Clozapine-d₄ is intended for use as an internal standard for the quantification of clozapine (Item Nos. 12059 | 25779) by GC- or LC-MS. Clozapine is a partial agonist at the serotonin (5-HT) receptor subtype 5-HT_1A (K_i = 180 nM).^1,2 It also binds to 5-HT_2A, 5-HT_2C, 5-HT₃, 5-HT₆ and 5-HT₇ receptors (K_is = 3.3, 13, 110, 4, and 21 nM, respectively), as well as the histamine H₁ and α₁-adrenergic receptors (K_is = 2.1 and 23 nM, respectively). It does not bind to the 5-HT_1B receptor and has a lower affinity for dopamine receptors (K_is = 540, 150, and 360 nM for D_1-3, respectively). Clozapine induces the release of glutamate and D-serine, an agonist at the glycine site of the NMDA receptor, from astrocytes, and reduces the expression of astrocytic glutamate transporters.³ It reverses locomotor hyperactivity and deficits in prepulse inhibition of acoustic startle in a rat neonatal ventral hippocampal ibotenic lesion model of schizophrenia when administered at a dose of 2.5 mg/kg per day.⁴ Formulations containing clozapine have been used in the treatment of schizophrenia.

WARNING This product is not for human or veterinary use.