Wright I K, Garratt J C, Marsden C A
Department of Physiology and Pharmacology, Medical School, Queen's Medical Centre, Nottingham.
Br J Pharmacol. 1990 Feb;99(2):221-2. doi: 10.1111/j.1476-5381.1990.tb14683.x.
Systemic administration of the 5-HT2 agonist 1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane (DOI) (50 and 100 micrograms kg-1, i.v.) inhibited dorsal raphe neuronal firing. DOI (100 micrograms kg-1, i.v.) also produced a decrease in extracellular 5-hydroxytryptamine (5-HT) and 5-hydroxyindoleacetic acid (5-HIAA) in the frontal cortex measured by microdialysis. However, local administration of DOI into the frontal cortex produced no change in extracellular 5-HT and 5-HIAA at any dose given (1, 10 and 100ng). The results demonstrate that DOI is a potent inhibitor of 5-HT neuronal firing and terminal release and that the effects on release are not mediated by an action within the terminal region. The site of action and the receptor involved in the inhibition remains to be determined.
对5-羟色胺2（5-HT2）激动剂1-(2,5-二甲氧基-4-碘苯基)-2-氨基丙烷（DOI）进行全身给药（静脉注射，剂量为50和100微克/千克）可抑制中缝背核神经元放电。DOI（静脉注射，剂量为100微克/千克）还可使通过微透析测量的额叶皮质细胞外5-羟色胺（5-HT）和5-羟吲哚乙酸（5-HIAA）减少。然而，向额叶皮质局部注射DOI，无论给予何种剂量（1、10和100纳克），细胞外5-HT和5-HIAA均无变化。结果表明，DOI是5-HT神经元放电和终末释放的有效抑制剂，且对释放的影响并非由终末区域内的作用介导。抑制作用的作用位点和相关受体仍有待确定。
