Pharmacology of the hypothermic response to 5-HT1A receptor activation in humans.
The selective 5-HT1A receptor ligand ipsapirone (IPS) caused dose-related hypothermia in humans. The response was attenuated by the nonselective 5-HT1/2 receptor antagonist metergoline and was completely antagonized by the nonselective beta-adrenoceptor antagonist pindolol, which interacts stereoselectively with the 5-HT1A receptor. The selective beta 1-adrenergic antagonist betaxolol had no effect. The findings indicate that IPS-induced hypothermia specifically involves activation of (presynaptic) 5-HT1A receptors. Therefore, the hypothermic response to IPS may provide a convenient in vivo paradigma to assess the function of the presynaptic 5-HT receptor in affective disorders and its involvement in the effects of psychotropic drugs.
Lesch
K P
KP
Department of Psychiatry, University of Würzburg, FRG.
Poten
B
B
Söhnle
K
K
Schulte
H M
HM
D000319:Adrenergic beta-Antagonists / Q000494:pharmacology; D000328:Adult; D015784:Betaxolol / Q000494:pharmacology; D001831:Body Temperature / Q000187:drug effects*; D004305:Dose-Response Relationship, Drug; D005260:Female; D006801:Humans; D008297:Male; D008711:Metergoline / Q000494:pharmacology; D010869:Pindolol / Q000494:pharmacology; D011743:Pyrimidines / Q000494:pharmacology; D011985:Receptors, Serotonin / Q000187:drug effects* / Q000502:physiology; D012702:Serotonin Antagonists / Q000494:pharmacology
D000319:Adrenergic beta-Antagonists; D011743:Pyrimidines; D011985:Receptors, Serotonin; D012702:Serotonin Antagonists; D008711:Metergoline; C043077:ipsapirone; D010869:Pindolol; D015784:Betaxolol