Laude D, Baudrie V, Martin G R, Chaouloff F
Laboratoire de Pharmacologie, CNRS, CHU Necker-EM, Paris, France.
Naunyn Schmiedebergs Arch Pharmacol. 1990 Oct;342(4):378-81. doi: 10.1007/BF00169452.
Recent results have indicated that the 5-HT1A receptor subtype mediates the adrenaline-releasing and hyperglycemic effects of 8-hydroxy-2-(di-n-propylamino)tetralin in the rat. The aim of this study was to analyse, by means of the peripherally acting 5-HT1A receptor agonist, N,N-dipropyl-5-carboxamidotryptamine (DP-5-CT), whether these 5-HT1A receptors are peripherally or centrally localised. In view of the appreciable affinity of DP-5-CT for the 5-HT1D receptor subtype, the effects of the mixed 5-HT1B/5-HT1D receptor agonist 7-trifluoromethyl-4-(4-methyl-1-piperazinyl)-pyrrolo(1,2-a)quinoxaline (CGS 12066B), and the mixed 5-HT1A/5-HT1B/5-HT1D receptor agonist 5-methoxy-3(1,2,3,6-tetrahydropyridine-4-yl)1H-indole (RU 24969) were also investigated. Administration of DP-5-CT (0.3 and 1 mg/kg i.v.) increased plasma glucose levels dose-dependently, whereas only the 1 mg/kg dose of DP-5-CT elicited a rise in plasma adrenaline levels. In contrast, CGS 12066B (1.5 and 4.5 mg/kg i.v.) did not affect either plasma adrenaline or plasma glucose levels. Administration of RU 24969 (0.5-4.5 mg/kg i.v.) increased dose-dependently both plasma adrenaline and glucose levels. The data suggest that central 5-HT1A receptors, but neither 5-HT1B nor 5-HT1D receptors, regulate plasma adrenaline and glucose levels.
近期研究结果表明，5-羟色胺1A（5-HT1A）受体亚型介导了8-羟基-2-（二正丙基氨基）四氢萘对大鼠的肾上腺素释放及血糖升高作用。本研究旨在通过外周作用的5-HT1A受体激动剂N,N-二丙基-5-羧酰胺色胺（DP-5-CT）分析这些5-HT1A受体是定位于外周还是中枢。鉴于DP-5-CT对5-羟色胺1D（5-HT1D）受体亚型有明显亲和力，还研究了5-HT1B/5-HT1D混合型受体激动剂7-三氟甲基-4-（4-甲基-1-哌嗪基）-吡咯并（1,2-a）喹喔啉（CGS 12066B）以及5-HT1A/5-HT1B/5-HT1D混合型受体激动剂5-甲氧基-3（1,2,3,6-四氢吡啶-4-基）1H-吲哚（RU 24969）的作用。静脉注射DP-5-CT（0.3和1毫克/千克）可使血浆葡萄糖水平呈剂量依赖性升高，而只有1毫克/千克剂量的DP-5-CT能引起血浆肾上腺素水平升高。相比之下，CGS 12066B（1.5和4.5毫克/千克静脉注射）对血浆肾上腺素或血浆葡萄糖水平均无影响。静脉注射RU 24969（0.5 - 4.5毫克/千克）可使血浆肾上腺素和葡萄糖水平均呈剂量依赖性升高。数据表明，中枢5-HT1A受体而非5-HT1B或5-HT1D受体调节血浆肾上腺素和葡萄糖水平。
