VU0152100

Research use only, not for human use.

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

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

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Animal Model:Adult male Sprague-Dawley rats (250-275 g; amphetamine-induced hyperlocomotion model).Dosage:10, 30, 56.6 mg/kg Administration:Intraperitoneal injection; single (pre-treatment)Result:Produced a robust dose-dependent reversal of amphetamine-induced hyperlocomotion.Animal Model:Adult male Sprague-Dawley rats (250-275 g; amphetamine-induced).Dosage:10, 30, 56.6 mg/kg Administration:Intraperitoneal injection; single (pre-treatment)Result:Blocked amphetamine-induced disruption of prepulse inhibition.Dose-dependently reversed the disruptive effects of amphetamine on the acquisition of a context-dependent fear.

VU152100

Cell Cycle/DNA Damage

AChR

5-HT2| H1 receptor| α1-adrenergic receptor

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409351-28-6

341.43

C18H19N3O2S

>98% (HPLC)

In Vitro:?DMSO : ≥ 50 mg/mL (146.44 mM)

CC1=C2C(SC(C(NCC3=CC=C(OC)C=C3)=O)=C2N)=NC(C)=C1

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(-20℃)

With Ice Pack

≥ 2 years