2. GPCR/G Protein Neuronal Signaling
  3. Dopamine Receptor mAChR Adrenergic Receptor 5-HT Receptor
  4. Clozapine hydrochloride

Clozapine hydrochloride  (Synonyms: HF 1854 hydrochloride)

目录号: HY-14539A
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Clozapine hydrochloride (HF 1854 hydrochloride) 是用于研究精神分裂症的抗精神病药。Clozapine hydrochloride 对许多神经受体有高度的亲和力，是多巴胺受体的有效拮抗剂，Ki 值为 75 nM。Clozapine hydrochloride 抑制毒蕈碱 M1 受体和血清素 5HT2A 受体，Ki 值分别为 9.5 nM 和 4 nM。Clozapine hydrochloride 也是选择性的毒蕈碱 M4 受体的激动剂 (EC50=11 nM)。

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Clozapine hydrochloride Chemical Structure

Clozapine hydrochloride Chemical Structure

CAS No. : 54241-01-9

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Clozapine hydrochloride 的其他形式现货产品:

Other Forms of Clozapine hydrochloride:

Clozapine hydrochloride 相关抗体

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Dopamine Receptor D1 Receptor D2 Receptor D3 Receptor D4 Receptor D5 Receptor

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mAChR1 mAChR2 mAChR3 mAChR4 mAChR5

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α adrenergic receptor β adrenergic receptor

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5-HT1 Receptor 5-HT2 Receptor 5-HT3 Receptor 5-HT4 Receptor 5-HT5 Receptor 5-HT6 Receptor 5-HT7 Receptor 5-HT Receptor

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  • 参考文献

生物活性

Clozapine hydrochloride (HF 1854 hydrochloride) is an antipsychotic used for the research of schizophrenia. Clozapine hydrochloride has high affinity for a number of neuroreceptors. Clozapine hydrochloride is a potent antagonist of dopamine D2 with a Ki of 75 nM. Clozapine hydrochloride inhibits the muscarinic M1 receptor and serotonin 5HT2A receptor with Kis of 9.5 nM and 4 nM, respectively[1][2][3]. Clozapine hydrochloride is also a potent and selective agonist at the muscarinic M4 receptor (EC50=11 nM)[4].

IC50 & Target

5-HT2A Receptor

4 nM (Ki)

5-HT6 Receptor

 

Human 5-HT7 Receptor

 

mAChR1

9.5 nM (Ki)

mAChR4

11 nM (EC50)

α2-adrenergic receptor

51 nM (Ki)

D2 Receptor

75 nM (Ki)

体内研究
(In Vivo)

Clozapine hydrochloride (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[3]。

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

Animal Model: Male 129 S6/Sv mice, lysergic acid diethylamide (LSD)-induced psychosis model[3]
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.
分子量

363.28

Formula

C18H20Cl2N4
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

Clozapine hydrochloride 相关分类

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Clozapine54241-01-9HF 1854HF1854HF-1854Dopamine ReceptormAChRAdrenergic Receptor5-HT ReceptorMuscarinic acetylcholine receptorBeta ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorantipsychoticschizophreniaHeLapsychosisInhibitorinhibitorinhibit

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