JNJ-37822681 dihydrochloride

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

JNJ-37822681二盐酸盐是一种新型、高选择性的多巴胺D2受体拮抗剂。

JNJ-37822681 dihydrochloride is a novel, highly selective dopamine D? receptor antagonist characterized by a rapid dissociation rate from the dopamine D? receptor. JNJ-37822681 dihydrochloride shows a moderate binding affinity for the dopamine D2L receptor with a Ki of 158 nM.(In Vivo):JNJ-37822681 dihydrochloride occupied D2 receptors in rat brain at relatively low doses (ED50 = 0.39 mg/kg) and was effective in animal models of psychosis (e.g., inhibition of apomorphine-induced stereotypy or D-amphetamine/phencyclidine-induced hyperlocomotion).

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JNJ-37822681 (0.0025-40 mg/kg; i.h.; once) blocks D2 receptors in rat brain at relatively low doses with an ED50 value of 0.39 mg/kg and has effective in animal models of psychosis.JNJ-37822681 (0.01-2.5 mg/kg; i.h.; once) induces minimal prolactin release at the lowest doses required for central D2 receptor blockade. Animal Model:Female Sprague-Dawley rats with apomorphine-induced, d-amphetamine-induced, or phencyclidine-induced Dosage:0.0025-40 mg/kg Administration:Subcutaneous injection; onceResult:Inhibited of D-amphetamine-induced hyperlocomotion with an ED50 value of 1.0 mg/kg.Inhibited of apomorphine-induced stereotypy with an ED50 value of 0.19 mg/kg.Inhibited of phencyclidine-induced hyperlocomotion with an ED50 value of 4.7 mg/kg.Animal Model:Female Sprague-Dawley rats Dosage:0.01, 0.02, 0.04, 0.08, 0.16, 0.31, 0.63, 1.25, and 2.5 mg/kg Administration:Subcutaneous injection; onceResult:Increased prolactin release in a dose-dependent manner.

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GPCR/G Protein

Dopamine Receptor

HBV

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2108806-02-4

445.26

C17H19Cl2F5N4

>98% (HPLC)

In Vitro:?DMSO : 33.33 mg/mL (74.86 mM)

Cl.Cl.Fc1ccc(CN2CCC(CC2)Nc2ccc(nn2)C(F)(F)F)cc1F

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(-20℃)

With Ice Pack

≥ 2 years