mAChR Agonist

Deschloroclozapine dihydrochloride, a metabolite of Clozapine, is a highly potent muscarinic DREADDs agonist. Deschloroclozapine binds to DREADD receptor subtypes hM3Dq and hM4Di with K_i of 6.3 and 4.2 nM, respectively. [¹¹C]-Deschloroclozapine is developed as a promising PET tracer for DREADD imaging.

Xanomeline (LY 246708) is the potent agonist of muscarinic M1/M4 receptor with antipsychotic-like activity. Xanomeline (LY 246708) increases neuronal excitability. Xanomeline (LY 246708) can be used for the research of schizophrenia.

Betovumeline hydrochloride is the agonist for muscarinic receptor and can be used for researchs of neurological disorders.

Arecoline hydrobromide, a naturally brain-penetrant and orally active occurring psychoactive alkaloid, is a partial agonist of nicotinic and muscarinic acetylcholine receptor. Arecoline hydrobromide exhibits stimulation, alertness, anxiolysis and anti-parasitic effects. Arecoline hydrobromide also can induce oxidative stress.

Xanomeline oxalate (LY246708 oxalate) is a potent and selective muscarinic receptor agonist (SMRA) and stimulates phosphoinositide hydrolysis in vivo. Xanomeline oxalate can be used for the research of Alzheimer’s disease.

Oxotremorine M iodide is a potent and non-selective muscarinic acetylcholine receptor (mAChR) agonist. Oxotremorine M iodide potentiates NMDA receptors by muscarinic receptor dependent and independent mechanisms.

Anethole trithione, a sulfur heterocyclic choleretic, is a bile secretion-stimulating agent. Anethole trithione enhances salivary secretion and increases mAChRs, and can be used for dry mouth research.

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).

PQCA 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.

Muscarine ((+)-Muscarine) chloride is an agonist of prototype mAChR. Muscarine chloride is a toxin that can stimulate the parasympathetic nervous system.

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.

Arecaidine 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.

Muscarine ((+)-Muscarine) iodide is a toxin that can stimulate the parasympathetic nervous system. Muscarine iodide is a prototype muscarinic acetylcholine receptor agonist.

LY593093 is a selective, orally active, and brain-penetrant muscarinic M1 receptor agonist with an EC₅₀ of 22.8 nM. LY593093 can be utilized in Alzheimer’s disease research.

M4 mAChR agonist-1 (compound 10a) is a potent M4 mAChR agonist with an EC₅₀ >10 μM for human M4.

PF-06767832 is a potent muscarinic M1 selective positive allosteric modulator (PAM), with the EC₅₀ of 60 nM. PF-06767832 has good brain penetration.

LASSBio-873 is an orally active muscarinic cholinergic receptor (mAChR) agonist that crosses the blood-brain barrier. LASSBio-873 has potent analgesic effects on acute and inflammatory pain. The analgesic effect of LASSBio-873 can be inhibited by intrathecal injection of the M2 receptor antagonist methoctramine.

Guvacoline hydrobromide, a pyridine alkaloid found in Areca triandra, can act as a weak full agonist of atrial and ileal mAChR.

Clozapine N-oxide (Standard) is the analytical standard of Clozapine N-oxide. This product is intended for research and analytical applications. Clozapine N-oxide is a major metabolite of Clozapine and a human muscarinic designer receptors (DREADDs) agonist. Clozapine N-oxide activates the DREADD receptor hM3Dq and hM4Di. Clozapine N-oxide cannot cross the blood-brain barrier[1][2][3][4]. Clozapine is a potent dopamine antagonist and also a potent and selective muscarinic M4 receptor (EC50=11 nM) agonist[5][6].

VU0152099 is a potent, selective and brain-penetrant mAChR M4 positive allosteric modulator with an EC₅₀ of 0.4 µM for rat M4 receptor. VU0152099 is inactive for other mAChR subtypes or other GPCRs. VU0152099 has no agonist activity but potentiated responses of M4 to acetylcholine.