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.
Nakagawa
T
T
Kaken Pharmaceutical Co., Ltd., Kyoto Research Institute, Japan.
Ukai
K
K
Kubo
S
S
D000109:Acetylcholine / Q000494:pharmacology; D000818:Animals; D000928:Antidepressive Agents / Q000494:pharmacology*; D001058:Apomorphine / Q000494:pharmacology; D001763:Blepharoptosis / Q000517:prevention & control; D001831:Body Temperature / Q000187:drug effects; D001923:Brain Chemistry / Q000187:drug effects; D003342:Corpus Striatum / Q000187:drug effects; D004308:Dothiepin / Q000494:pharmacology*; D006168:Guinea Pigs; D066298:In Vitro Techniques; D051379:Mice; D008813:Mice, Inbred ICR; D009119:Muscle Contraction / Q000187:drug effects; D010095:Oxotremorine / Q000494:pharmacology; D011813:Quinuclidinyl Benzilate; D051381:Rats; D017208:Rats, Wistar; D012110:Reserpine / Q000494:pharmacology; D013237:Stereoisomerism; D013239:Stereotyped Behavior / Q000187:drug effects; D013574:Synaptosomes / Q000187:drug effects; D013747:Tetrabenazine / Q000037:antagonists & inhibitors / Q000494:pharmacology
D000928:Antidepressive Agents; D010095:Oxotremorine; D011813:Quinuclidinyl Benzilate; D012110:Reserpine; D001058:Apomorphine; D000109:Acetylcholine; D004308:Dothiepin; D013747:Tetrabenazine