Clozapine

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[1][2][3]. Clozapine is also a potent and selective agonist at the muscarinic M4 receptor (EC50=11 nM) [4].

Product Specifications

CAS Number

[5786-21-0]

Product Name Alternative

HF 1854

UNSPSC

12352005

Hazard Statement

H301, H341, H361

Target

5-HT Receptor; Adrenergic Receptor; Dopamine Receptor; mAChR

Type

Reference compound

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

Neuroscience-Neurodegeneration

Field of Research

Neurological Disease; Cancer

Assay Protocol

https://www.medchemexpress.com/Clozapine.html

Concentration

10mM

Purity

99.84

Solubility

DMSO : 50 mg/mL (ultrasonic)

Smiles

CN1CCN(CC1)C2=NC3=CC(Cl)=CC=C3NC4=CC=CC=C42

Molecular Formula

C18H19ClN4

Molecular Weight

326.83

Precautions

H301, H341, H361

References & Citations

[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.