VU6009048 is a potent, selective M4 positive allosteric modulator (PAM) with EC50 of 85 nM (hM4) and 379 nM (rM4).

VU6007215 is a potent, selective M4 positive allosteric modulator (PAM) with EC50 of 144 nM (hM4) and 295 nM (rM4).

ML381 (VU0488130) is a highly mAChR subtype selective M5 orthosteric antagonist with IC50/Ki of 450/340 nM for hM5, has no inhibitory activity on hM1-4 (IC50>30 uM); exhibits good DMPK properties and CNS penetration (B:P ratio of 0.58) to support both in vitro and in vivo studies.

LSN3172176 is a novel potent, selectiive M1 mAChR partial agonist (EC50 2.4-7.0nM, Emax 43%-73%), shows binding selectivity for M1 mAChRs (Kd=1.5 nM); LSN3172176 is a potential PET tracer for assessment of M1 mAChR target engagement in the clinic and to further elucidate the function of M1 mAChRs in health and disease.

GSK1034702 (GSK-1034702) is a potent, allosteric M1 receptor agonist, inhibits binding of [3H]-NMS (0.5 nM) to M1 mAChR with pKi of 6.5; improves memory encoding potentially by modulating hippocampal function.

McN-A-343 is a selective M1 muscarinic agonist that stimulates muscarinic transmission in sympathetic ganglia. McN-A-343 reduces inflammation and oxidative stress in an experimental model of ulcerative colitis.

Heliosupine N-oxide, Heliosupin metabolite, inhibits muscarinic acetylcholine receptor (mAChR) with the IC50 of 350 μM. Heliosupine N-oxide is a pyrrolizidine alkaloid (PA).

VU0455691 is a potent, selective orthosteric M1 mAChR antagonist (pIC50=6.64; IC50=0.23 µM for hM1).

VU 0238429 is positive allosteric modulator of muscarinic acetylcholine receptor subtype 5 (mAChR5 or M5), with an EC50 of 1.16 μM.

(±)-Muscarine chloride is the racemate of Muscarine chloride. Muscarine is a prototype muscarinic acetylcholine receptor agonist.

AF-DX 384 is a selective antagonist of M2 and M4 muscarinic acetylcholine receptors (Kis=6.03 and 10 nM, respectively). AF-DX 384 reverses deficits in novel object recognition and passive avoidance in aged rats, as well as in young rats with impairments induced by scopolamine.

Prifinium bromide is antimuscarinic agent with antispasmodic, antiemetic effect.

Octamylamine is an anticholinergic and antispasmodic agent.

VU 0365114 is a mAChR M5 positive allosteric modulator, with an EC50 of 2.7 μM.

Batefenterol（GSK961081，TD-5959）is a Muscarinic Antagonist and β2-Agonist possessing both muscarinic antagonist (MA) and β2-adrenoceptor agonist (BA) properties (MABA).

Methoctramine tetrahydrochloride is a potent and cardioselectivity antagonist of M2 muscarinic receptor. Methoctramine tetrahydrochloride can inhibit Muscarine-induced bradycardia in vivo.

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.

Sabcomeline (hydrochloride) is a potent and functionally selective muscarinic M1 receptor partial agonist that improve cognition.

Milameline is a muscarinic receptor agonist that improves cognition.

MK-6884-11C is a positron emission tomography (PET) imaging agent for the study of M4 muscarinic receptor positive allosteric modulators (PAMs) in neurodegenerative diseases.

Nor-benzetimide is a major metabolite of Benzetimide. Benzetimide is a mAChR antagonist with anticholinergic activity.

VU0119498 is a pan Gq mAChR M1, M3, M5 positive allosteric modulator (PAM), with EC50s of 6.04, 6.38, and 4.08 μM, respectively. VU0119498 has antidiabetic activity.

JHU37152 is a Designer Receptors Exclusively Activated by Designer Drug (DREADD) agonist with Ki of 1.8 nM and 8.7 nM for human muscarinic acetylcholine M3 receptors (hM3Dq) and hM4Di in vitro, respectively. And EC50 values are 5 nM and 0.5 nM for hM3Dq and hM4Di in fluorescent and BRET-based assays in HEK-293 cells, respectively.,hM4Di [1](Cell-free assay) hM3Dq [1](Cell-free assay) hM3Dq [1](Cell-free assay) hM4Di [1](Cell-free assay) 0.5 nM(EC50) 1.8 nM(Ki) 5 nM(EC50) 8.7 nM(Ki),JHU37152 is a potent DREADD agonist with high potency and efficacy in fluorescent and BRET-based assays in HEK-293 cells, whereas no responses are observed in untransfected HEK-293 cells.[1],JHU37152 exhibits high in vivo DREADD potency. JHU37152 exhibits selective [3H]clozapine displacement from DREADDs in brain tissue from WT and D1-DREADD mice.[1]

DREADD agonist 21 is a potent muscarinic hM3Dq DREADD agonist (EC50 = 1.7 nM). Highly selective for hM3Dq DREADDs over endogenous hM3 receptors.

Iperoxo is a superagonist of the muscarinic acetylcholine receptors and an OxotremorineM analog.

Navafenterol (AZD-8871) is an inhaled dual-acting, potent, selective, and long-lasting M3-antagonist/β2-agonist (MABA) with long-lasting effects and favorable safety profile. The pIC50 is 9.5 for human M3 receptor, and the pEC50 is 9.5 for β2-adrenoceptor. Navafenterol can be used for the research of chronic obstructive pulmonary disease (COPD). Bronchoprotective and antisialagogue effects. Favorable cardiovascular profile.

(Rac)-5-Hydroxymethyl Tolterodine ((Rac)-Desfesoterodine), an active metabolite of Tolterodine, is a mAChR antagonist (Ki values of 2.3 nM, 2 nM, 2.5 nM, 2.8 nM, and 2.9 nM for M1, M2, M3, M4, and M5 receptors, respectively). (Rac)-5-Hydroxymethyl Tolterodine can be used for overactive bladder research.

(Rac)-5-Hydroxymethyl Tolterodine ((Rac)-Desfesoterodine) hydrochloride, an active metabolite of Tolterodine, is a mAChR antagonist (Ki values of 2.3 nM, 2 nM, 2.5 nM, 2.8 nM, and 2.9 nM for M1, M2, M3, M4, and M5 receptors, respectively). (Rac)-5-Hydroxymethyl Tolterodine hydrochloride can be used for overactive bladder research.

Navafenterol (AZD-8871) saccharinate is an inhaled, long-acting bronchodilator, which is a muscarinic antagonist and β2 agonist.

LY2033298 is a robust allosteric potentiator that is highly selective for the human M4 muscarinic acetylcholine receptor subtype. LY2033298 enhances inhibition by oxotremorine of light-induced phase shifts in hamster circadian activity rhythms.