2. Signaling Pathways
  3. GPCR/G Protein
    Neuronal Signaling
  4. mAChR

mAChR

Muscarinic acetylcholine receptor

mAChR

Related Products

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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.

mAChR Isoform Specific Products:

mAChR Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-149733
    M1/M2/M4 muscarinic agonist 3
    		Agonist
    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-17360R
    Tiotropium Bromide (Standard)
    		Antagonist
    Tiotropium (Bromide) (Standard) is the analytical standard of Tiotropium (Bromide). This product is intended for research and analytical applications. 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.
    Tiotropium Bromide (Standard)
  • HY-14541S2
    Olanzapine-d8
    		Antagonist
    Olanzapine-d8 is a deuterated labeled Olanzapine. Olanzapine (LY170053) is a selective, orally active monoaminergic antagonist with high affinity binding to serotonin H1, 5HT2A/2C, 5HT3, 5HT6 (Ki=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (Ki=11 to 31 nM), muscarinic M1-5 (Ki=1.9-25 nM), and adrenergic α1 receptor (Ki=19 nM). Olanzapine is an atypical antipsychotic.
    Olanzapine-d<sub>8</sub>
  • HY-107111A
    GSK1034702 hydrochloride
    		Agonist
    GSK1034702 hydrochloride is an orally active and allosteric agonist of M1 mAChR (pEC50=8.1) that can cross the blood-brain barrier. GSK1034702 hydrochloride activates the Gq/11 protein-mediated signaling pathway, enhancing neuronal firing and long-term potentiation (LTP) in the CA1 region of the hippocampus. GSK1034702 hydrochloride can modulate hippocampal function, improve memory encoding in the nicotine withdrawal cognitive dysfunction model, and show pro-cognitive effects in rodents. GSK1034702 hydrochloride 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 hydrochloride
  • HY-113616
    VU0364572
    		Agonist
    VU0364572 is a selective allosteric agonist of the M1 muscarinic receptor with an EC50 of 0.11 μM. VU0364572 has neuroprotective potential for preventing memory impairments and reducing neuropathology in Alzheimer’s Disease. VU0364572 is orally active and is CNS penetrant.
    VU0364572
  • HY-B0781S1
    Promethazine-d3(hydrochloride)
    		Antagonist
    Promethazine-d3 (hydrochloride) is deuterium labeled Promethazine (hydrochloride). Promethazine hydrochloride is an orally active phenothiazine derivative with antihistaminic (H1), sedative, antiemetic, anticholinergic, and antimotion sickness properties. Promethazine hydrochloride is a potent H1 receptor antagonist and a mAChR antagonist. It also has a certain affinity for 5-HT2A and 5-HT2C receptors.
    Promethazine-d<sub>3</sub>(hydrochloride)
  • HY-107652
    AF-DX 384
    		Antagonist 98.0%
    AF-DX 384 is a selective antagonist of M2 and M4 muscarinic acetylcholine receptors (Kis=6.03 and 10 nM, respectively). AF-DX 384 reverses deficits in novel object recognition and passive avoidance in aged rats, as well as in young rats with impairments induced by scopolamine.
    AF-DX 384
  • HY-151801
    DIBA-Cy5
    DIBA-Cy5 is a fluorescent DIBA antagonist made up be DIBA-alkyne binding Cyanine5 fluorophores (Cy5) and polyethylene glycol (PEG) biomolecules. DIBA-Cy5 can serve as a fluorescent ligand, suitable for probe attachment through click chemistry. DIBA-Cy5 exerts a high binding affinity to type-2 mAChR (M2R) with the Kd value of 1.80 nM, can directly stain M2R receptors in the sinoatrial node of a mouse heart.
    DIBA-Cy5
  • HY-148526
    β2AR/M3-receptor agonist-1
    		Agonist
    β2AR/M3-receptor agonist-1 (example 9) is a potent β2AR and M3 receptor agonist. β2AR/M3-receptor agonist-1 shows M3 receptor affinity with a pIC50 value of 9.3. β2AR/M3-receptor agonist-1 has the potential for the research of respiratory tract disorders.
    β2AR/M3-receptor agonist-1
  • HY-B0954A
    Oxyphencyclimine
    		Antagonist
    Oxyphencyclimine is an orally active muscarinic receptor (mAChR) antagonist. Oxyphencyclimine is effective in reducing ulceration index and increasing pepsin activity in rat gastric ulcer model. Oxyphencyclimine can be used in studies of peptic ulcer disease and gastrointestinal spasm.
    Oxyphencyclimine
  • HY-B0520AS
    Benztropine-13C,d3 mesylate
    		Inhibitor
    Benztropine-13C,d3 (mesylate) is the 13C- and deuterium labeled Benztropine (mesylate). Benztropine mesylate (Benzatropine mesylate) is an orally active centrally acting anticholinergic agent that can be used for Parkinson's disease research. Benztropine mesylate is an anti-histamine agent and a dopamine re-uptake inhibitor. Benztropine mesylate is also a human D2 dopamine receptor allosteric antagonist. Benztropine mesylate also has anti-CSCs (cancer stem cells) effects.
    Benztropine-<sup>13</sup>C,d<sub>3</sub> mesylate
  • HY-N15736
    Petiline
    		Antagonist
    Petiline is a steroidal alkaloid found in Petilium raddeanum, acting as a selective antagonist of M cholinergic receptors. Petiline exerts anticholinergic effects (e.g., reducing vagal influence on the heart) by competitively blocking M cholinergic receptors, and also has central excitatory, cardiotonic, and spasmolytic activities. Petiline is promising for research of cholinergic system-related diseases (e.g., arrhythmia, intestinal spasm) .
    Petiline
  • HY-135460
    Milameline
    		Agonist
    Milameline (CI-979; RU35926) is a nonselective, partical and orally active muscarinic receptor agonist that improves cognition. Milameline has equal affinity for different subtypes of human muscarinic receptors with IC50 of 1.3 µM for M1-, 1.1 µM for M2-, 1.5 µM for M3-, and 1.9 µM for M4-muscarinic receptors. Milameline has a higher affinity for sites [3H]CMD (IC50 = 20 nM), than [3H]QNB, (IC50 = 3059 nM). Milameline produces both central and peripheral cholinergic effects and reverses the cognitive deficits induced by Scopolamine (HY-N0296). Milameline can be used for the study of Alzheimer’s Disease.
    Milameline
  • HY-B1205B
    Atropine hydrobromide
    		Antagonist
    Atropine (Tropine tropate) hydrobromide 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 hydrobromide inhibits ACh-induced relaxations in human pulmonary veins. Atropine hydrobromide can be used for research of anti-myopia and bradycardia.
    Atropine hydrobromide
  • HY-13204B
    Biperiden lactate
    		Inhibitor
    Biperiden (KL 373) lactate is an orally active non-selective muscarinic receptor antagonist that competitively binds to M1 muscarinic receptors. Biperiden (KL 373) lactate inhibits acetylcholine and enhances dopamine signaling in the central nervous system. Biperiden (KL 373) lactate has the potential for the research of Parkinson's disease and other related psychiatric disorders.
    Biperiden lactate
  • HY-B0761
    (R,R)-Glycopyrrolate
    (R,R)-Glycopyrrolate ((R,R)-Glycopyrronium (bromide); (R,R)-Glycopyrrolate (bromide)) is an anticholinergic agent. (R,R)-Glycopyrrolate ((R,R)-Glycopyrronium (bromide); (R,R)-Glycopyrrolate (bromide)) has the ability to reduce the frequency of drooling in vivo with developmental disabilities.
    (R,R)-Glycopyrrolate
  • HY-P5846
    Muscarinic toxin 3
    		Antagonist
    Muscarinic toxin 3 (MT3) is a potent and non-competitive mAChR and adrenoceptors antagonist with pIC50s of 6.71, 8.79, 8.86, 7.57, 8.13, 8.49, <6.5, 7.29 against M1, M4, α1A, α1B, α1D,α2A,α2B and α2C receptors, respectively. Muscarinic toxin 3 displays prominent adrenoceptor activity.
    Muscarinic toxin 3
  • HY-159177
    M4 mAChR Modulator-1
    		Modulator
    M4 mAChR Modulator-1 (compound 23i) is a M4 mAChR positive allosteric modulator (PAM). M4 mAChR Modulator-1 exhibits significantly greater cooperativity with ACh in β-arrestin recruitment over G protein activation. M4 mAChR Modulator-1 displays weak PAM effect in G protein-mediated responses, but strong PAM effect in β-arrestin recruitment.
    M4 mAChR Modulator-1
  • HY-120329
    Lu 26-046
    		Modulator
    Lu 26-046 is the agonist for muscarinic M1 receptor and M2 receptor and a weak antagonist for M3 receptor, with Ki of 0.51, 26 and 5 nM, respectively. Lu 26-046 exhibits specific stimulus property, that can be recognized by rats.
    Lu 26-046
  • HY-170444
    ADS1017
    		Antagonist
    ADS1017 is the antagonist for histamine receptor and muscarinic receptor, that exhibits good affinities to hH3R, hH4R, hM2R and hM4R with pKi of 6.8, 5.5, 7.4 and 7.2. ADS1017 exhibits analgesic and anti-allodynic efficacy in mice Capsaicin (HY-10448)-or Oxaliplatin (HY-17371)-induced pain models.
    ADS1017
Cat. No. Product Name / Synonyms Application Reactivity
mAChR Isoform Comparison

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