machr m1

Xanomeline tartrate (LY 246708 tartrate) is an M1 and M4 mAChR agonist with antipsychotic-like activity that improves cognition and can be used in studies of schizophrenia and Alzheimer's disease.

YM-58790 free base is a potent mAChR antagonist that inhibits M1 mAChR, M2 mAChR, and M3 mAChR with Ki values of 28 nM, 260 nM, and 15 nM, respectively. It inhibits reflex rhythmic bladder contractions in rats by inhibiting bladder pressurization.

(Rac)-Sabcomeline ((Rac)-SB-202026) is an M1 M4 muscarinic agonist used in the study of neurologic disorders such as schizophrenia.

CDD0102 HCl is a selective and potent M1 muscarinic receptor agonist for the treatment of Alzheimer's disease.

AF-710B is a specific variant of M1 muscarinic and Sigma-1 receptor agonist used in the study of neurological disorders such as Alzheimer's disease dementia and schizophrenia.

GSK-1034702 is an M1 mAChR agonist that improves cognitive deficits and may be useful in the study of neurologic disorders.

Tazomeline is a muscarinic M1 receptor agonist with neuroprotective activity.

Solifenacin (YM905 free base) (YM905 free base) is a novel muscarinic receptor antagonist, its pKis for M1, M2 and M3 receptors is of 7.6, 6.9 and 8.0, respectively.

Glycopyrrolate (Glycopyrrolate bromide) is a muscarinic antagonist used as an antispasmodic, in some disorders of the gastrointestinal tract, and to reduce salivation with some anesthetics.

Irsogladine (Dicloguamine) is an anti-gastric ulcer agent that facilitates gap-junctional intercellular communication through M1 muscarininc acetylcholine receptor binding.

Trihexyphenidyl hydrochloride (Benzhexol hydrochloride) is an antiparkinsonian agent of the antimuscarinic class.

Clozapine (HF 1854) is a tricylic dibenzodiazepine, classified as an atypical antipsychotic agent. It binds several types of central nervous system receptors, and displays a unique pharmacological profile. Clozapine is a serotonin antagonist, with strong binding to 5-HT 2A 2C receptor subtype. It also displays strong affinity to several dopaminergic receptors, but shows only weak antagonism at the dopamine D2 receptor, a receptor commonly thought to modulate neuroleptic activity.

VU0357017 hydrochloride (ML071 hydrochloride) is highly selective M1 agonists act at an allosteric site to activate the receptor (EC50: 477 ± 172 nM; Pec50: 6.37 ± 0.15).

Pimethixene (Calmixen) is a highly potent 5-HT1A, 5-HT2A, 5-HT2B, 5-HT2C, histamine H1, dopamine D2 and D4.4 as well as muscarinic M1 and M2 receptors antagonist(pKis of 7.63, 10.22, 10.44, 8.42, 10.14, 8.19, 7.54, 8.61 and 9.38, respectively).

VU0119498 is a M1 muscarinic receptor agonist (EC50 = 3.1 μM) and pan mAChR M3, M5 positive allosteric modulator (PAM),and is a neuroprotective agent.

Nebracetam hydrochloride (WEB 1881 FU hydrochloride) is an agonist nootropic M1-muscarinic. Nebracetam hydrochloride induces a rise of intracellular Ca2+ concentration. Nebracetam hydrochloride exhibits an EC50 of 1.59 mM for elevating [Ca2+]i.

DREADD agonist 21 is a potent agonist of human muscarinic acetylcholine M3 receptors (EC50=1.7 nM).

BQCA (benzylquinolone carboxylic acid) a highly selective allosteric M1 mAChR modulator.

McN-A 343 is a selective M1 muscarinic agonist known for its ability to stimulate muscarinic transmission in sympathetic ganglia. It has been found to effectively reduce inflammation and oxidative stress in experimental models of ulcerative colitis.

Terodiline hydrochloride is an antagonist of M1-selective muscarinic receptor (mAChR)(Kbs of 15, 160, 280, and 198 nM in rabbit vas deferens (M1), atria (M2), bladder (M3) and ileal muscle (M3), respectively).

Muscarinic toxin 3 (MT3), a potent non-competitive antagonist of mAChR and adrenoceptors, exhibits pIC50 values of 6.71 for M1, 8.79 for M4, 8.86 for α1A, 7.57 for α1B, 8.13 for α1D, 8.49 for α2A, <6.5 for α2B, and 7.29 for α2C receptors. MT3 notably demonstrates significant adrenoceptor activity [1].

TBPB, an allosteric M1 mAChR agonist, is an [iso]propyl (2-{4-methoxy-3-[3-(4-methylpiperidin-1-yl)propoxy]phenyl}ethyl)carbamate exhibiting a molar mass of 430.6 g mol.

Oxotremorine acts as an agonist of mAChR, specifically activating the M1 and M3 acetylcholine receptors. In drug discrimination experiments with macaques, it exhibits effects similar to nicotine.

Penehyclidine hydrochloride (Penequinine hydrochloride) is an M1 and M3 antagonist and activates NF-κB in lung tissue. Penehyclidine hydrochloride inhibits the release of inflammatory factors and shows anticholinergic properties.