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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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Product Name
Application
Product Information
Product Citation
  1. A17371
    Procyclidine HCl

    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.
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  2. A17376
    Carbachol

    Carbamoylcholine chloride is used to study responses mediated by nAChR and mAChR, including smooth muscle contraction, gut motility, and neuronal signaling.
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  3. A17384
    Mepenzolate Bromide

    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.
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  4. A17916
    Pirenzepine dihydrochloride

    M1 muscarinic receptor antagonist

    Pirenzepine dihydrochloride (LS519) is a selective M1 muscarinic receptor antagonist.
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  5. A18009
    Pirmenol hydrochloride

    Pirmenol hydrochloride inhibits IK.ACh by blocking muscarinic receptors. The IC50 of Pirmenol for inhibition of Carbachol-induced IK.ACh is 0.1 μM.
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  6. A18026
    Atropine methyl bromide

    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.
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  7. A18092
    Cevimeline hydrochloride

    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.
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  8. A18144
    Piperidolate hydrochloride

    Piperidolate hydrochloride is an antimuscarinic, Also a potential inhibitor of human glutathione transferase P1-1.
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  9. A18215
    Anisodamine

    alpha-1 adrenergic receptors / mAChRs inhibitor

    Anisodamine is an inhibitor of alpha-1 adrenergic receptors and mAChRs isolated from Chinese solanacea plant.
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  10. A18257
    Piperidolate

    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.
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  11. A18290
    Cimetropium Bromide

    mAChR antagonist

    Cimetropium Bromide (DA-3177) is a mAChR antagonist for long-term treatment of irritable bowel syndrome.
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  12. A18488
    VU6005806

    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.
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  13. A18571
    Talsaclidine

    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.
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  14. A18626
    TAK-071

    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.
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  15. A19267
    Dexetimide

    Dexetimide ((+)-Benzetimide) is a high-affinity muscarinic receptor antagonist and a potent and persistent anticholinergic agent used to treat neuroleptic-induced parkinsonism.
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  16. A19271
    Alvameline

    partial M1 agonist and M2/M3 antagonist

    Alvameline (Lu25-109) is a partial M1 agonist and M2/M3 antagonist.
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  17. A19519
    Elucaine

    mAChR antagonist

    Elucaine is a muscarinic acetylcholine receptor antagonist with anti-ulcerative activity.
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  18. A19842
    VU0467154

    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.
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  19. A19896
    VU 0365114

    mAChR M5 positive allosteric modulator

    VU 0365114 is a mAChR M5 positive allosteric modulator, with an EC50 of 2.7 μM.
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  20. A19917
    YM-58790

    M3 muscarinic receptor antagonist

    YM-58790 is a potent antagonist of M3 muscarinic receptor, with Ki of 15 nM.
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  21. A20406
    VU 6008667

    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.
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  22. A20534
    DREADD agonist 21

    hM3Dq agonist.

    DREADD agonist 21 is a potent human muscarinic acetylcholine M3 receptors (hM3Dq) agonist(EC50=1.7 nM).
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  23. A21095
    Blarcamesine (AVex-73)

    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.
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  24. A21119
    Rapacuronium bromide

    mAChR modulator

    Rapacuronium bromide is an allosteric modulator of muscarinic acetylcholine receptor (mAChR).
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  25. A21398
    mAChR-IN-1 hydrochloride

    mAChR antagonist

    mAChR-IN-1 hydrochloride is a potent muscarinic cholinergic receptor (mAChR) antagonist, with an IC50 of 17 nM.
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  26. A21477
    Tarafenacin D-tartrate

    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.
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  27. A21518
    mAChR-IN-1

    mAChR antagonist

    mAChR-IN-1 is a potent muscarinic cholinergic receptor(mAChR) antagonist with IC50 of 17 nM.
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  28. A21519
    VU 0238429

    mAChR5 modulator

    VU 0238429 is positive allosteric modulator of muscarinic acetylcholine receptor subtype 5 (mAChR5 or M5), with an EC50 of 1.16 μM.
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  29. A21769
    VU0152100

    mAChR M4 potentiator

    VU0152100 is a potent and selective allosteric potentiator of M4 mAChR with an EC50 of 380 ?? 93 nM.
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  30. A21820
    Levetimide

    [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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  31. A21917
    Biperiden

    Muscarinic Receptor Antagonist

    Biperiden(KL 373) is an antiparkinsonian agent, which is the selective central M1 cholinoreceptors blocker.
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  32. A21936
    Aclidinium Bromide

    muscarinic antagonist

    Aclidinium Bromide(LAS 34273; LAS-W 330) is a long-acting, inhaled muscarinic antagonist as a maintenance treatment for chronic obstructive pulmonary disease (COPD).
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  33. A21939
    (Rac)-VU 6008667

    mAChR M5 negative allosteric modulator

    (Rac)-VU 6008667 is a selective negative allosteric modulator of muscarinic acetylcholine receptor subtype 5 (M5 NAM) (IC50=1.8 μM, pIC50= 5.75), has high CNS penetration.
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  34. A21977
    Oxotremorine M iodide

    mAChR agonist

    Oxotremorine M iodide is a potent and non-selective muscarinic acetylcholine receptor (mAChR) agonist.
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  35. A22204
    Perlapine

    hM3Dq DREADD agonist

    Perlapine is a potent and selective hM3Dq DREADD agonist (EC50 = 2.8 nM). This drug exhibits >10,000-fold selectivity for hM3Dq over hM3.
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  36. A22589
    Benzetimide hydrochloride

    muscarinic acetylcholine receptor antagonist

    Benzetimide hydrochloride is a muscarinic acetylcholine receptor antagonist.
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  37. A22684
    Nor-benzetimide

    mAChR antagonist

    Nor-benzetimide is a major metabolite of Benzetimide. Benzetimide is a mAChR antagonist with anticholinergic activity.
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