muscarinic m1

Compound 40 is a selective M1 M4 muscarinic antagonist with an IC50 of 19 nM for M1 receptors and 42 nM for M4 receptors [1].

Compound 42, also known as M1 M2 M4 muscarinic agonist 1, is a muscarinic M4 M1 M2 agonist exhibiting EC50 values of 6.5, 26, and 210 nM for M4, M1, and M2 respectively. This compound is utilized in research focused on mental disorders, including schizophrenia and delusion [1].

Muscarinic agonist 3 (compound 45) is a muscarinic mAChR M1 M2 M4 agonist with EC50 values of 3.2 nM, 32 nM, and 1.7 nM, respectively [1].

Compound 44, identified as an M1 M4 muscarinic agonist, exhibits potent activity with EC50 values of 31 nM at M1 and 9.3 nM at M4 mAChRs, respectively [1].

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.

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.

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

Tazomeline is a muscarinic M1 receptor agonist with neuroprotective activity.

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

Solifenacin succinate (YM905) is a quinuclidine and tetrahydroisoquinoline derivative and selective M3 MUSCARINIC ANTAGONIST. It is used as a UROLOGIC AGENT in the treatment of URINARY INCONTINENCE.

Diphenidol hydrochloride (Difenidol hydrochloride), a muscarinic antagonist, is employed as an anti-vertigo and as an antiemetic drug.

Oxybutynin chloride (Oxybutynin HCl) is an anticholinergic medication used to relieve urinary and bladder difficulties. It competitively antagonizes the M1, M2, and M3 subtypes of the muscarinic acetylcholine receptor.

Fesoterodine fumarate (Toviaz) is the fumarate salt form of fesoterodine, a competitive muscarinic receptor antagonist with muscle relaxant and urinary antispasmodic properties. Fesoterodine is rapidly hydrolyzed in vivo into its active metabolite 5-hydroxymethyl tolterodine, which binds and inhibits muscarinic receptors on the bladder detrusor muscle, thereby preventing bladder contractions or spasms caused by acetylcholine.

Pirenzepine dihydrochloride (LS519) is a selective M1 muscarinic receptor antagonist, inhibiting gastric secretion.

Olanzapine (LY170053) is an atypical antipsychotic that is used currently in the treatment of schizophrenia and bipolar illness.

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.

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.

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).

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

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.

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).

WEB-1868 is one of the metabolites of nebracetam which is an agonist for human M1-muscarinic receptors.