Clorotepine ( ; brand names INN Clotepin, Clopiben), also known as octoclothepin or octoclothepine, is an antipsychotic of the tricyclic group which was derived from perathiepin in 1965 and marketed in the Czech Republic by Spofa in or around 1971 for the treatment of schizophrenic psychosis.     
Clorotepine is known to have high
affinity for the dopamine D, 1  D, 2  D, 3 and  D, 4 receptors the  serotonin 5-HT, 2A  5-HT, 2B  5-HT, 2C  5-HT, 6 and  5-HT, 7 receptors the  α, 1A-  α, 1B- and  α, 1D-adrenergic receptors and the  histamine H 1 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 D
2 receptor, along with tefludazine, clorotepine was used as the basis for developing a 3-dimensional (3D) pharmacophore for D 2 receptor antagonists.
See also [ edit ]
References [ edit ]
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