Switch to
| Predicate | Object |
|---|---|
| rdf:type | |
| lifeskim:mentions | |
| pubmed:issue |
2
|
| pubmed:dateCreated |
1997-2-12
|
| pubmed:abstractText |
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.
|
| pubmed:language |
eng
|
| pubmed:journal | |
| pubmed:citationSubset |
IM
|
| pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Adenylate Cyclase,
http://linkedlifedata.com/resource/pubmed/chemical/Anti-Anxiety Agents,
http://linkedlifedata.com/resource/pubmed/chemical/Benzothiazoles,
http://linkedlifedata.com/resource/pubmed/chemical/Piperidines,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Serotonin,
http://linkedlifedata.com/resource/pubmed/chemical/Serotonin Antagonists,
http://linkedlifedata.com/resource/pubmed/chemical/Thiazoles
|
| pubmed:status |
MEDLINE
|
| pubmed:month |
Jun
|
| pubmed:issn |
0091-3057
|
| pubmed:author | |
| pubmed:issnType |
Print
|
| pubmed:volume |
54
|
| pubmed:owner |
NLM
|
| pubmed:authorsComplete |
Y
|
| pubmed:pagination |
509-16
|
| pubmed:dateRevised |
2006-11-15
|
| pubmed:meshHeading |
pubmed-meshheading:8743616-Adenylate Cyclase,
pubmed-meshheading:8743616-Animals,
pubmed-meshheading:8743616-Anti-Anxiety Agents,
pubmed-meshheading:8743616-Avoidance Learning,
pubmed-meshheading:8743616-Behavior, Animal,
pubmed-meshheading:8743616-Benzothiazoles,
pubmed-meshheading:8743616-Brain Chemistry,
pubmed-meshheading:8743616-Dose-Response Relationship, Drug,
pubmed-meshheading:8743616-Electrophysiology,
pubmed-meshheading:8743616-Male,
pubmed-meshheading:8743616-Mice,
pubmed-meshheading:8743616-Motor Activity,
pubmed-meshheading:8743616-Piperidines,
pubmed-meshheading:8743616-Raphe Nuclei,
pubmed-meshheading:8743616-Rats,
pubmed-meshheading:8743616-Rats, Sprague-Dawley,
pubmed-meshheading:8743616-Receptors, Serotonin,
pubmed-meshheading:8743616-Serotonin Antagonists,
pubmed-meshheading:8743616-Synaptic Transmission,
pubmed-meshheading:8743616-Thiazoles
|
| pubmed:year |
1996
|
| pubmed:articleTitle |
Preclinical profile of the mixed 5-HT1A/5-HT2A receptor antagonist S 21,357.
|
| pubmed:affiliation |
Békésy Laboratory of Neurobiology, John A. Burns School of Medicine, University of Hawaii, Honolulu 96822, USA.
|
| pubmed:publicationType |
Journal Article,
In Vitro
|