M4 mAChR Modulator-2

M4 mAChR Modulator-2 is an orally active, selective, brain-penetrant positive allosteric modulator (PAM) of the M4 muscarinic acetylcholine receptor (M4 mAChR) (EC50 = 513 nM) . M4 mAChR Modulator-2 exhibits high target selectivity, showing negligible affinity and low inhibition rates for non-target receptors (D1R/D2R/D3R, 5-HT subtypes, κ/δ/μ opioid receptors, H1, M1/M2) while specifically binding to M4 mAChR with a Ki of 377 nM and an inhibition rate of 62.8%. M4 mAChR Modulator-2 reverses Dizocilpine (MK-801) (HY-15084B) -induced hyperlocomotion in mice. M4 mAChR Modulator-2 can be used for the study of schizophrenia[1]

Product Specifications

CAS Number

[3062458-27-6]

UNSPSC

12352005

Target

MAChR

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Smiles

CC1=C2C(CN(C(CC3CN(C4=CC(C5=CC=C(C#N)C(F)=C5)=NC=C4)C3)=O)C2)=NC(C)=C1

Molecular Formula

C26H24FN5O

Molecular Weight

441.50

References & Citations

[1]Luo Y, et al. Design, synthesis, and pharmacological evaluation of novel M4 muscarinic receptor positive allosteric modulators for schizophrenia treatment. Eur J Med Chem. 2025 Nov 15;298:117993.