Octoclothepin (Clorotepine) is a D 2 dopamine receptor antagonist and 5-HT 2 serotonin receptor antagonist, with K i values of 0.67 nM, 0.57 nM, and 0.19 nM for the dopamine D 2, 5-HT 2A, and 5-HT 2C receptors, respectively. Octoclothepin also binds to adrenergic receptors, with K i values of 0.66 nM, 0.56 nM, and 0.77 nM for α 1a, α 1b, and α 1d, respectively. Octoclothepin can be used in schizophrenia research [1].
In Vitro, Octoclothepin (Compound 8) binds with subnanomolar to nanomolar affinity to bovine α1a-, hamster α1b-, rat α1d-adrenoceptors, human D2, human 5-HT2A, and human 5-HT2C receptors,, with Ki values of 0.66 nM, 0.56 nM, 0.77 nM, 0.67 nM, 0.57 nM, and 0.19 nM, respectively[1].
References:
[1]. Helia O, et al. Reduction of octoclothepine-N-oxide by rat liver microsomes. Eur J Drug Metab Pharmacokinet. 1981;6(2):155-8.
[2]. Roth BL, et al. Binding of typical and atypical antipsychotic agents to 5-hydroxytryptamine-6 and 5-hydroxytryptamine-7 receptors. J Pharmacol Exp Ther. 1994 Mar;268(3):1403-10.
In Vitro, Octoclothepin (Compound 8) binds with subnanomolar to nanomolar affinity to bovine α1a-, hamster α1b-, rat α1d-adrenoceptors, human D2, human 5-HT2A, and human 5-HT2C receptors,, with Ki values of 0.66 nM, 0.56 nM, 0.77 nM, 0.67 nM, 0.57 nM, and 0.19 nM, respectively[1].
References:
[1]. Helia O, et al. Reduction of octoclothepine-N-oxide by rat liver microsomes. Eur J Drug Metab Pharmacokinet. 1981;6(2):155-8.
[2]. Roth BL, et al. Binding of typical and atypical antipsychotic agents to 5-hydroxytryptamine-6 and 5-hydroxytryptamine-7 receptors. J Pharmacol Exp Ther. 1994 Mar;268(3):1403-10.