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M1 mAChR

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83

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13

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-B0298A
    Clemastine fumarate
    Maximum Cited Publications
    11 Publications Verification

    HS-592 fumarate; Meclastine fumarate

    Histamine Receptor Apoptosis mAChR Pyroptosis Keap1-Nrf2 p62 Autophagy mTOR IKK Neurological Disease Metabolic Disease
    Clemastine (HS-592; Meclastine) fumarate is an orally active, blood-brain barrier-permeable H1 histamine receptor (H1 histamine receptor) antagonist with potent antiallergic effects. Clemastine fumarate also antagonizes muscarinic acetylcholine receptors (mAChR), particularly the M1 and M4 subtypes. In addition to antihistamine effects, Clemastine fumarate exhibits multiple pharmacological activities, especially in promoting central nervous system remyelination, activating autophagy and pyroptosis, exerting anti-apoptotic and neuroprotective effects, and suppressing inflammation .
    Clemastine fumarate
  • HY-12100
    Umeclidinium bromide
    1 Publications Verification

    GSK573719A

    mAChR Inflammation/Immunology Cancer
    Umeclidinium bromide is a novel mAChR antagonist. The affinity (Ki) of Umeclidinium bromide for the cloned human M1-M5 mAChRs ranges from 0.05 to 0.16 nM.
    Umeclidinium bromide
  • HY-B0406A
    Bethanechol chloride
    2 Publications Verification

    Carbamyl-β-methylcholine chloride

    mAChR Neurological Disease Cancer
    Bethanechol chloride (Carbamyl-β-methylcholine chloride), a parasympathomimetic agent, is a mAChR agonist that exerts its effects via directly stimulating the mAChR (M1, M2, M3, M4, and M5) of the parasympathetic nervous system .
    Bethanechol chloride
  • HY-B0461

    mAChR Neurological Disease
    Trospium chloride is an orally active, specific and competitive antagonist of muscarinic cholinergic receptors (mAChRs), with antimuscarinic activity. Trospium chloride binds to muscarinic receptors M1, M2 and M3 with high affinity, but not nicotinic, cholinergic receptors .
    Trospium chloride
  • HY-A0030

    mAChR Neurological Disease Metabolic Disease Cancer
    Fesoterodine Fumarate 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 Fumarate is used for the overactive bladder (OAB) .
    Fesoterodine fumarate
  • HY-17037
    Pirenzepine dihydrochloride
    5 Publications Verification

    LS 519; Pirenzepin dihydrochloride; Gastrozepin dihydrochloride

    mAChR Metabolic Disease Cancer
    Pirenzepine (LS 519) dihydrochloride is a selective M1 mAChR (muscarinic acetylcholine receptor) antagonist, with poor penetration of the blood-brain barrier. Pirenzepine dihydrochloride reduces gastric acid secretion and reduces muscle spasm, can be used in peptic ulcers research. Pirenzepine dihydrochloride shows anti-proliferative activity to cancer cells .
    Pirenzepine dihydrochloride
  • HY-B0298
    Clemastine
    Maximum Cited Publications
    11 Publications Verification

    HS-592; Meclastine

    Histamine Receptor mAChR Autophagy Apoptosis Keap1-Nrf2 p62 mTOR Pyroptosis IKK Cardiovascular Disease Neurological Disease Inflammation/Immunology
    Clemastine (HS-592; Meclastine) is an orally active, blood-brain barrier-permeable H1 histamine receptor (H1 histamine receptor) antagonist with potent antiallergic effects. Clemastine also antagonizes muscarinic acetylcholine receptors (mAChR), particularly the M1 and M4 subtypes. In addition to antihistamine effects, Clemastine exhibits multiple pharmacological activities, especially in promoting central nervous system remyelination, activating autophagy and pyroptosis, exerting anti-apoptotic and neuroprotective effects, and suppressing inflammation .
    Clemastine
  • HY-108234
    VU 0255035
    1 Publications Verification

    VU 255035

    mAChR Neurological Disease
    VU0255035 is a highly selective and competitive M1 mAChR antagonist. VU0255035 blocks M1 mAChR signals to reduce epileptic seizures and regulate neuronal membrane potential. VU0255035 can be used in research related to central nervous system diseases, such as epilepsy, Parkinson's disease, and dystonia .
    VU 0255035
  • HY-17037A
    Pirenzepine
    5 Publications Verification

    LS 519 free base; Pirenzepin; Gastrozepin

    mAChR Metabolic Disease Cancer
    Pirenzepine (LS 519 free base) is a selective M1 mAChR (muscarinic acetylcholine receptor) antagonist, with poor penetration of the blood-brain barrier. Pirenzepine reduces gastric acid secretion and reduces muscle spasm, can be used in peptic ulcers research. Pirenzepine shows anti-proliferative activity to cancer cells .
    Pirenzepine
  • HY-101858

    mAChR Neurological Disease
    BQCA a highly selective allosteric modulator of the M1 mAChR.
    BQCA
  • HY-15618

    M1 receptor modulator

    mAChR Calcium Channel Neurological Disease
    MK-7622 (M1 receptor modulator) is an orally active positive allosteric modulator of muscarinic M1 acetylcholine receptors (mAChRs). MK-7622 enhances ACh-induced calcium flux in CHO cells expressing human M1 receptors (EC50 = 21 nM) and shows robust agonist activity in rat M1-expressing CHO cells, increasing intracellular calcium. MK-7622 reverses Scopolamine (HY-N0296)-induced cognitive deficits in rhesus macaques in an object retrieval detour task. MK-7622 can be used for the study of Alzheimer's disease (AD) .
    MK-7622
  • HY-122743
    Iperoxo
    2 Publications Verification

    mAChR Neurological Disease
    Iperoxo is a potent superagonist of muscarinic acetylcholine receptor (mAChR) that activates M1, M2 and M3 receptors with pEC50 of 9.87, 10.1 and 9.78. Iperoxo can be used for direct probing activation-related conformational transitions of muscarinic receptors when labeled with tritium .
    Iperoxo
  • HY-70053

    mAChR Neurological Disease Metabolic Disease
    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 is used for the overactive bladder (OAB) .
    Fesoterodine
  • HY-107111

    mAChR Neurological Disease
    GSK1034702 is an orally active and allosteric agonist of M1 mAChR (pEC50=8.1) that can cross the blood-brain barrier. GSK1034702 activates the Gq/11 protein-mediated signaling pathway, enhancing neuronal firing and long-term potentiation (LTP) in the CA1 region of the hippocampus. GSK1034702 can modulate hippocampal function, improve memory encoding in the nicotine withdrawal cognitive dysfunction model, and show pro-cognitive effects in rodents. GSK1034702 can be used for the study of the mechanisms of cognitive impairment diseases such as Alzheimer's disease, and has certain peripheral M receptor activation-related side effects (such as gastrointestinal reactions) .
    GSK1034702
  • HY-107651
    VU 0365114
    1 Publications Verification

    mAChR Metabolic Disease
    VU 0365114 is a selective mAChR M5 positive allosteric modulator, with an EC50 of 2.7 μM, and >30 μM for M1, M2, M3 and M4 receptors. VU 0365114 increases insulin secretion stimulated by ACh in human β-cells .
    VU 0365114
  • HY-B0662

    KRP-197; ONO-8025

    mAChR Vasopressin Receptor Neurological Disease Endocrinology
    Imidafenacin (KRP-197; ONO-8025) is an orally active inhibitor of muscarinic (mAChR) M1 and M3 receptors. Imidafenacin potently inhibits bladder contraction in vivo and exerts an antidiuretic effect by enhancing the signaling pathway of vasopressin (antidiuretic hormone). Imidafenacin can be used in research related to overactive bladder .
    Imidafenacin
  • HY-177498

    mAChR Neurological Disease
    M1 mAChR modulator-1 (Example 66) is a muscarinic M1 receptor (mAChR1) positive allosteric modulator. M1 mAChR modulator-1 effectively promotes gastrointestinal motility and defecation in mouse models with low central permeability. M1 mAChR modulator-1 can be used for constipation research .
    M1 mAChR modulator-1
  • HY-12439
    ML380
    1 Publications Verification

    mAChR Neurological Disease
    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 exhibits moderate selectivity versus the M1 and M3 mAChR subtypes. ML380 could increase the affinity of ACh for the M5 mAChR .
    ML380
  • HY-12567

    VU0483253

    mAChR Neurological Disease
    ML375 (VU0483253) is a potent, highly selective, brain-penetrant and orally active M5 mAChR negative allosteric modulator (NAM) with IC50s of 300 nM and 790 nM for human and rat M5, respectively. ML375 is inactive at human and rat M1-M4 .
    ML375
  • HY-14562

    mAChR Amyloid-β Neurological Disease Inflammation/Immunology
    TBPB (tert-butyl peroxybenzoate) is a highly selective, blood-brain-permeable M1 mAChR allosteric agonist (EC50=289 nM) with anti-schizophrenia and anti-inflammatory activities. TBPB can enhance the sensitivity of M1 receptors to acetylcholine, activate downstream signaling pathways, and inhibit the release of pro-inflammatory cytokines (TNF-α, IL-6). TBPB can regulate the processing of amyloid and can be used in the study of neurodegenerative diseases (such as Alzheimer's disease) and inflammation-related diseases (such as sepsis) .
    TBPB
  • HY-114933
    VU0119498
    1 Publications Verification

    mAChR Neurological Disease Metabolic Disease
    VU0119498 is a pan Gq mAChR M1, M3, M5 positive allosteric modulator (PAM), with EC50s of 6.04, 6.38, and 4.08 µM, respectively. VU0119498 has antidiabetic activity .
    VU0119498
  • HY-B0461R

    mAChR Reference Standards Neurological Disease
    Trospium (chloride) (Standard) is the analytical standard of Trospium (chloride). This product is intended for research and analytical applications. Trospium chloride is an orally active, specific and competitive antagonist of muscarinic cholinergic receptors (mAChRs), with antimuscarinic activity. Trospium chloride binds to muscarinic receptors M1, M2 and M3 with high affinity, but not nicotinic, cholinergic receptors .
    Trospium chloride (Standard)
  • HY-76570

    (Rac)-Desfesoterodine; (Rac)-PNU-200577

    mAChR Neurological Disease
    (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 can be used for overactive bladder research .
    (Rac)-5-Hydroxymethyl Tolterodine
  • HY-B0406

    Carbamyl-β-methylcholine

    mAChR Neurological Disease Cancer
    Bethanechol (Carbamyl-β-methylcholine), a parasympathomimetic agent, is a mAChR agonist that exerts its effects via directly stimulating the mAChR (M1, M2, M3, M4, and M5) of the parasympathetic nervous system .
    Bethanechol
  • HY-B0461S

    Isotope-Labeled Compounds mAChR Neurological Disease
    Trospium-d8 (chloride) is the deuterium labeled Trospium chloride. Trospium chloride is an orally active, specific and competitive antagonist of muscarinic cholinergic receptors (mAChRs), with antimuscarinic activity. Trospium chloride binds to muscarinic receptors M1, M2 and M3 with high affinity, but not nicotinic, cholinergic receptors .
    Trospium-d8 chloride
  • HY-70053A

    mAChR Neurological Disease Metabolic Disease Cancer
    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 is used for the overactive bladder (OAB) .
    Fesoterodine L-mandelate
  • HY-119918

    mAChR Neurological Disease
    Cycrimine is an orally active muscarinic cholinergic receptor (mAChR) M1 antagonist, reduces the acetylcholine levels in parkinson model. Cycrimine shows antispasmodic activity, can be used in studies of behavioral and mental disorder .
    Cycrimine
  • HY-A0030S

    mAChR Metabolic Disease
    Fesoterodine-d7 (fumarate) is the deuterium labeled Fesoterodine fumarate . Fesoterodine Fumarate 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 Fumarate is used for the overactive bladder (OAB) .
    Fesoterodine-d7 fumarate
  • HY-W037331

    Bis(4-fluorophenyl)methanol

    mAChR Others
    4,4-Difluorobenzhydrol is a precursor of a mAChR antagonist, and its derivative 4,4-Difluorobenzhydrol Carbamate can selectively target the M1 subtype .
    4,4-Difluorobenzhydrol
  • HY-65036

    4-Bromo-2-pyridone

    Biochemical Assay Reagents Drug Intermediate Neurological Disease
    4-Bromo-2-hydroxypyridine is an intermediate. 4-Bromo-2-hydroxypyridine can be used to synthesize M1 muscarinic acetylcholine receptor (M1 mAChR) positive allosteric modulators. 4-Bromo-2-hydroxypyridine can be used in the research of Alzheimer's disease and schizophrenia .
    4-Bromo-2-hydroxypyridine
  • HY-118356

    Neurokinin Receptor mAChR Neurological Disease
    WIN 62,577 is a rat-specific, but non-human, NK1 receptor antagonist. WIN 62,577 interacts with M1-M4 mAChRs and is an allosteric enhancer of acetylcholine affinity targeting the M3 receptor.
    WIN 62,577
  • HY-B0406AS

    Carbamyl-β-methylcholine-d6 chloride

    Isotope-Labeled Compounds mAChR Neurological Disease
    Bethanechol-d6 (chloride) is the deuterium labeled Bethanechol chloride. Bethanechol chloride (Carbamyl-β-methylcholine chloride), a parasympathomimetic agent, is a mAChR agonist that exerts its effects via directly stimulating the mAChR (M1, M2, M3, M4, and M5) of the parasympathetic nervous system .
    Bethanechol-d6 chloride
  • HY-108171A

    mAChR Inflammation/Immunology
    Hexocyclium methylsulfate is a potent mAChR antagonist with pKi values of 8.9, 7.7, 8.4, 8.8 for M1, M2, M3, and M4 subtype, respectively. Hexocyclium methylsulfate has the potential for the research of duodenal ulcer and irritable bowel syndrome .
    Hexocyclium methylsulfate
  • HY-159578S

    mAChR Neurological Disease
    VU6036864 (compound 45) is an orally active, selective mAChR M5 antagonist with IC50=20 nM for human M5. VU6036864 is >500-fold selective for human M1-4, with BBB characteristic and high oral bioavailability (%F>100%) .
    VU6036864
  • HY-12158

    mAChR Neurological Disease
    VU0238441 is a pan muscarinic acetylcholine receptor (mAChR) positive allosteric modulator (PAM) with EC50s of 3.2 μM, 2.8 μM, 2.2 μM, 2.1 μM, >10 μM for M1, M2, M3, M5 and M4, respectively .
    VU0238441
  • HY-101679A

    mAChR Neurological Disease
    YM-58790 free base is a potent antagonist of mAChR. YM-58790 free base binds M1, M2, M3 with Ki values of 28 nM, 260 nM, and 15 nM. YM-58790 free base exhibits potent inhibitory activity on bladder pressuer in reflexly-evoked rhythmic contraction in rats .
    YM-58790 free base
  • HY-116569

    mAChR Cardiovascular Disease
    VU0455691 is a potent, selective orthosteric M1 mAChR antagonist (pIC50=6.64; IC50=0.23 µM for hM1) .
    VU0455691
  • HY-175532

    mAChR Neurological Disease
    M4 mAChR Modulator-2 is an orally active, selective, brain-penetrant positive allosteric modulator (PAM) of the M4 muscarinic acetylcholine receptor (M4 mAChR) (EC50 = 513 nM). M4 mAChR Modulator-2 exhibits high target selectivity, showing negligible affinity and low inhibition rates for non-target receptors (D1R/D2R/D3R, 5-HT subtypes, κ/δ/μ opioid receptors, H1, M1/M2) while specifically binding to M4 mAChR with a Ki of 377 nM and an inhibition rate of 62.8%. M4 mAChR Modulator-2 reverses Dizocilpine (MK-801) (HY-15084B)-induced hyperlocomotion in mice. M4 mAChR Modulator-2 can be used for the study of schizophrenia
    M4 mAChR Modulator-2
  • HY-120576

    VU0405652

    mAChR Neurological Disease
    ML169 (VU0405652) is a potent, selective and brain penetrant positive allosteric modulator (PAM) of M1 mAChR, with an EC50 of 1.38 µM. ML169 is a MLPCN probe and can be used for Alzheimer’s disease .
    ML169
  • HY-148961

    mAChR Neurological Disease
    HTL-9936 is a selective M1 muscarinic acetylcholine receptor (M1-mAChR) agonist. HTL-9936 is promising for research of neurodegenerative disorders (e.g., Alzheimer’s) .
    HTL-9936
  • HY-149732

    mAChR Neurological Disease
    M1/M4 muscarinic agonist 3 (compound 44) is a muscarinic mAChR M1/M4 agonist with EC50s of 31 nM and 9.3 nM, respectively .
    M1/M4 muscarinic agonist 3
  • HY-149731

    mAChR Neurological Disease
    M1/M2/M4 muscarinic agonist 2 (compound 43) is a muscarinic mAChR M1/M2/M4 agonist with EC50s of 30 nM, 200 nM and 6.2 nM, respectively .
    M1/M2/M4 muscarinic agonist 2
  • HY-155367

    mAChR Neurological Disease
    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
  • HY-149733

    mAChR Neurological Disease
    M1/M2/M4 muscarinic agonist 3 (compound 45) is a muscarinic mAChR M1/M2/M4 agonist with EC50s of 3.2 nM, 32 nM and 1.7 nM, respectively .
    M1/M2/M4 muscarinic agonist 3
  • HY-B1789

    mAChR Neurological Disease
    Telenzepine is an antimuscarinic agent with Kis of 0.94 nM (M1 mAChR) and 17.8 nM (M2 mAChR) binding to muscarinic receptors. Telenzepine effectively blocks synaptic transmission promoted by muscarinic or M1 receptor agonists. Thus, Telenzepine can reduce the amplitude of extracellular slow excitatory postsynaptic potentials (EC50=38 nM) and slow inhibitory postsynaptic potentials (EC50=253 nM) .
    Telenzepine
  • HY-12100S1

    GSK573719A-d10

    mAChR Inflammation/Immunology
    Umeclidinium-d10 (bromide) is the deuterium labeled Umeclidinium bromide. Umeclidinium bromide is a novel mAChR antagonist. The affinity (Ki) of Umeclidinium bromide for the cloned human M1-M5 mAChRs ranges from 0.05 to 0.16 nM.
    Umeclidinium-d10 bromide
  • HY-12100S

    GSK573719A-d5

    Isotope-Labeled Compounds mAChR Inflammation/Immunology
    Umeclidinium-d5 (bromide) is the deuterium labeled Umeclidinium bromide. Umeclidinium bromide is a novel mAChR antagonist. The affinity (Ki) of Umeclidinium bromide for the cloned human M1-M5 mAChRs ranges from 0.05 to 0.16 nM.
    Umeclidinium-d5 bromide
  • HY-16489A

    mAChR Calcium Channel Neurological Disease
    Terodiline hydrochloride is an M1-selective muscarinic receptor (mAChR) antagonist with Kbs of 15, 160, 280, and 198 nM in rabbit vas deferens (M1), atria (M2), bladder (M3) and ileal muscle (M3), respectively. Terodiline hydrochloride also is a Ca 2+ blocker. Terodiline hydrochloride acts as a treatment for urinary frequency and urge incontinence .
    Terodiline hydrochloride
  • HY-170032

    mAChR Neurological Disease
    Oxotremorine is an agonist for mAChR, that activates M1 and M3 acetylcholine receptors. Oxotremorine exhibits nicotine-like effects in drug discrimination experiments in macaques .
    Oxotremorine
  • HY-U00104

    mAChR Endocrinology
    YM-46303 is an mAChR antagonist which exhibits the highest affinities for M1 and M3 receptors, and selectivity for M3 over M2 receptor.
    YM-46303

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