VU0467154 是 M4 毒蕈碱的乙酰胆碱受体的正向调节剂,能够增强小鼠、人和食蟹猴 M4 受体对乙酰胆碱的反应,pEC50值分别为 7.75、6.2 和 6。
产品描述
VU0467154 is a positive allosteric modulator of the M4 muscarinic acetylcholine receptor.
体外活性
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[1].
体内活性
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[1]. VU0467154 also enhanced the acquisition of both contextual and cue-mediated fear conditioning when administered alone in wild-type mice[1].
Cas No.
1451993-15-9
分子式
C17H15F3N4O3S2
分子量
444.45
别名
VU0467154
储存和溶解度
DMSO:50 mg/mL (112.50 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years