m4 machr

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).

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.

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.

Clozapine N-oxide is the major metabolite of Clozapine and is blood-brain barrier permeable. Clozapine N-oxide is an agonist of DREADDs and activates the DREADD receptors hM3Dq and hM4Di. Clozapine N-oxide is also a dopamine antagonist and selective muscarinic M4 receptor agonist.

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

Tropicamide (Ro 1-7683) is a synthetic muscarinic antagonist with anticholinergic properties similar to atropine. Upon ocular administration, it binds to and blocks muscarinic receptors in the sphincter and ciliary muscles, inhibiting cholinergic responses and causing pupil dilation and ciliary muscle paralysis. Tropicamide is used as a diagnostic agent to induce short-duration mydriasis and cycloplegia.

VU10010 (VU 10010) is allosteric potentiator of M4 acetylcholine receptors.

VU0152099 is a potent and selective M4 mAChR allosteric potentiator(EC50 = 380 ± 93 nM).

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

VU0467154 is a positive allosteric modulator of the M4 muscarinic acetylcholine receptor (M4 mAChR).

Emraclidine (CVL-231) is a novel, highly selective allosteric modulator of the muscarinic M4 receptor positive receptor for the study of neurological diseases.

AF-DX 384 free base is a selective and efficient M2 muscarinic acetylcholine receptor (M2 mAChR) and M4 muscarinic acetylcholine receptor (M4 mAChR) antagonist. It can be used for research on neurodegenerative diseases like Parkinson's.

PCS1055 dihydrochloride is an effective, selective, and competitive muscarinic M4 receptor antagonist (IC50: 18.1 nM and a Kd: 5.72 nM). PCS1055 dihydrochloride is also a potent AChE inhibitor (IC50 s: 22 nM and 120 nM for electric eel and human AChE, res

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].

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].

LY2119620 is a specific, and allosteric agonist of human M2 and M4 muscarinic acetylcholine 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.

Umeclidinium bromide (GSK573719A) is a novel mAChR antagonist.

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).

VU0152100 is an effective and selective allosteric potentiator of M4 mAChR (EC50: 380 ± 93 nM).

(Rac)-5-Hydroxymethyl Tolterodine hydrochloride, also known as (Rac)-Desfesoterodine hydrochloride, is an active metabolite of Tolterodine that functions as a mAChR antagonist. It exhibits significant affinity (K i values) for M1, M2, M3, M4, and M5 receptors, with values of 2.3 nM, 2 nM, 2.5 nM, 2.8 nM, and 2.9 nM, respectively. This compound is commonly employed in research related to overactive bladder conditions.

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].

Compound 4a, a mAChR antagonist, exhibits K i values of 255 nM for M1 and M5 subtypes, and lower values of 121 nM and 158 nM for M3 and M4 subtypes, respectively [1].

Xanomeline (LY-246708) is a functionally selective M1 M4 activator used in the study of neurological disorders such as schizophrenia and has shown promising treatment in preclinical trials. Xanomeline is well absorbed orally, crosses the blood-brain barrier and undergoes extensive liver metabolism with at least six metabolites.