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  4. GPR52 agonist-1

GPR52 agonist-1 是一种有效且具有口服活性和血脑屏障透过性的 GPR52 激动剂，pEC50 为 7.53。GPR52 agonist-1 通过与 GPR52 的直接互作来影响 cAMP 积累。GPR52 agonist-1 能显著抑制甲基苯丙胺 (Methamphetamine) 诱导的小鼠多动行为。具有抗精神病活性。

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GPR52 agonist-1 Chemical Structure

GPR52 agonist-1 Chemical Structure

CAS No. : 1207965-40-9

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GPR52 agonist-1 相关抗体

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生物活性

GPR52 agonist-1 is a potent, orally active and blood-brain barrier (BBB) penetrant GPR52 agonist with an pEC50 value of 7.53. GPR52 agonist-1 affects cAMP accumulation through direct interaction with GPR52. GPR52 agonist-1 can significantly suppress Methamphetamine-induced hyperactivity in mice. Antipsychotic activity[1].

IC50 & Target

pEC50: 7.53 (GPR52)[1]
体内研究
(In Vivo)

GPR52 agonist-1 (compound 7m) (3, 10, and 30 mg/kg; PO; single dosage) attenuates Methamphetamine-induced hyperlocomotion in mice[1].
GPR52 agonist-1 (0.1 mg/kg, IV and 1 mg/kg, PO; single dosage) exhibits good oral pharmacokinetic profile with an Cmax of 108.1 ng/mL, an AUC0-8h of 613.7 ng·h/mL, and an F (bioavailability) of 73% in mouse[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male ICR mice (7-8 weeks; subcutaneously injected with 2 mg/kg Methamphetamine after 60 min administration)[1]
Dosage: 3, 10, and 30 mg/kg
Administration: PO; single dosage
Result: Attenuated Methamphetamine-induced hyperlocomotion dose-dependently.
Did not show significant cataleptogenic effects even at a dose of 100 mg/kg and had a low risk of extrapyramidal side effects.
分子量

453.96

Formula

C25H21ClFNO2S
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

GPR52 agonist-1 相关分类

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Keywords:

GPR52 agonist-11207965-40-9Othersorally activeblood-brain barrierBBBcAMP accumulationhyperactivityantipsychoticICR miceInhibitorinhibitorinhibit

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