FSL0477

Structure

• InChI=1S/C18H19ClN4/c1-22-8-10-23(11-9-22)18-14-4-2-3-5-15(14)20-16-7-6-13(19)12-17(16)21-18/h2-7,12,20H,8-11H2,1H3
• InChIKey=QZUDBNBUXVUHMW-UHFFFAOYSA-N

Synonyms

• 5786-21-0
• Clozapine

Origin

Chemically synthesized

Biological activities

Dopaminergic activity coupled with a broad spectrum of cholinergic, adrenergic, and sertonerigic activity

Therapeutic

Antipsychotic

Target

Neurotransmitter receptors

Assay information

Dopamiergic activity (K_i [nM]): D1 (189), D2 (431), D3 (646), D4 (39), D5 (235)
Serotonergic activity (K_i [nM]): 5-HT1A (105), 5-HT1B (398), 5-HT1C (110), 5-HT1D (2100), 5-HT1E (966), 5-HT2A (13), 5-HT2B (7.5), 5-HT2C (29), 5-HT3 (241), 5-HT5 (3.8), 5-HT6 (17), 5-HT7 (18)
Adrenergic activity (K_i [nM]): α1A (1.6), α1B (7.0), α2C (142), β1 (>gt; 10000), β2 (>gt; 10000)
Cholinerigic activity (K_i [nM]): M₁ (14), M₂ (204), M₃ (25), M₄ (29), M₅ (94)

References

• Wenthur CJ, Lindsley CW
  Classics in chemical neuroscience: clozapine.
  ACS Chem Neurosci, 4(7): 1018-1025 (2013)  24047509  doi: 10.1021/cn400121z
• Kuoppamäki M, Syvälahti E, Hietala J
  Clozapine and N-desmethylclozapine are potent 5-HT1C receptor antagonists.
  Eur J Pharmacol, 245(2): 179-182 (1993)  8387927
• Jean Schmutz, Fritz Hunziker
  (1970). 11-basic substituted dibenzodiazepines and dibenzothiazepines. US3539573.
• (1963). Procédé de préparation d'amidines de la série des 5-dibenzo-[b,e] [1,4]-diazépines . FR1334944.