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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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  1. A10098
    Atropine

    mAChR antagonist

    Atropine is a competitive antagonist for the muscarinic acetylcholine receptor types M1, M2, M3, M4 and M5.
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  2. A10147
    Biperiden HCl

    muscarinic receptor antagonist

    Biperiden hydrochloride is a muscarinic receptor antagonist that displays some selectivity for the M1 subtype
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  3. A10386
    Fesoterodine fumarate (Toviaz)

    AChR antagonist

    Fesoterodine fumarate is a medicine which is used in urinary urgency, reducing the frequency of passing urine and urge urinary incontinence
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  4. A10417
    Gallamine triethiodide

    mAChR M2 antagonist

    Gallamine Triethiodide is a mAChR M2 antagonist with pronounced cardioselectivity.
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  5. A10476
    Ipratropium bromide

    Ipratropium bromide is a muscarinic antagonist, bronchodilator, N-Isopropyl salt of atropine.
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  6. A10803
    Rocuronium bromide

    AchR antagonist

    Rocuronium Bromide is a competitive AchR antagonist, used in modern anaesthesia.
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  7. A10808
    SVT-40776 (Tarafenacin)

    muscarinic receptor antagonist

    SVT-40776 is a novel M3 muscarinic receptor antagonist, for the treatment of overactive bladder.
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  8. A10934
    Tiotropium Bromide

    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.
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  9. A10937
    Tolterodine tartrate (Detrol LA)

    muscarinic receptor antagonist

    Tolterodine tartrate (Detrol LA) is a muscarinic receptor antagonist which is used for the treatment of urinary incontinence.
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  10. A11166
    5-hydroxymethyl tolterodine (PNU 200577)

    muscarinic receptor antagonist

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

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  11. A11215
    Solifenacin succinate

    muscarinic M3 receptor antagoinst

    Solifenacin-succinate is a muscarinic M3 receptor antagoinst, used in treatment of urinary incontinence.
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  12. A11712
    Orphenadrine citrate

    NMDA receptor antagonist

    Orphenadrine citrate is a NMDA receptor antagonist with Ki of 6.0 +/- 0.7 μM, HERG potassium channel blocker.
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  13. A12382
    Beperidium iodide

    acetylcholine receptor antagonist

    Beperidium iodide shows a competitive antagonistic effect against acetylcholine receptor with a pA2 of 7.93.
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  14. A12641
    Glycopyrrolate

    muscarinic antagonist

    Glycopyrrolate is a muscarinic competitive antagonist used as an antispasmodic.
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  15. A12900
    Flavoxate

    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.
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  16. A13548
    PF-3635659

    muscarinic M(3) receptor antagonist

    PF-3635659 is a potent muscarinic M(3) receptor antagonist.
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  17. A13856
    AF-DX 384

    mAChR antagonist

    AF-DX 384 is a drug which acts as a selective antagonist of the muscarinic acetylcholine receptors.
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  18. A14244
    Diphenidol HCl

    M2/M3 antagonist

    Diphenidol HCl is a potent antagonist of muscarinic M2 and M3 receptor with pKb of 6.72 and 7.02.
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  19. A15268
    Umeclidinium bromide

    Muscarinic receptor antagonist

    Umeclidinium bromide(GSK573719A) is a muscarinic receptor antagonist which is useful in treatment of chronic obstructive pulmonary disease (COPD).
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  20. A15986
    Revefenacin

    muscarinic receptor antagonist

    Revefenacin is potent and selective muscarinic receptor antagonist in development for the treatment of COPD.
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  21. A16947
    Solifenacin

    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.
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  22. A17354
    Anisotropine Methylbromide (CB-154)

    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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  23. 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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  24. 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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  25. A17916
    Pirenzepine dihydrochloride

    M1 muscarinic receptor antagonist

    Pirenzepine dihydrochloride (LS519) is a selective M1 muscarinic receptor antagonist.
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  26. 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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  27. 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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  28. A19519
    Elucaine

    mAChR antagonist

    Elucaine is a muscarinic acetylcholine receptor antagonist with anti-ulcerative activity.
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  29. 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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  30. 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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  31. 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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  32. 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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  33. A21917
    Biperiden

    Muscarinic Receptor Antagonist

    Biperiden(KL 373) is an antiparkinsonian agent, which is the selective central M1 cholinoreceptors blocker.
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  34. 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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  35. A22589
    Benzetimide hydrochloride

    muscarinic acetylcholine receptor antagonist

    Benzetimide hydrochloride is a muscarinic acetylcholine receptor antagonist.
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  36. 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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