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• W1968406619 endingPage "516" @default.
• W1968406619 startingPage "509" @default.
• W1968406619 abstract "This study evaluated the pharmacological and behavioral effects of S 21,357, a drug with high affinity for both 5-HT1A and 5-HT2A receptors. The drug behaved as antagonist at both 5-HT1A autoreceptors and postsynaptic 5-HT1A receptors, as it prevented the inhibitory effect of lesopitron on the electrical discharge of the dorsal raphé nucleus (DRN) 5-HT neurons and the activity of forskolin-stimulated adenylate cyclase in hippocampal homogenates. In addition, S 21,357 (4 and 128 mg/kg, PO) inhibited 5-HTP-induced head-twitch responses in mice, indicating that it possesses 5-HT2A antagonistic properties. In a test battery designed to assess defensive behaviors of Swiss-Webster mice to the presence of, or situations associated with, a natural threat stimulus (i.e., rat), S 21,357 (0.12-2 mg/kg, IP) reduced contextual defense reactions after the rat was removed, risk assessment activities when the subject was chased, and finally, defensive attack behavior. These behavioral changes are consistent with fear/anxiety reduction. Furthermore, the drug strongly reduced flight reactions in response to the approaching rat. This last finding, taken together with recent results with panic-modulating drugs, suggest that S 21,357 may have potential efficacy against panic attack. Finally, our results suggest that compounds sharing high affinities for both 5-HT1A and 5-HT2A receptors may directly or synergistically increase the range of defensive behaviors affected." @default.
• W1968406619 created "2016-06-24" @default.
• W1968406619 creator A5001950169 @default.
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• W1968406619 date "1996-05-01" @default.
• W1968406619 modified "2023-10-17" @default.
• W1968406619 title "Preclinical profile of the mixed 5-HT1A/5-HT2A receptor antagonist S 21357" @default.
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• W1968406619 doi "https://doi.org/10.1016/0091-3057(95)02215-5" @default.
• W1968406619 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/8743616" @default.
• W1968406619 hasPublicationYear "1996" @default.
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