产品
编 号：F395631
分子式：C18H19ClN4
分子量：326.82
分子式：C18H19ClN4
分子量：326.82
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50mg
640
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100mg
976
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CAS No: 5786-21-0
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生物活性：
Clozapine (HF 1854) is an antipsychotic used for the research of schizophrenia. Clozapine has high affinity for a number of neuroreceptors. Clozapine is a potent antagonist of dopamine D2 with a Ki of 75 nM. Clozapine inhibits the muscarinic M1 receptor and serotonin 5HT2A receptor with Kis of 9.5 nM and 4 nM, respectively. Clozapine is also a potent and selective agonist at the muscarinic M4 receptor (EC50=11 nM).
体内研究：
Clozapine (HF 1854) (25 mg/kg/天；腹腔注射；21 天) 在麦角酸二乙胺诱导的精神病小鼠模型中显示出抗精神病作用。Animal Model:Male 129 S6/Sv mice, lysergic acid diethylamide (LSD)-induced psychosis model
Dosage:25 mg/kg/day
Administration:Intraperitoneal injection, 21 days
Result:Decreased head-twitch response, reduced 5-HT2A mRNA, rescued induction of c-fos, but not egr-1 and egr-2.
体外研究：
Clozapine (HF 1854) 是一种 D2 受体拮抗剂，Ki 为 75 nM，阻断血清素 5HT2A 受体，Ki 为 4 nM，抑制毒蕈碱 M1 受体Ki 为 9.5 nM，阻断 α2-肾上腺素受体，Ki 值为 51 nM。 Clozapine (0-1 μM；24 h) 在 HeLa 细胞中下调 5-HT6 并上调 5-HT7 受体。 Clozapine 是 CHO 细胞中表达的毒蕈碱 M4 受体 (EC50=11 nM) 的完全激动剂。
Clozapine (HF 1854) is an antipsychotic used for the research of schizophrenia. Clozapine has high affinity for a number of neuroreceptors. Clozapine is a potent antagonist of dopamine D2 with a Ki of 75 nM. Clozapine inhibits the muscarinic M1 receptor and serotonin 5HT2A receptor with Kis of 9.5 nM and 4 nM, respectively. Clozapine is also a potent and selective agonist at the muscarinic M4 receptor (EC50=11 nM).
体内研究：
Clozapine (HF 1854) (25 mg/kg/天；腹腔注射；21 天) 在麦角酸二乙胺诱导的精神病小鼠模型中显示出抗精神病作用。Animal Model:Male 129 S6/Sv mice, lysergic acid diethylamide (LSD)-induced psychosis model
Dosage:25 mg/kg/day
Administration:Intraperitoneal injection, 21 days
Result:Decreased head-twitch response, reduced 5-HT2A mRNA, rescued induction of c-fos, but not egr-1 and egr-2.
体外研究：
Clozapine (HF 1854) 是一种 D2 受体拮抗剂，Ki 为 75 nM，阻断血清素 5HT2A 受体，Ki 为 4 nM，抑制毒蕈碱 M1 受体Ki 为 9.5 nM，阻断 α2-肾上腺素受体，Ki 值为 51 nM。 Clozapine (0-1 μM；24 h) 在 HeLa 细胞中下调 5-HT6 并上调 5-HT7 受体。 Clozapine 是 CHO 细胞中表达的毒蕈碱 M4 受体 (EC50=11 nM) 的完全激动剂。
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