Antidepressive effects of the stereoisomer cis-dosulepin hydrochloride

The central action of cis-dosulepin (CAS 113-53-1) was compared with that of its antidepressant stereoisomer trans-dosulepin, cis-dosulepin exerted weaker anti-reserpine, anti-tetrabenazine, and 3H-5-HT (serotonin) uptake inhibiting actions than trans-dosulepin, but cis-dosulepin's inhibition of 3H-dopamine and 3H-norepinephrine uptake was slightly more potent than that of trans-dosulepin. On the other hand, cis-dosulepin exhibited extremely potent anticholinergic action in oxotremorine induced tremor, isolated ileums and the 3H-quinuclidinyl benzilate binding test. It also showed potent apomorphine enhancing action and shortened the period of immobility in the forced swimming test in animals. The pharmacological profile of cis-dosulepin appears interesting with respect to investigating the mechanism of action of antidepressants.