Clozapine
Clozapine is an atypical antipsychotic that also exhibits some immunosuppressive activity. Clozapine is clinically used to treat mood disorders. Clozapine binds Kv1.1 channels, prolonging the QT interval and also causes granulocytosis, limiting its clinical use. Clozapine acts as an antagonist at M1/2/3/5 muscarinic acetylcholine receptors (mAChRs) and D2 receptors, a partial agonist at 5-HT1A receptors, and as a full agonist at M4 mAChRs. Additionally, clozapine binds 5-HT2/3/6/7 receptors, D4 receptors, α1/2 adrenergic receptors, and histamine H1 receptors. Clozapine also potentiates GABAergic neurotransmission.
References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18852857
| Cas No. |
5786-21-0 |
|---|---|
| Purity |
≥97% |
| Formula |
C18H19ClN4 |
| Formula Wt. |
326.82 |
| Chemical Name |
8-chloro-11-(4-methyl-1-piperazinyl)-5H-Dibenzo(b,e)(1,4)diazepine |
| IUPAC Name |
3-chloro-6-(4-methylpiperazin-1-yl)-5H-benzo[b][1,4]benzodiazepine |
| Synonym |
Clozaril, Leponex |
| Melting Point |
183-184°C |
| Solubility |
Soluble in DMSO or dilute aqueous acid. |
| Appearance |
Yellow crystalline powder |
Hill AP, Perrin MJ, Heide J, et al. Kinetics of drug interaction with the Kv11.1 potassium channel. Mol Pharmacol. 2014 May;85(5):769-76. PMID: 24586056.
Tanahashi S, Yamamura S, Nakagawa M, et al. Clozapine, but not haloperidol, enhances glial D-serine and L-glutamate release in rat frontal cortex and primary cultured astrocytes. Br J Pharmacol. 2012 Mar;165(5):1543-55. PMID: 21880034.
Wu Y, Blichowski M, Daskalakis ZJ, et al. Evidence that clozapine directly interacts on the GABAB receptor. Neuroreport. 2011 Sep 14;22(13):637-41. PMID: 21753741.
Nord M, Farde L. Antipsychotic occupancy of dopamine receptors in schizophrenia. CNS Neurosci Ther. 2011 Apr;17(2):97-103. PMID: 21143431.
Alvir JM, Lieberman JA, Safferman AZ, et al. Clozapine-induced agranulocytosis. Incidence and risk factors in the United States. N Engl J Med. 1993 Jul 15;329(3):162-7. PMID: 8515788.
