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Chlorprothixene (hydrochloride) is an antagonist of dopamine receptor and histamine receptors [1]. Chlorprothixene is also an inhibitor of GABAA receptor [2]. All of these three receptors are implicated in many neurological processes, including motivation, pleasure, cognition, memory and learning.

In vitro: Chlorprothixene exihibited strong binding affinities to dopamine and histamine receptors, The Ki values of D1, D2, D3, D5 and H1 were 18nM, 2.96 nM, 4.56 nM, 9 nM and 3.75 nM, respectively. Chlorprothixene showed little affinity to H3 with the Ki value of >1000 nM[1]. In COS-7 cells transiently expressed rat 5-HT7 receptors and HEK-293 cells stably transfected with rat 5-HT6, the Ki values of chlorprothixene were 5.6 nM and 3 nM, respectively [3]. In Vero 76 cells, chlorprothixene treatment inhibited SARS-CoV replication, with IC50 of 16.7 μM for Urbani strain, 13.0 μM for Frankfurt-1, 18.5 μM for CHUK-W1 and 15.8 μM for Toronto-2 [4].

In vivo: In rat brain depressing the release of hypothalamic and hypophyseal hormones, chlorprothixene blocked postsynaptic mesolimbic dopaminergic D1 and D2 receptors [5]. Chlorprothixene treatment restored normal ceramide concentrations in murine bronchial epithelial cells, reduced inflammation in the lungs of mice with cystic fibrosis (CF) and prevented infection with Pseudomonas aeruginosa [6].

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