis.
  40. M1 agonist

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

    Umeclidinium bromide(GSK573719A) is a muscarinic receptor antagonist which is useful in treatment of chronic obstructive pulmonary disease (COPD).
  42. 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).
  43. muscarinic receptor antagonist

    Revefenacin is potent and selective muscarinic receptor antagonist in development for the treatment of COPD.
  44. 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.
  45. Choline bitartrate is a form of the nutrient choline which is found in foods.
  46. Diphemanil methylsulfate is a quaternary ammonium anticholinergic.
  47. 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.
  48. mAChR PAM

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

    Methacholine chloride is a synthetic choline ester that acts as a non-selective muscarinic receptor agonist in the parasympathetic nervous system.
  50. 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.

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