Bioactivity | Clozapine (HF 1854) dihydrochloride 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[1][2][3]. Clozapine is also a potent and selective agonist at the muscarinic M4 receptor (EC50=11 nM)[4]. |
Invitro | 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[1]。 Clozapine (0-1 μM;24 h) 在 HeLa 细胞中下调 5-HT6 并上调 5-HT7 受体[2]。 Clozapine 是 CHO 细胞中表达的毒蕈碱 M4 受体 (EC50=11 nM) 的完全激动剂[4]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> Clozapine dihydrochloride 相关抗体: |
In Vivo | 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[3]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: |
CAS | 2711603-38-0 |
Formula | C18H21Cl3N4 |
Molar Mass | 399.75 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [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. [4]. Zorn SH, et al. Clozapine is a potent and selective muscarinic M4 receptor agonist. Eur J Pharmacol. 1994 Nov 15;269(3):R1-2. |