标签归档：clozapine

Clozapine；氯氮平

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Clozapine；氯氮平

货号：
IC1530

品牌：
Jinpan

Clozapine；氯氮平

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产品简介
MDL MFCD00153785
EC EINECS 227-313-7
别名 Iprox;Azaleptine
英文名称 Clozapine
CAS 5786-21-0
分子式 C18H19ClN4
分子量 326.83
纯度 HPLC≥98%
单位 支
生物活性 Clozapine (HF 1854) 是用于治疗精神分裂症的抗精神病药。氯氮平是多巴胺和许多其他受体的有效拮抗剂，结合M1受体的Ki值为9.5 nM。[1-3]
IC50 Ki: 9.5 nM (M1), 51 nM (α2-adrenoceptor), 75 nM (D2)[1]
In Vitro 氯氮平显示出具有抗精神病作用但不具有帕金森样运动副作用的独特性质。氯氮平的化学结构促进了与D2受体的相对快速的解离。在短期占据D2受体后，峰值神经活动会引起突触多巴胺，然后取代氯氮平。虽然氯氮平也占据其他类型的受体，但它们在预防帕金森病方面可能没有显著作用。氯氮平对D2受体非常有效，Ki为75 nM。氯氮平对α2-肾上腺素能受体也有效，Ki值为51 nM [1]。氯氮平导致5-HT2A受体的反常下调。氯氮平还与高度亲和力的5-HT6和5-HT7受体结合[2]。
In Vivo 慢性氯氮平后1天，7天和14天，头部抽搐反应降低，[3H]酮色林结合下调。慢性氯氮平后1天，5-HT2A mRNA减少。在慢性氯氮平[3]后7天，拯救c-fos而非egr-1和egr-2的诱导。
SMILES CN1CCN(CC1)C2=NC3=CC(Cl)=CC=C3NC4=CC=CC=C42
靶点 5-HT2;Dopamine Receptor
动物实验 小鼠：用25mg/kg /天氯氮平长期治疗小鼠（21天）。在最后一次氯氮平给药后1,7,14和21天进行实验。 [3H]在小鼠躯体感觉皮层中测定酮色林结合和5-HT2A mRNA表达。测定头痉挛行为，由所有5-HT2A激动剂诱导的c-fos表达，以及LSD样特异性的egr-1和egr-2的表达[3]。
数据来源文献 [1]. Seeman P, et al. Clozapine, a fast-off-D2 antipsychotic. ACS Chem Neurosci. 2014 Jan 15;5(1):24-9.

[2]. Zhukovskaya NL, et al. Clozapine downregulates 5-hydroxytryptamine6 (5-HT6) and upregulates 5-HT7 receptors in HeLa cells. Neurosci Lett. 2000 Jul 21;288(3):236-40.

[3]. Moreno JL, et al. Persistent effects of chronic clozapine on the cellular and behavioral responses to LSD in mice. Psychopharmacology (Berl). 2013 Jan;225(1):217-26
规格 100mg 10mM*1mL in DMSO 200mg 500mg

是多巴胺和许多其他受体的有效拮抗剂。

Clozapine N-oxide BML-NS105 (1)

发表于由

Clozapine N-oxide BML-NS105 (1)

Clozapine N-oxide  BML-NS105  

氯氮平主要代谢物

纯度≥99% (HPLC)，适用于体内和体外实验。

外观：黄色固体

可溶性：可溶于水，溶解度为5mg/ml。

稳定性：液体-20度能够保持4个月。


参考文献：

Activation and inhibition of transient receptor potential TRPM3-induced gene transcription: A. Lesch, et al. ; Br. J. Pharmacol.171, 2645 (2014), Abstract;

Chemogenetic silencing of neurons in retrosplenial cortex disrupts sensory preconditioning: S. Robinson, et al.; J. Neurosci. 34, 10982 (2014), Abstract;

CREB Regulates Memory Allocation in the Insular Cortex: Y. Sano, et al.; Curr. Biol. 24, 2833 (2014), Abstract;

Cyclin-Dependent Kinase 5 in the Ventral Tegmental Area Regulates Depression-Related Behaviors: P. Zhong, et al.; J. Neurosci. 34, 6352 (2014), Abstract; Full Text

Direct excitation of parvalbumin-positive interneurons by M1 muscarinic acetylcholine receptors: roles in cellular excitability, inhibitory transmission and cognition: F. Yi, et al.; J. Physiol. 592, 3463 (2014), Abstract;

Muscarinic excitation of parvalbumin-positive interneurons contributes to the severity of pilocarpine-induced seizures: F. Yi, et al.; Epilepsia (2014), Abstract;

Regulation of immediate-early gene transcription following activation of Gα(q)-coupled designer receptors: A. Kaufmann, et al.; J. Cell. Biochem. 114, 681 (2013), Abstract;

Developing chemical genetic approaches to explore G protein-coupled receptor function: validation of the use of a receptor activated solely by synthetic ligand (RASSL): E. Alvarez-Curto, et al.; Mol. Pharmacol. 80, 1033 (2011), Abstract; Full Text

Small molecule inhibitors of the Candida albicans budded-to-hyphal transition act through multiple signaling pathways: J. Midkiff, et al.; PLoS One 6, e25395 (2011), Abstract; Full Text

Binding of typical and atypical antipsychotic agents to 5-hydroxytryptamine-6 and 5-hydroxytryptamine-7 receptors: B.L. Roth, et al.; J. Pharmacol. Exp. Ther. 268, 1403 (1994), Abstract;

Decomposition of clozapine N-oxide in the qualitative and quantitative analysis of clozapine and its metabolites: G. Lin, etal.; J. Pharm. Sci. 83, 1412 (1994), Abstract;

Clozapine N-oxide BML-NS105

发表于由

Clozapine N-oxide BML-NS105

Clozapine N-oxide  BML-NS105  

氯氮平主要代谢物

纯度≥99% (HPLC)，适用于体内和体外实验。

外观：黄色固体

可溶性：可溶于水，溶解度为5mg/ml。

稳定性：液体-20度能够保持4个月。


参考文献：

Activation and inhibition of transient receptor potential TRPM3-induced gene transcription: A. Lesch, et al. ; Br. J. Pharmacol.171, 2645 (2014), Abstract;

Chemogenetic silencing of neurons in retrosplenial cortex disrupts sensory preconditioning: S. Robinson, et al.; J. Neurosci. 34, 10982 (2014), Abstract;

CREB Regulates Memory Allocation in the Insular Cortex: Y. Sano, et al.; Curr. Biol. 24, 2833 (2014), Abstract;

Cyclin-Dependent Kinase 5 in the Ventral Tegmental Area Regulates Depression-Related Behaviors: P. Zhong, et al.; J. Neurosci. 34, 6352 (2014), Abstract; Full Text

Direct excitation of parvalbumin-positive interneurons by M1 muscarinic acetylcholine receptors: roles in cellular excitability, inhibitory transmission and cognition: F. Yi, et al.; J. Physiol. 592, 3463 (2014), Abstract;

Muscarinic excitation of parvalbumin-positive interneurons contributes to the severity of pilocarpine-induced seizures: F. Yi, et al.; Epilepsia (2014), Abstract;

Regulation of immediate-early gene transcription following activation of Gα(q)-coupled designer receptors: A. Kaufmann, et al.; J. Cell. Biochem. 114, 681 (2013), Abstract;

Developing chemical genetic approaches to explore G protein-coupled receptor function: validation of the use of a receptor activated solely by synthetic ligand (RASSL): E. Alvarez-Curto, et al.; Mol. Pharmacol. 80, 1033 (2011), Abstract; Full Text

Small molecule inhibitors of the Candida albicans budded-to-hyphal transition act through multiple signaling pathways: J. Midkiff, et al.; PLoS One 6, e25395 (2011), Abstract; Full Text

Binding of typical and atypical antipsychotic agents to 5-hydroxytryptamine-6 and 5-hydroxytryptamine-7 receptors: B.L. Roth, et al.; J. Pharmacol. Exp. Ther. 268, 1403 (1994), Abstract;

Decomposition of clozapine N-oxide in the qualitative and quantitative analysis of clozapine and its metabolites: G. Lin, etal.; J. Pharm. Sci. 83, 1412 (1994), Abstract;