machr in 1

mAChR-IN-1 is muscarinic cholinergic receptor(mAChR) antagonist (IC50=17 nM).

mAChR-IN-1 hydrochloride is a potent antagonist of muscarinic cholinergic receptors (mAChR) with an IC50 of 17 nM.

M4 mAChR Modulator-1 (compound 23i) acts as a positive allosteric modulator (PAM) of the M4 mAChR. It demonstrates a stronger synergistic effect in β-arrestin recruitment compared to G protein activation when interacting with ACh. Additionally, while its PAM effects are weaker in G protein-mediated responses, they are more potent in β-arrestin recruitment.

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.

M3mAChRagonist 1 is a dual positive allosteric modulator (PAM) that primarily targets the M3 subtype of M3/M5 mAChRs. It demonstrates high subtype selectivity over other mAChR subtypes, including M1, M2, and M4. By modulating the M3 muscarinic acetylcholine receptor, M3mAChRagonist 1 enhances the signaling pathway, leading to increased contraction of isolated rat bladder strips.

mAChR antagonist 1 (Compound 4a), an mAChR antagonist, exhibited Ki values of 255 nM, 121 nM, 158 nM and 255 nM for the M1, M3, M4 and M5 subtypes, respectively.

M4 mAChR agonist-1 (4-Piperidinecarboxamide, 1-(5,6-dimethylthieno[2,3-d]pyrimidin-4-yl)-) is an effective agonist of M4 mAChR (EC50 >10 μM).

Aceclidine (1-azabicyclo[2.2.2]octan-3-yl acetate) is a modulator of M3 mAChR and can be used in studies about treating glaucoma by reducing intraocular pressure.

Atropine methyl bromide (Methylatropine bromide) is a quaternary ammonium salt of atropine, characterized as a muscarinic receptor (mAChR) antagonist. It functions as a mydriatic to dilate the pupil during ophthalmic examination. Compared to atropine, it demonstrates reduced penetration into the central nervous system[1][2]. Its high polarity makes it particularly effective in relieving pyloric spasm in infants.

Cycrimine is an orally active antagonist of the muscarinic cholinergic receptor (mAChR) M1 that reduces the level of acetylcholine in the Parkinson's model. Cycrimine exhibits antispasmodic activity that can be used in behavioral and mental disorders research [1] [2] [3] [4].

N-Demethyl MK-6884 (compound 34) is a significant allosteric modulator of the M4 mAChR, relevant in Alzheimer's disease research and studies of other M4 mAChR-related diseases [1].

VU6019650 is a potent and selective orthosteric antagonist of M5 mAChR ( IC 50 =36 nM), can be used for opioid use disorder (OUD) relief. VU6019650 can cross blood brain barrier, potentially modulates the mesolimbic dopaminergic reward circuitry. VU6019650 blocks Oxotremorine M iodide induced increases of neuronal firing rates of midbrain dopamine neurons in the ventral tegmental area (VTA) [1] [2] .