The 5-HT1A receptor antagonist (S)-UH-301 blocks the qR)-8-OH-DPAT-induced inhibition of serotonergic dorsal raphe cell firing in the rat.
(S)-UH-301 [(S)-5-fluoro-8-hydroxy-2-(dipropylamino)-tetralin, 0.5-4.0 mg/kg i.v.] did not significantly alter the firing rate of 5-hydroxytryptamine (5-HT) containing neurons in the dorsal raphe nucleus (DRN) as a group, although some individual cells were activated whereas others were depressed. However, (S)-UH-301 (2.0 mg/kg i.v.) consistently reversed the inhibition of DRN-5-HT cells produced by the selective 5-HT1A receptor agonist (R)-8-OH-DPAT (0.5 microgram/kg i.v.) and the dose-response curve for this effect of (R)-8-OH-DPAT was markedly shifted to the right by pretreatment with (S)-UH-301 (1.0 mg/kg i.v.). These results support the notion that (S)-UH-301 acts as an antagonist at central 5-HT1A receptors.
Arborelius
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L
Department of Physiology and Pharmacology, Karolinska Institutet, Stockholm, Sweden.
Höök
B B
BB
Hacksell
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Svensson
T H
TH
D017371:8-Hydroxy-2-(di-n-propylamino)tetralin / Q000031:analogs & derivatives* / Q000037:antagonists & inhibitors* / Q000494:pharmacology; D000200:Action Potentials / Q000187:drug effects; D000818:Animals; D004305:Dose-Response Relationship, Drug; D004594:Electrophysiology; D008297:Male; D009474:Neurons / Q000187:drug effects*; D011903:Raphe Nuclei / Q000166:cytology / Q000187:drug effects*; D051381:Rats; D017207:Rats, Sprague-Dawley; D012701:Serotonin / Q000502:physiology*; D012702:Serotonin Antagonists / Q000494:pharmacology*
D012702:Serotonin Antagonists; C064282:UH 301; D012701:Serotonin; D017371:8-Hydroxy-2-(di-n-propylamino)tetralin