产品
编 号：F620786
分子式：C17H19Cl2F5N4
分子量：445.26
分子式：C17H19Cl2F5N4
分子量：445.26
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
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5mg
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10mg
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25mg
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50mg
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100mg
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结构图
CAS No: 2108806-02-4
产品详情
生物活性：
JNJ-37822681 dihydrochloride is a potent, specific, centrally active, fast-dissociating dopamine D2 receptor antagonist with a moderate binding affinity for the dopamine D2L receptor (Ki =158 nM), which has potential for the treatment of schizophrenia and bipolar disorder.
体内研究：
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; once
Result: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; once
Result:Increased prolactin release in a dose-dependent manner.
JNJ-37822681 dihydrochloride is a potent, specific, centrally active, fast-dissociating dopamine D2 receptor antagonist with a moderate binding affinity for the dopamine D2L receptor (Ki =158 nM), which has potential for the treatment of schizophrenia and bipolar disorder.
体内研究：
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; once
Result: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; once
Result:Increased prolactin release in a dose-dependent manner.
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