VU0467154

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

VU0467154 是 M4 毒蕈碱乙酰胆碱受体的正变构调节剂。

VU0467154 is a positive allosteric modulator of the M4 muscarinic acetylcholine receptor.(In Vitro):VU0467154 potentiates the response to ACh with pEC50s of 7.75(rat), 6.2(human) and 6(cynomolgus monkey) for M4 receptor, respectively. VU0467154 does not potentiate the ACh response at rat and human M1, M2, M3, or M5.(In Vivo):VU0467154 produced a robust dose-dependent reversal of MK-801-induced hyperlocomotion and deficits in preclinical models of associative learning and memory functions, including the touchscreen pairwise visual discrimination task in wild-type mice, but failed to reverse these stimulant-induced deficits in M4 KO mice. VU0467154 also enhanced the acquisition of both contextual and cue-mediated fear conditioning when administered alone in wild-type mice.

VU0467154 is a positive allosteric modulators of the M4 muscarinic acetylcholine receptor (mAChR), robustly potentiates the response to ACh with pEC50s of 7.75, 6.2 and 6 for rat, human and cynomolgus monkey (cyno) M4 receptor, respectively. VU0467154 does not potentiate the ACh response at rat and human M1, M2, M3, or M5.

VU0467154 (1-56.6 mg/kg, p.o. or i.p.) reverses amphetamine-induced hyperlocomotion in rats. VU0467154 (0.3-30 mg/kg, i.p.) reverses amphetamine- and MK-801-induced hyperlocomotion in wild-type but not M4 KO mice. VU0467154 alone also enhances the acquisition of both contextual and cue-mediated fear conditioning in wild-type mice.

——

Cell Cycle/DNA Damage

AChR

Nucleoside Antimetabolite/Analog

——

——

1451993-15-9

444.45

C17H15F3N4O3S2

>98% (HPLC)

In Vitro:?DMSO : 13.89 mg/mL (31.25 mM)

Cc1nnc2sc(C(=O)NCc3ccc(cc3)S(=O)(=O)C(F)(F)F)c(N)c2c1C

——

(-20℃)

With Ice Pack

≥ 2 years