VU0152099 (C09-1184-863)

VU0152099 is a potent, selective and brain-penetrant mAChR M4 positive allosteric modulator with an EC 50 of 0.4 µM for rat M4 receptor. VU0152099 is inactive for other mAChR subtypes or other GPCRs. VU0152099 has no agonist activity but potentiated responses of M4 to acetylcholine.In VitroVU0152099 (30 µM) induces a dose-dependent leftward shift of the acetylcholine (ACh) concentration response curve (CRC) with maximal shifts of 30-fold observed with 30 µM. VU0152099 dose-dependently potentiates the response to an EC20 concentration of ACh with EC 50 values of 1.2 µM, and increases the maximal response to ACh to approximately 130%. VU0152099 is a potent positive allosteric modulator that enhance the response of the M4 receptor to the endogenous agonist ACh. MCE has not independently confirmed the accuracy of these methods. They are for reference only.In VivoVU0152099 (56.6 mg/kg; i.p.; once) reverses Amphetamine-induced hyperlocomotion in rats . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male Sprague-Dawley rats (270-300 g) injected with Amphetamine Dosage: 56.6 mg/kg Administration: i.p.; once Result: Reversed Amphetamine-induced hyperlocomotion in rats.Form:Solid. Specification: 0.98 Molecular Formula: C18H17N3O3S Molecular Weight: 355.4 PubChem CID: 1541501 Isomeric SMILES: CC1=CC(=NC2=C1C(=C(S2)C(=O)NCC3=CC4=C(C=C3)OCO4)N)C