VU0152100 是一种选择性 M4 mAChR 变构增强剂，EC50为 380 ± 93 nM。

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

VU0152100 was selective for M4 relative to M1, M2, M3, and M5. VU0152100 dose-dependently potentiated the response to an EC20 concentration of ACh (EC50: 1.9 ± 0.2 μM) and increased the maximal response to ACh to approximately 130%. VU0152100 (10 μM) also increased the potency of ACh to induce GIRK-mediated thallium flux, as manifest by a robust (≈30-fold) leftward shift in the ACh CRC from 77 ± 1.2 nM (veh) to 2.35 ± 0.5 nM [1].

Systemic administration of VU0152099 and VU0152100 provides robust brain levels of these compounds, the effects of VU0152099 and VU0152100 were evaluated in reversing amphetamine-induced hyperlocomotion in rats using a dose of 56.6 mg/kg i.p. for each compound with a 30-min pretreatment interval [1].

409351-28-6

C18H19N3O2S

341.43

VU152100;VU0152100

DMSO:45 mg/mL (131.80 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years