Kennett G A, Marcou M, Dourish C T, Curzon G
Eur J Pharmacol. 1987 Jun 12;138(1):53-60. doi: 10.1016/0014-2999(87)90336-0.
The 5-HT1A agonists, 8-hydroxy-2-(di-n-propylamino) tetralin (8-OH-DPAT), buspirone or TVXQ 7821 (ipsapirone) but not the 5-HT1B agonist RU 24969, attenuated the hyperphagic response to 8-OH-DPAT administered on the next day. Attenuation was still apparent on the fifth day after either 8-OH-DPAT or buspirone but not on the tenth day after 8-OH-DPAT administration. The ability of 8-OH-DPAT to reduce raphe 5-HIAA levels was also impaired by previous 8-OH-DPAT treatment. However, the 8-OH-DPAT or 5-methoxy-N,N-dimethyltryptamine-induced 5-HT syndromes were unaltered. The results indicate that a single pretreatment with 5-HT1A agonists rapidly desensitises 5-HT1A presynaptic receptor-mediated responses. This effect may mediate the antidepressant-like action of the drugs in an animal model of depression.
5-羟色胺1A（5-HT1A）激动剂，8-羟基-2-（二正丙基氨基）四氢萘（8-OH-DPAT）、丁螺环酮或TVXQ 7821（伊沙匹隆），而非5-HT1B激动剂RU 24969，可减弱次日给予8-OH-DPAT后的摄食亢进反应。在给予8-OH-DPAT或丁螺环酮后的第五天，这种减弱仍很明显，但在给予8-OH-DPAT后的第十天则不明显。先前的8-OH-DPAT处理也损害了8-OH-DPAT降低中缝5-羟吲哚乙酸（5-HIAA）水平的能力。然而，8-OH-DPAT或5-甲氧基-N，N-二甲基色胺诱导的5-羟色胺（5-HT）综合征未改变。结果表明，单次用5-HT1A激动剂预处理可使5-HT1A突触前受体介导的反应迅速脱敏。这种效应可能介导了这些药物在抑郁症动物模型中的抗抑郁样作用。
