Chaouloff F, Baudrie V, Coupry I
Laboratoire de Pharmacologie, Groupe de Neuropharmacologie, CNRS, CHU Necker, Paris, France.
Eur J Pharmacol. 1993 Nov 2;249(1):117-20. doi: 10.1016/0014-2999(93)90670-d.
Numerous studies have brought evidence for reciprocal relationships between glucocorticoids and 5-HT2 receptors; however, whether glucocorticoids affect 5-HT2 receptor regulation is still unknown. Herein, we have analyzed whether 5-HT2 receptor down-regulation following repeated administration of the 5-HT2/5-HT1C receptor agonist 1-(4-iodo-2,5-dimethoxyphenyl)-2-aminopropane (DOI) is affected by glucocorticoid removal. Compared with sham surgery, adrenalectomy (11-15 days beforehand) did not affect either frontal cortex [3H]ketanserin binding nor the number of head shakes elicited by a single administration of DOI (2.5 mg/kg s.c.). Pretreatment with DOI (2.5 mg/kg s.c. x 4 in 48 h) decreased to similar extents the head shake response to DOI injection in sham (-88%) and adrenalectomised (-95%) rats. Confirmingly, this paradigm was found to diminish the Bmax for [3H]ketanserin binding in sham and adrenalectomised rats by 64% and 46%, respectively. From these data, it is concluded that glucocorticoid removal does not alter 5-HT2 receptor binding and function nor does it affect 5-HT2 receptor down-regulation.
众多研究已为糖皮质激素与5-羟色胺2（5-HT2）受体之间的相互关系提供了证据；然而，糖皮质激素是否影响5-HT2受体调节仍不清楚。在此，我们分析了重复给予5-HT2/5-HT1C受体激动剂1-(4-碘-2,5-二甲氧基苯基)-2-氨基丙烷（DOI）后5-HT2受体下调是否受糖皮质激素去除的影响。与假手术相比，肾上腺切除术（提前11 - 15天）既不影响额叶皮质[3H]酮色林结合，也不影响单次给予DOI（2.5 mg/kg皮下注射）引起的摇头次数。DOI预处理（2.5 mg/kg皮下注射，48小时内共4次）使假手术组（-88%）和肾上腺切除组（-95%）大鼠对DOI注射的摇头反应下降程度相似。经证实，该模式使假手术组和肾上腺切除组大鼠中[3H]酮色林结合的最大结合量（Bmax）分别减少64%和46%。从这些数据得出结论，糖皮质激素去除不会改变5-HT2受体结合和功能，也不会影响5-HT2受体下调。
