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
All Product Categories
-
mAChR Inhibitors
(114)
View all products
-
mAChR Agonists
(146)
View all products
-
mAChR Antagonists
(320)
View all products
-
mAChR Activators
(20)
View all products
-
mAChR Modulators
(48)
View all products
-
mAChR Inducer
(1)
View all products
-
mAChR Controls
(9)
View all products
-
mAChR Ligands
(8)
View all products
-
mAChR Related Products (719)
Related Products (719)
-
Antibodies (2)
-
mAChR Isoform Comparison
-
Cevimeline hydrochloride hemihydrate
0 ImagesSynonyms: SNI-2011; AF102B hydrochloride hemihydrateCevimeline hydrochloride hemihydrate (SNI-2011) is a quinuclidine derivative of acetylcholine and a selective and orally active muscarinic M1 and M3 receptor agonist. Cevimeline hydrochloride hemihydrate stimulates secretion by the salivary glands and can be used as a sialogogue for xerostomia. Cevimeline hydrochloride hemihydrate can cross the blood-brain barrier (BBB).
-
MK-7622
0 ImagesSynonyms: M1 receptor modulatorMK-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).
-
VU0467154
0 ImagesVU0467154 is a positive allosteric modulator of the M4 muscarinic acetylcholine receptor (mAChR), potentiating the response to ACh with pEC50s of 7.75, 6.2 and 6 for rat, human and cynomolgus monkey M4 receptor, respectively.
-
VU0453595
0 ImagesVU0453595 is a highly selective, systemically active M1 positive allosteric modulator (PAM, EC50=2140 nM) for the research of schizophrenia.
-
Sabcomeline hydrochloride
0 ImagesSynonyms: SB-202026 hydrochloride; Memric hydrochlorideSabcomeline (SB-202026; Memric) hydrochloride is a muscarinic receptor agonist capable of crossing the blood-brain barrier. Sabcomeline hydrochloride exhibits affinity for all hM1 to hM5 subtypes (pKi=6.72-7.23), and shows near-full agonism at the hM3 receptor, inducing extracellular acidification. Sabcomeline hydrochloride alters the binding kinetics of dopamine D2 receptors through neural network regulation. Sabcomeline hydrochloride also causes minimal cardiovascular changes, effectively reverses spatial memory deficits in rodents and induces conditioned taste aversion. Sabcomeline hydrochloride is an important tool compound in studies of Alzheimer's disease and related neurodegenerative diseases.
-
GSK1034702
0 ImagesGSK1034702 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).
-
Smilagenin
0 ImagesSmilagenin (SMI) is a small-molecule steroidal sapogenin from Anemarrhena asphodeloides and Pelargonium hortorum widely used in traditional Chinese medicine for treating chronic neurodegeneration diseases. Smilagenin (SMI) improves memory of aged rats by increasing the muscarinic receptor subtype 1 (M1)-receptor density. Smilagenin (SMI) attenuates Aβ(25-35)-induced neurodegenerationvia stimulating the gene expression of brain-derived neurotrophic factor, may represents a novel therapeutic strategy for AD.
-
VU0357017 hydrochloride
0 ImagesSynonyms: CID-25010775VU0357017 hydrochloride (CID-25010775) is a potent, selective and brain-penetrant allosteric agonist of M1 muscarinic acetylcholine receptor, with an EC50 of 477 nM. VU0357017 hydrochloride is highly selective for M1 and has no activity at M2-M5 up to the highest concentrations tested (30 μM). VU0357017 hydrochloride can be used for the research of Alzheimer’s disease and schizophrenia.
-
N-Desmethylclozapine
0 ImagesSynonyms: Norclozapine; Desmethylclozapine; NormethylclozapineN-Desmethylclozapine is a major active metabolite of the atypical antipsychotic agent Clozapine. N-Desmethylclozapine is a potent, allosteric and partial M1 receptors agonist (EC50=115 nM) and is able to potentiate hippocampal N-methyl-d-aspartate (NMDA) receptor currents through M1 receptor activation. N-Desmethylclozapine is also a δ-opioid agonist.
-
McN-A-343
0 ImagesMcN-A-343 is a selective M1 muscarinic agonist that stimulates muscarinic transmission in sympathetic ganglia. McN-A-343 produces a significant inhibitory effect on Muscarine (HY-121404)-evoked catecholamine secretion from the isolated perfused rat adrenal gland. McN-A-343 is involved in the regulation of neuronal firing and activates enteroendocrine L cells to release glucagon-like peptide 1 (GLP-1) and modulates the secretion of α-melanocyte stimulating hormone (α-MSH) from the pituitary gland in the central nervous system. McN-A-343 reduces colonic inflammation and oxidative stress in Acetic acid (HY-Y0319)-induced ulcerative colitis (UC) mice. McN-A-343 can be used for the study of ulcerative colitis.
-
VU0364572 TFA
0 ImagesVU0364572 TFA is an orally active and selective allosteric agonist of the M1 muscarinic receptor with an EC50 of 0.11 μM. VU0364572 TFA has neuroprotective potential for preventing memory impairments and reducing neuropathology in Alzheimer’s Disease. VU0364572 TFA is CNS penetrant.
-
PQCA
0 ImagesPQCA is a highly selective and potent muscarinic M1 receptor positive allosteric modulator. PQCA has an EC50 value of 49 nM and 135 nM on rhesus and human M1 receptor, respectively. PQCA is inactive for other muscarinic receptors. PQCA has potential to reduce the cognitive deficits associated with Alzheimer's disease.
-
VU 0238429
0 ImagesVU 0238429 is positive allosteric modulator of muscarinic acetylcholine receptor subtype 5 (mAChR5 or M5), with an EC50 of 1.16 μM.
-
TBPB
0 ImagesTBPB (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).
-
ML380
0 ImagesML380 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.
-
Arecaidine but-2-ynyl ester tosylate
0 ImagesSynonyms: ABETArecaidine but-2-ynyl ester tosylate (ABET) is a selective mAChR M2 agonist that dose-dependently decreases mean arterial pressure and heart rate in rats. Arecaidine but-2-ynyl ester tosylate can be used for cardiovascular disease research. Arecaidine but-2-ynyl ester (tosylate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
