hf-1854

Clozapine (HF 1854) is a tricylic dibenzodiazepine, classified as an atypical antipsychotic agent. It binds several types of central nervous system receptors, and displays a unique pharmacological profile. Clozapine is a serotonin antagonist, with strong binding to 5-HT 2A/2C receptor subtype. It also displays strong affinity to several dopaminergic receptors, but shows only weak antagonism at the dopamine D2 receptor, a receptor commonly thought to modulate neuroleptic activity.

Clozapine (HF 1854) dihydrochloride is utilized for researching psychiatric disorders. This compound exhibits high affinity for numerous neuroreceptors and acts as an effective antagonist of dopamine receptors, with a Ki value of 75 nM. Clozapine inhibits the muscarinic M1 receptor and serotonin 5HT2A receptor, with Ki values of 9.5 nM and 4 nM, respectively. Additionally, Clozapine is a selective agonist of the muscarinic M4 receptor (EC50 = 11 nM).

Clozapine-d8 is the deuterium-labeled analog of the antipsychotic compound Clozapine, wherein eight hydrogen atoms have been replaced with the stable isotope deuterium. Like its parent molecule, Clozapine-d8 acts as a selective ligand for the D4-dopamine receptor and the 5HT2 serotonin receptor, making it a valuable internal standard for the quantitative mass spectrometric analysis of Clozapine, which is an atypical antipsychotic used primarily for the research of treatment-resistant schizophrenia and exhibits high affinity for a diverse number of neuroreceptors beyond its primary targets.