Clorotepine

Clorotepine (INN; brand names Clotepin, Clopiben), also known as octoclothepin or octoclothepine, is a very potent atypical antipsychotic and central depressant of the tricyclic series which was derived from perathiepin in 1965 and soon thereafter marketed in the Czech Republic by Spofa for the treatment of schizophrenic psychosis. It is known to have high affinity for the D₁, D₂, D₃, D₄, 5-HT_2A, 5-HT_2B, 5-HT_2C, 5-HT₆, 5-HT₇, α_1A-adrenergic, α_1B-adrenergic, α_1D-adrenergic, and H₁ receptors, where it has been it has been confirmed to act as an antagonist (or inverse agonist) at most sites (and likely is as such at all of them based on structure-activity relationships), and it also blocks the reuptake of norepinephrine via inhibition of the norepinephrine transporter. Due to its very potent activity at the D₂ receptor, along with tefludazine, clorotepine was used as the basis for developing a 3-dimensional (3D) pharmacophore for D₂ receptor antagonists.