Participation of opioid mechanism in the antinociceptive effects induced by oxaprotiline enantiomers in mice.

The purpose of the present study was to assess the activity of (+)-oxaprotiline [(+)-OXA] (a noradrenaline uptake inhibitor) and (-)-oxaprotiline [(-)-OXA] (with unknown mechanism of action) in two experimental models of pain in mice, a hot plate test and a writhing syndrome induced by phenylbenzoquinone (PHBQ), and to determine whether the opioidergic system may be engaged in their antinociceptive effects. Morphine was used as a reference drug. Administration of (+)-OXA (0.

9-substituted 1,2,3,4-tetrahydro-beta-carbolin-1-ones, new 5-HT1A and 5-HT2A receptor ligands.

Three series of new 9-substituted 1,2,3,4-tetrahydro-beta-carbolin-1-ones with 2-, 3- and 4-membered alkyl chain (1, 2 and 3, respectively) were synthesized, and the effect of some structural modifications on their 5-HT1A and 5-HT2A receptor affinities and functional in vivo properties was discussed. Radioligand binding measurements showed that the majority of compounds had a distinct affinity for 5-HT1A (1b, 2a, 2b, 2c, 3b; Ki = 0.3-64 nM) and 5-HT2A receptors (1b, 2b, 2c, 3b; Ki = 0.

On the bioactive conformation of NAN-190 (1) and MP3022 (2), 5-HT(1A) receptor antagonists.

Structural modifications of 1, a postsynaptic 5-HT(1A) receptor antagonist, provided its flexible (8, 12) and rigid (7, 9, 11, 13) analogues. Compounds 7, 8, 9, and 11 showed high 5-HT(1A) receptor affinity (K(i) = 4-72 nM). They acted as 5-HT(1A) postsynaptic receptor antagonists, since, like 1, they inhibited the behavioral syndrome, i.

[A case of hydatidiform mole with an unclear clinical picture].

The authors presented the case of hydatidiform mole with unclear clinical picture. They discussed clinical difficulties in the diagnosing of that lesion, and stressed the role of US method in establishing the specific final diagnosis.