Pharmacological effects of oxaprotiline enantiomers on the central serotonin system.
The study examined the effect of both oxaprotiline (OXA) enantiomers on the serotonin system in rats and mice. (+)-OXA and (-)-OXA partly inhibit the behavioral syndrome induced by 8-OH-DPAT and 5-methoxy-dimethyltryptamine (5-MeODMT) in normal and reserpinized rats. Imipramine and desipramine produced a similar but less potent effect. (+)-OXA and, to a lesser extent, (-)-OXA antagonized the m-chlorophenylpiperazine (m-CPP)-induced hypothermia in mice. Imipramine and desipramine produced no such effect. (+)-OXA attenuated the head-twitch response to L-5-HTP in mice, but (-)-OXA has no such action. Neither enantiomer inhibited the fenfluramine-induced hyperthermia in rats nor antagonized m-CPP-induced stimulation of hind limb flexor reflex of spinal rat. The obtained results indicate that both enantiomers may have a 5-HT1B-antagonistic action and a less potent 5-HT1A-antagonistic one; on the other hand, they shown no 5-HT2-antagonistic activity.
Maj
J
J
Institute of Pharmacology Polish Academy of Sciences, Kraków.
Dereń
A
A
Moryl
E
E
D006916:5-Hydroxytryptophan / Q000494:pharmacology; D017371:8-Hydroxy-2-(di-n-propylamino)tetralin; D000818:Animals; D000873:Anthracenes / Q000494:pharmacology*; D000928:Antidepressive Agents / Q000494:pharmacology*; D001522:Behavior, Animal / Q000187:drug effects; D001831:Body Temperature / Q000187:drug effects; D002490:Central Nervous System / Q000187:drug effects*; D005277:Fenfluramine / Q000494:pharmacology; D008297:Male; D008376:Maprotiline / Q000031:analogs & derivatives / Q000494:pharmacology*; D008732:Methoxydimethyltryptamines / Q000494:pharmacology; D051379:Mice; D010879:Piperazines / Q000494:pharmacology; D051381:Rats; D011919:Rats, Inbred Strains; D011985:Receptors, Serotonin / Q000187:drug effects; D012110:Reserpine / Q000494:pharmacology; D012701:Serotonin / Q000502:physiology*; D013237:Stereoisomerism; D013764:Tetrahydronaphthalenes / Q000494:pharmacology
D000873:Anthracenes; D000928:Antidepressive Agents; D008732:Methoxydimethyltryptamines; D010879:Piperazines; D011985:Receptors, Serotonin; D013764:Tetrahydronaphthalenes; D005277:Fenfluramine; D008376:Maprotiline; D012701:Serotonin; C027299:hydroxymaprotilin; D017371:8-Hydroxy-2-(di-n-propylamino)tetralin; D012110:Reserpine; D006916:5-Hydroxytryptophan; C015068:1-(3-chlorophenyl)piperazine