Lesch K P, Poten B, Söhnle K, Schulte H M
Department of Psychiatry, University of Würzburg, FRG.
Eur J Clin Pharmacol. 1990;39(1):17-9. doi: 10.1007/BF02657050.
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.
选择性5-羟色胺1A受体配体伊沙匹隆（IPS）可使人体出现剂量相关的体温过低。非选择性5-羟色胺1/2受体拮抗剂美替拉酮可减弱该反应，而非选择性β-肾上腺素能受体拮抗剂吲哚洛尔可完全拮抗该反应，吲哚洛尔可与5-羟色胺1A受体发生立体选择性相互作用。选择性β1-肾上腺素能拮抗剂倍他洛尔则无此作用。这些发现表明，IPS诱导的体温过低具体涉及（突触前）5-羟色胺1A受体的激活。因此，对IPS的体温过低反应可能为评估突触前5-羟色胺受体在情感障碍中的功能及其在精神药物作用中的参与情况提供一种便捷的体内范例。
