Clorotepine is known to have high affinity for the dopamine D1,[7] D2,[8] D3,[8] and D4 receptors,[8] the serotonin 5-HT2A,[7] 5-HT2B,[9] 5-HT2C,[9] 5-HT6,[10] and 5-HT7 receptors,[10] the α1A-,[11] α1B-,[11] and α1D-adrenergic receptors,[11] and the histamine H1 receptors,[12] 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.[13]