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Home >> Signaling Pathways >> GPCR/G protein >> mAChR

mAChR

mAChRs (muscarinic acetylcholine receptors) are acetylcholine receptors that form G protein-receptor complexes in the cell membranes of certainneurons and other cells. They play several roles, including acting as the main end-receptor stimulated by acetylcholine released from postganglionic fibersin the parasympathetic nervous system. mAChRs are named as such because they are more sensitive to muscarine than to nicotine. Their counterparts are nicotinic acetylcholine receptors (nAChRs), receptor ion channels that are also important in the autonomic nervous system. Many drugs and other substances (for example pilocarpineand scopolamine) manipulate these two distinct receptors by acting as selective agonists or antagonists. Acetylcholine (ACh) is a neurotransmitter found extensively in the brain and the autonomic ganglia.

Targets for  mAChR

Products for  mAChR

  1. Cat.No. Product Name Information
  2. GC34957 (+)-Cevimeline hydrochloride hemihydrate

    (-)-SNI-2011; (-)-AF102B hydrochloride hemihydrate

     (+)-Cevimeline hydrochloride hemihydrate ((+)-SNI-2011), a potent muscarinic receptor agonist, is a candidate therapeutic drug for xerostomia in Sjogren's syndrome. (+)-Cevimeline hydrochloride hemihydrate Chemical Structure
  3. GC70383 (-)-Vesamicol (-)-Vesamicol (AH5183) is an inhibitor of acetylcholine transport into synaptic vesicles, with the IC50 of 75 nM. (-)-Vesamicol Chemical Structure
  4. GC11219 (R)-(+)-Tolterodine (R)-(+)-Tolterodine(PNU-200583) is a potent muscarinic receptor antagonists that show selectivity for the urinary bladder over salivary glands in vivo. (R)-(+)-Tolterodine Chemical Structure
  5. GC71634 (R)-Oxybutynin hydrochloride (R)-Oxybutynin hydrochloride, a (R)-isomer of Oxybutynin hydrochloride, is an orally active muscarinic receptor antagonist. (R)-Oxybutynin hydrochloride Chemical Structure
  6. GC63452 (Rac)-5-Hydroxymethyl Tolterodine (Rac)-5-Hydroxymethyl Tolterodine ((Rac)-Desfesoterodine), an active metabolite of Tolterodine, is a mAChR antagonist (Ki values of 2.3 nM, 2 nM, 2.5 nM, 2.8 nM, and 2.9 nM for M1, M2, M3, M4, and M5 receptors, respectively). (Rac)-5-Hydroxymethyl Tolterodine Chemical Structure
  7. GC71582 (Rac)-5-Hydroxymethyl Tolterodine hydrochloride (Rac)-5-Hydroxymethyl Tolterodine ((Rac)-Desfesoterodine) hydrochloride, an active metabolite of Tolterodine, is a mAChR antagonist (Ki values of 2.3 nM, 2 nM, 2.5 nM, 2.8 nM, and 2.9 nM for M1, M2, M3, M4, and M5 receptors, respectively). (Rac)-5-Hydroxymethyl Tolterodine hydrochloride Chemical Structure
  8. GC30859 AC260584 AC260584 is an M1 muscarinic receptor allosteric agonist with a pEC50 of 7.6. AC260584 Chemical Structure
  9. GC64332 Aceclidine Aceclidine is a modulator of M3 muscarinic acetylcholine receptor. Aceclidine Chemical Structure
  10. GC14096 Aclidinium Bromide

    LAS 34273, LAS-W 330

     LAMAs antagonist Aclidinium Bromide Chemical Structure
  11. GC10219 AF-DX 116 AF-DX 116 (AF-DX 116) is a selective and competitive M2 muscarinic acetylcholine receptor antagonist, with IC50 values of 640 nM and 386 nM for rabbit peripheral lung and rat heart, respectively. AF-DX 116 Chemical Structure
  12. GC30996 Alvameline (Lu 25-109)

    Lu 25-109

     Alvameline (Lu 25-109) (Lu25-109) is a partial M1 agonist and M2/M3 antagonist. Alvameline (Lu 25-109) Chemical Structure
  13. GC31815 Ambutonium bromide (BL700)

    BL700

     Ambutonium bromide (BL700) is an acetylcholine antagonist. Ambutonium bromide (BL700) Chemical Structure
  14. GC60049 Anisodamine hydrobromide Anisodamine hydrobromide (6-Hydroxyhyoscyamine hydrobromide), a belladonna alkaloid, is a non-subtype-selective muscarinic and a nicotinic cholinoceptor antagonist. Anisodamine hydrobromide Chemical Structure
  15. GC35381 Arborine Arborine inhibits the peripheral action of acetylcholine and induces a fall in blood pressure. Arborine Chemical Structure
  16. GC10264 Arecoline hydrobromide muscarinic acetylcholine receptor agonist Arecoline hydrobromide Chemical Structure
  17. GC16526 Atropine

    Tropine

     MAChRs antagonist Atropine Chemical Structure
  18. GC35427 Atropine methyl bromide

    NSC 61810

     A muscarinic acetylcholine receptor antagonist Atropine methyl bromide Chemical Structure
  19. GC35428 Atropine sulfate Atropine (Tropine tropate) sulfate is a competitive muscarinic acetylcholine receptor (mAChR) antagonist with IC50 values of 0.39 and 0.71 nM for Human mAChR M4 and Chicken mAChR M4, respectively. Atropine sulfate Chemical Structure
  20. GC63827 Atropine sulfate monohydrate Atropine (Tropine tropate) sulfate monohydrate is a broad-spectrum and competitive muscarinic acetylcholine receptor (mAChR) antagonist with anti-myopia effect. Atropine sulfate monohydrate Chemical Structure
  21. GC31690 Batefenterol (GSK961081)

    GSK961081, TD-5959

     Batefenterol (GSK961081) (GSK961081;TD-5959) is a novel muscarinic receptor antagonist and β2-adrenoceptor agonist; displays high affinity for hM2, hM3 muscarinic and hβ2-adrenoceptor with Ki values of 1.4, 1.3 and 3.7 nM, respectively. Batefenterol (GSK961081) Chemical Structure
  22. GC35492 Benzamide Derivative 1 Benzamide Derivative 1 is a benzamide derivative from patent EP0213775A1, compound 18. Benzamide Derivative 1 Chemical Structure
  23. GC30925 Benzetimide hydrochloride (R4929)

    Dioxatrine, R 4929, Spasmentral

     Benzetimide hydrochloride (R4929) is a muscarinic acetylcholine receptor antagonist. Benzetimide hydrochloride (R4929) Chemical Structure
  24. GC16791 Benztropine mesylate

    NSC 169913

     Dopamine transporter (DAT) inhibitor Benztropine mesylate Chemical Structure
  25. GC31942 Beperidium iodide (SX 810) Beperidium iodide (SX 810) shows a competitive antagonistic effect against acetylcholine receptor with a pA2 of 7.93. Beperidium iodide (SX 810) Chemical Structure
  26. GC14419 Bethanechol chloride

    (±)-Bethanechol, Carbamyl-β-methylcholine chloride, NSC 30783

     Muscarinic receptor agonist Bethanechol chloride Chemical Structure
  27. GC35524 Biperiden Biperiden (KL 373) is a non-selective muscarinic receptor antagonist that competitively binds to M1 muscarinic receptors, thereby inhibiting acetylcholine and enhancing dopamine signaling in the central nervous system. Biperiden Chemical Structure
  28. GC10621 Biperiden HCl

    NSC 84989, NSC 170950

     Biperiden (KL 373) hydrochloride is a non-selective muscarinic receptor antagonist that competitively binds to M1 muscarinic receptors, thereby inhibiting acetylcholine and enhancing dopamine signaling in the central nervous system. Biperiden HCl Chemical Structure
  29. GC15758 BQCA positive allosteric modulator of the M1 muscarinic acetylcholine receptor (mAChR) BQCA Chemical Structure
  30. GC32039 BTM-1086 BTM-1086 is a potent anti-ulcer and gastric secretory inhibiting agent. BTM-1086 Chemical Structure
  31. GC31072 Camylofine

    Camylofin is an antimuscarinic, is a smooth muscle relaxant

     Camylofine Chemical Structure
  32. GC16937 Carbamoylcholine chloride

    Carbachol

    Cholinergic receptor agonist

     Carbamoylcholine chloride Chemical Structure
  33. GC31255 CDD0102 (CDD0102A)

    CDD0102A

     CDD0102 (CDD0102A) is a potent M1 Muscarinic receptor agonist. CDD0102 (CDD0102A) Chemical Structure
  34. GC14215 Cevimeline A muscarinic receptor agonist Cevimeline Chemical Structure
  35. GC43232 Cevimeline (hydrochloride)

    AF 102B, SNI 2011, SNK 508

     Cevimeline is a muscarinic receptor agonist (EC50s = 23, 48, and 63 nM for M1, M3, and M5, respectively, and >1 μM for M2 and M4). Cevimeline (hydrochloride) Chemical Structure
  36. GC17157 Cevimeline hydrochloride hemihydrate Cevimeline hydrochloride hemihydrate Chemical Structure
  37. GC38693 Choline bitartrate Choline bitartrate is a vitamin-like essential nutrient, can affect diseases such as liver disease, atherosclerosis and neurological disorders. Choline bitartrate Chemical Structure
  38. GC30955 Cimetropium Bromide (DA-3177) Cimetropium Bromide (DA-3177) (DA-3177) is a mAChR antagonist for long-term treatment of irritable bowel syndrome. Cimetropium Bromide (DA-3177) Chemical Structure
  39. GC31048 Clidinium bromide (Ro 2-3773)

    Ro 2-3773

     Clidinium bromide (Ro 2-3773) is a quaternary amine antimuscarinic agent. Clidinium bromide (Ro 2-3773) Chemical Structure
  40. GC17760 Clozapine

    HF 1854

     Clozapine (HF 1854) is an antipsychotic used for the research of schizophrenia. Clozapine Chemical Structure
  41. GC50193 Clozapine - d8

    HF 1854-d8

     Clozapine - d8 (HF 1854-d8) is the deuterium labeled Clozapine. Clozapine - d8 Chemical Structure
  42. GC10822 Clozapine N-oxide (CNO)

    CNO

     Clozapine N-oxide(CNO) is a potent dopamine antagonist and also a potent and selective muscarinic M4 receptor (EC50=11 nM) agonist. Clozapine N-oxide (CNO) Chemical Structure
  43. GC31209 Cyclodrine hydrochloride Cyclodrine hydrochloride is a cholinergic (muscarinic, nicotinic) (mAChR and nAChR) receptor antagonist. Cyclodrine hydrochloride Chemical Structure
  44. GC43347 Cyclopentolate (hydrochloride)

    (±)-Cyclopentolate

     Cyclopentolate is an antagonist of muscarinic acetylcholine receptors (Kis = 1.62, 27.5, and 2.63 nM for M1, M2, and M3 receptors, respectively). Cyclopentolate (hydrochloride) Chemical Structure
  45. GC72907 Cycrimine Cycrimine is an orally active muscarinic cholinergic receptor (mAChR) M1 antagonist, reduces the acetylcholine levels in parkinson model. Cycrimine Chemical Structure
  46. GC31136 Darenzepine Darenzepine is a muscarinic receptor inhibitor extracted from patent US 20170095465 A1. Darenzepine Chemical Structure
  47. GC35810 Darifenacin Darifenacin(UK88525) is a selective M3 muscarinic receptor antagonist with pKi of 8.9. Darifenacin Chemical Structure
  48. GC15772 Darifenacin HBr

    UK 88525-04

     Darifenacin HBr (UK-88525 hydrobromide) is a selective M3 muscarinic receptor antagonist with pKi of 8.9. Darifenacin HBr Chemical Structure
  49. GC60758 Deschloroclozapine Deschloroclozapine, a metabolite of Clozapine, is a highly potent muscarinic DREADDs agonist. Deschloroclozapine Chemical Structure
  50. GC74124 Deschloroclozapine dihydrochloride Deschloroclozapine didrochloride, a metabolite of Clozapine, is a highly potent muscarinic DREADDs agonist. Deschloroclozapine dihydrochloride Chemical Structure
  51. GC35842 Desfesoterodine Desfesoterodine (PNU-200577) is a potent and selective muscarinic receptor (mAChR) antagonist with a KB and a pA2 of 0.84 nM and 9.14, respectively. Desfesoterodine Chemical Structure
  52. GC35845 Dexetimide Dexetimide ((+)-Benzetimide; (S)-(+)-Dexetimide; Dexbenzetimide) is a piperidine anticholinergic and a high-affinity muscarinic receptor antagonist. Dexetimide Chemical Structure
  53. GC16635 Diphemanil Methylsulfate

    NSC 41725

     Diphemanil methylsulfate is a quaternary ammonium anticholinergic. Diphemanil Methylsulfate Chemical Structure
  54. GC10300 Diphenidol HCl

    SKF 478A

     Diphenidol HCl (Difenidol hydrochloride) is a non-selective muscarinic M1-M4 receptor antagonist, has anti-arrhythmic activity. Diphenidol HCl Chemical Structure
  55. GC30849 DREADD agonist 21 A muscarinic hM3Dq DREADD agonist DREADD agonist 21 Chemical Structure
  56. GC50446 DREADD agonist 21 dihydrochloride Potent muscarinic DREADD agonist; water soluble version of DREADD agonist 21 DREADD agonist 21 dihydrochloride Chemical Structure
  57. GC16073 Dronedarone An antiarrhythmic agent Dronedarone Chemical Structure
  58. GC30409 Elucaine Elucaine is a muscarinic acetylcholine receptor antagonist with anti-ulcerative activity. Elucaine Chemical Structure
  59. GC63484 Emraclidine

    CVL-231

    Emraclidine (CVL-231) is a muscarinic M4 receptor positive allosteric modulator (WO2018002760, compound 11).

     Emraclidine Chemical Structure
  60. GC31017 ENS-163 phosphate (ENS 213-163)

    ENS 213-163; Sandoz ENS 163 phosphate; Thiopilocarpine phosphate

     ENS-163 phosphate (ENS 213-163) is a selective muscarinic M1 receptor agonist. ENS-163 phosphate (ENS 213-163) Chemical Structure
  61. GC39379 Fesoterodine Fesoterodine is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pKi values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. Fesoterodine Chemical Structure
  62. GC16087 Fesoterodine Fumarate

    SMP 8272, SPM 907

     Muscarinic AChR receptor antagonist Fesoterodine Fumarate Chemical Structure
  63. GC39380 Fesoterodine L-mandelate Fesoterodine L-mandelate is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pKi values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. Fesoterodine L-mandelate Chemical Structure
  64. GC13361 Flavoxate hydrochloride

    NSC 114649, Rec 7/0040

     muscarinic AChR antagonist Flavoxate hydrochloride Chemical Structure
  65. GC11385 G-Protein antagonist peptide Inhibits G protein activation by GPCRs G-Protein antagonist peptide Chemical Structure
  66. GC63766 G-Protein antagonist peptide TFA G-Protein antagonist peptide TFA is a truncated substance P-related peptide, competes with receptor for G protein binding. G-Protein antagonist peptide TFA Chemical Structure
  67. GC10972 Gallamine Triethiodide Cholinergic receptor blocker Gallamine Triethiodide Chemical Structure
  68. GC15029 Glycopyrrolate

    AHR 504, NSC 250836, NSC 251251, NSC 251252

     Muscarinic competitive antagonist Glycopyrrolate Chemical Structure
  69. GC65379 Guvacoline hydrochloride Guvacoline hydrochloride, a pyridine alkaloid found in Areca triandra, can act as a weak full agonist of atrial and ileal muscarinic receptors. Guvacoline hydrochloride Chemical Structure
  70. GC13897 Homatropine Bromide

    (±)-Homatropine

     Muscarinic AChR antagonist Homatropine Bromide Chemical Structure
  71. GC17908 Homatropine Methylbromide

    NSC 34399

     Muscarinic AChR antagonist Homatropine Methylbromide Chemical Structure
  72. GC11035 Hyoscyamine

    L-Hyoscyamine, (S)-Hyoscyamine

     Hyoscyamine (Daturine), a natural plant tropane alkaloid, is a potent and competitive muscarinic receptor (MR) antagonist. Hyoscyamine Chemical Structure
  73. GC30812 Imidafenacin (KRP-197) Imidafenacin (KRP-197)(KRP-197; ONO-8025) is a potent and selective inhibitor of M3 receptors with Kb of 0.317 nM; less potent for M2 receptors(IC50=4.13 nM). Imidafenacin (KRP-197) Chemical Structure
  74. GC12717 Ipratropium Bromide AChR antagonist Ipratropium Bromide Chemical Structure
  75. GC68326 Ipratropium-d3 bromide

    Sch 1000-d3

     Ipratropium-d3 bromide Chemical Structure
  76. GC13191 Irsogladine PDE4 inhibitor Irsogladine Chemical Structure
  77. GC33878 Irsogladine maleate (Dicloguamine maleate) Irsogladine is a PDE4 inhibitor and muscarinic acetylcholine receptor binder. Irsogladine maleate (Dicloguamine maleate) Chemical Structure
  78. GC39076 Isopteropodine Isopteropodine is heteroyohimbine-type oxindole alkaloid components of Uncaria tomentosa (Willd. Isopteropodine Chemical Structure
  79. GC50681 JHU 37152 JHU 37152 is a potent and brain-penetrant DREADD agonist, with EC50s of 5nM and 0.5nM for hM3Dq and hM4Di DREADDs in HEK-293 cells, respectively. JHU 37152 Chemical Structure
  80. GC50682 JHU 37160 JHU 37160 is a potent and brain-penetrant DREADD agonist, with EC50s of 18.5nM and 0.2nM for hM3Dq and hM4Di DREADDs in HEK-293 cells, respectively. JHU 37160 Chemical Structure
  81. GC39130 L-Hyoscyamine sulfate L-Hyoscyamine sulfate (Daturine sulfate), a natural plant tropane alkaloid, is a potent and competitive muscarinic receptor (MR) antagonist. L-Hyoscyamine sulfate Chemical Structure
  82. GC65504 L-Hyoscyamine-d3

    Daturine-d3

     L-Hyoscyamine-d3 Chemical Structure
  83. GC36442 Levetimide Levetimide is a potent and stereoselective inhibitor of [3H](+)pentazocine binding, with a Ki of 2.2 nM. Levetimide Chemical Structure
  84. GC17779 Levetiracetam

    UCBL 059

     Antiepileptic drug Levetiracetam Chemical Structure
  85. GC13445 LY2119620 positive allosteric modulator of M2/M4 receptor LY2119620 Chemical Structure
  86. GC31984 M3 receptor antagonist 1 M3 receptor antagonist 1 is a selective, long-acting and competitive muscarinic M3 receptor antagonist. M3 receptor antagonist 1 Chemical Structure
  87. GC65567 M4 mAChR agonist-1 M4 mAChR agonist-1 (compound 10a) is a potent M4 mAChR agonist with an EC50 >10 μM for human M4. M4 mAChR agonist-1 Chemical Structure
  88. GC71334 mAChR antagonist 1 mAChR antagonist 1 (compound 4a) is a mAChR antagonist with Ki values of 255 nM, 121 nM, 158 nM, and 255 nM for M1, M3, M4, and M5 subtype, respectively. mAChR antagonist 1 Chemical Structure
  89. GC36523 mAChR-IN-1 mAChR-IN-1 is a potent muscarinic cholinergic receptor (mAChR) antagonist, with an IC50 of 17 nM. mAChR-IN-1 Chemical Structure
  90. GC36524 mAChR-IN-1 hydrochloride mAChR-IN-1 hydrochloride is a potent muscarinic cholinergic receptor (mAChR) antagonist, with an IC50 of 17 nM. mAChR-IN-1 hydrochloride Chemical Structure
  91. GC67620 Methacholine bromide

    Acetyl-β-methylcholine bromide

     Methacholine (Acetyl-β-methylcholine) bromide is a potent muscarinic-3 (M3) agonist. Methacholine bromide acts directly on acetylcholine receptors on smooth muscle causing bronchoconstriction and airway narrowing. Methacholine bromide shows a high sensitivity to identify bronchial hyperresponsiveness (BHR). Methacholine bromide can be used to measure airway hyperresponsiveness (AHR) as a diagnostic aid in the assessment of individuals with asthma-like symptoms and normal resting expiratory flow rates. Methacholine bromide Chemical Structure
  92. GC33434 Methacholine chloride

    Methacholine

     Methacholine (Acetyl-β-methylcholine) choride is a potent muscarinic-3 (M3) agonist. Methacholine chloride Chemical Structure
  93. GC17825 Methscopolamine

    NSC 61809, NSC 120606, U-5036

     Muscarinic acetylcholine receptor blocker Methscopolamine Chemical Structure
  94. GC31946 Methylbenactyzium Bromide Methylbenactyzium Bromide is a muscarinic acetylcholine receptor (mAChR) inhibitor. Methylbenactyzium Bromide Chemical Structure
  95. GC30968 Metixene hydrochloride hydrate Metixene (Piperidine) hydrochloride hydrate is an anticholinergic and antiparkinsonian agent. Metixene hydrochloride hydrate Chemical Structure
  96. GC30446 MHP 133 MHP 133 is a drug with multiple CNS targets, and inhibits acetylcholinesterase (AChE) with Ki of 69 μM; also active against muscarinic M1 and M2 receptors, serotonin 5HT4 receptors, and imidazole I2 receptors. MHP 133 Chemical Structure
  97. GC67979 MK-6884 MK-6884 Chemical Structure
  98. GC30836 MK-7622 (M1 receptor modulator) MK-7622 (M1 receptor modulator) (M1 receptor modulator) is a muscarinic M1 receptor positive allosteric modulator. MK-7622 (M1 receptor modulator) Chemical Structure
  99. GC69476 ML375

    VU0483253

    ML375 (VU0483253) is an effective, highly selective, blood-brain barrier penetrant and orally active M5 mAChR negative allosteric modulator (NAM), with IC50 values of 300 nM and 790 nM for human and rat M5, respectively. ML375 has no activity on human and rat M1-M4.

     ML375 Chemical Structure
  100. GC61802 ML380 ML380 is a potent, subtype-selective, and brain-penetrant positive allosteric modulator (PAM) of M5 mAChR, with EC50s of 190 and 610 nM for human and rat M5, respectively. ML380 Chemical Structure
  101. GC70225 ML381 ML381 (VU0488130) is a highly selective, central nervous system penetrant mAChR M5 orthogonal antagonist (IC50 = 450 nM; Ki = 340 nM). ML381 Chemical Structure

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