mAChR
Muscarinic acetylcholine receptor
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
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mAChR Inhibitors
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mAChR Agonists
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mAChR Antagonists
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mAChR Activators
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mAChR Modulators
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mAChR Inducer
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mAChR Controls
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mAChR Ligands
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mAChR Related Products (727)
Related Products (727)
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Antibodies (2)
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mAChR Isoform Comparison
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ML169
0 ImagesCat. No.: HY-120576CAS No.: 1222878-02-5Synonyms: VU0405652ML169 (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.
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LAS190792
0 ImagesCat. No.: HY-148527CAS No.: 1347232-69-2Synonyms: AZD8999LAS190792 is a bifunctional muscarinic acetylcholine receptor (mAChR) antagonist and β2-adrenergic receptor agonist. LAS190792 has a pIC50 of 8.8 against human M3 muscarinic receptor and a pIC50 of 9.1 against human β2-adrenergic receptor. LAS190792 exhibits vasodilatory and anti-inflammatory activities, and induces sustained bronchodilation in dogs. LAS190792 inhibits the release of IL-8, MMP9, IL-1β and GM-CSF from lipopolysaccharide-stimulated neutrophils. LAS190792 can be used in research related to respiratory system diseases.
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BTM-1042
0 ImagesCat. No.: HY-136634CAS No.: 72293-40-4BTM-1042 is a newly synthesized compound with antispasmodic effects. It can inhibit the twitch reaction of the guinea pig ileum under electrical stimulation and is not affected by naloxone. It has similar effects to atropine and can block muscarinic receptors, but has less effect on other types of receptors. BTM-1042 also has an inhibitory effect on the ileal reaction caused by nicotine and 5-hydroxytryptamine. BTM-1042 showed a dose-dependent inhibitory effect on the spontaneous movement of the rabbit stomach. In general, BTM-1042 is a agent with a strong antispasmodic effect.
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Cetiedil citrate
0 ImagesCat. No.: HY-128547CAS No.: 16286-69-4Cetiedil citrate is a vasodilator and antihemolytic agent. Cetiedil citrate exerts anti-sickle cell anemia effects by blocking Ca2+-activated K+ channels (Gardos/KCa3.1). Cetiedil citrate is a muscarinic receptor antagonist that inhibits calcium-dependent release of acetylcholine (ACh) from mediated reconstituted proteoliposomes, with a Ki value of 5 μM. Cetiedil citrate possesses analgesic, spasmolytic and local anesthetic activities. Cetiedil citrate can be used in research related to ischemic leg pain caused by vascular diseases and sickle cell disease.
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Fesoterodine-d7 fumarate
0 ImagesCat. No.: HY-A0030SCAS No.: 2747918-94-9Fesoterodine-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).
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Xanomeline-NH-Boc
0 ImagesCat. No.: HY-186320CAS No.: 1018846-42-8Xanomeline-NH-Boc is a derivative of Xanomeline (HY-105182), which serves as the orthosteric pharmacophore of M1/M4 muscarinic agonist 4 (HY-187957) for activating mAChR1/4.
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Biperiden hydrochloride (Standard)
0 ImagesBiperiden (hydrochloride) (Standard) is the analytical standard of Biperiden (hydrochloride). This product is intended for research and analytical applications. 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 hydrochloride has the potential for the research of Parkinson's disease and other related psychiatric disorders.
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M1/M2/M4 muscarinic agonist 3
0 ImagesCat. No.: HY-149733CAS No.: 2640109-28-8M1/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.
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Tiotropium Bromide (Standard)
0 ImagesSynonyms: BA679 BR (Standard)Tiotropium (Bromide) (Standard) is the analytical standard of Tiotropium (Bromide). This product is intended for research and analytical applications. Tiotropium bromide (BA-679 BR) is a long-acting anticholinergic bronchodilator. Tiotropium bromide blocks the action of acetylcholine at muscarinic M1, M2, and M3 receptors, prevents bronchoconstriction, and dilates bronchial airways. Tiotropium bromide is applicable to research related to chronic obstructive pulmonary disease and asthma.
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Tiotropium-d3 iodide
0 ImagesCat. No.: HY-166417STiotropium-d3 iodide is the deuterium labeled Tiotropium iodide. Tiotropium-d3 iodide is a muscarinic acetylcholine receptor (mAChR) antagonist that blocks the binding of the acetylcholine ligand. Tiotropium-d3 iodide serves as a stable isotope tracer for quantitative analysis.
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Olanzapine-d8
0 ImagesCat. No.: HY-14541S2CAS No.: 1093380-13-2Synonyms: LY170053-d8Olanzapine-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.
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GSK1034702 hydrochloride
0 ImagesCat. No.: HY-107111ACAS No.: 932373-86-9GSK1034702 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).
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VU0364572
0 ImagesCat. No.: HY-113616CAS No.: 1240514-87-7VU0364572 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.
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Promethazine-d3(hydrochloride)
0 ImagesCat. No.: HY-B0781S1Promethazine-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.
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DIBA-Cy5
0 ImagesCat. No.: HY-151801DIBA-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.
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β2AR/M3-receptor agonist-1
0 ImagesCat. No.: HY-148526CAS No.: 1206887-00-4β2AR/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.
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Oxyphencyclimine
0 ImagesOxyphencyclimine 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.
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Benztropine-13C,d3 mesylate
0 ImagesCat. No.: HY-B0520ASBenztropine-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.
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CI-933
0 ImagesCat. No.: HY-106740CAS No.: 91829-95-7CI-933 is a nootropic. CI-933 can be used for the research of neurological disease.
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Petiline
0 ImagesCat. No.: HY-N15736CAS No.: 26989-18-4Petiline 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) .
