m1 machr

M1mAChRmodulator-1 (Example 66) is a positive allosteric modulator of the muscarinic M1 receptor (mAChR1). It effectively enhances gastrointestinal motility and defecation in mouse models while exhibiting low central penetration. M1mAChRmodulator-1 is applicable for constipation research.

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.

(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.

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.

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

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).

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

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).

Pimethixene maleate (Pimetixene maleate) is a potent 5-HT2B receptor antagonist with sedative and antitussive activity.Pimethixene maleate inhibits 5-HT1A, 5-HT2A, 5-HT2B, 5-HT2C, histamine H1, dopamine D2 and D4.4 as well as muscarinic M1 and M2, and can be used in studies of dry and irritant cough in children. irritant cough in children.

TAK-071 is a potent, novel and highly selective modulator of muscarinic acetylcholine receptor 1 (M1R) positive allosteric(EC50 : 520 nM).

MK-7622 (M1 receptor modulator) is a positive allosteric modulator of the muscarinic M1 receptor.

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.

(S)-(+)-Dimethindene maleate is an orally available, selective muscarinic M2 receptor and histamine H1 receptor antagonist that also inhibits muscarinic M1, M3, and M4 receptors.

Aclidinium bromide (LAS-W 330) is a synthetic anticholinergic agent that is used as an inhalant for treatment of acute bronchospasm due to chronic bronchitis or emphysema. Aclidinium has not been implicated in causing liver enzyme elevations or clinically apparent acute liver injury.

VU0453595 is a M1 positive allosteric modulator (PAM).

Umeclidinium bromide (GSK573719A) is a novel mAChR antagonist.

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.

Oxomemazine is a phenothiazine-based histamine H1-receptor blocker with pronounced antimuscarinic activity. It is a selective antagonist of mycotoxins M1 receptors, exhibiting high (Ki=84 nM, M1 receptors) and low (Ki=1.65 μM, M2 receptors) affinity, with a 20-fold difference. Oxomemazine is an antihistamine and anticholinergic agent used in cough studies[1][2].

Fesoterodine ((R) Fesoterodine) is an orally active, competitive mAChR antagonist with pKi values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. It is used for the overactive bladder (OAB).

PQCA is a muscarinic M1 receptor-positive allosteric regulator, which is highly selective and effective. PQCA exhibited EC50 values of 49 nM in rhesus monkey and 135 nM in human M1 receptors, but showed no activity against other muscarinic receptors. PQCA is a potential compound for reducing cognitive deficits associated with Alzheimer's disease.

Tazomeline is a muscarinic M1 receptor agonist with neuroprotective activity.

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.