Komissarov I V, Dolzhenko A T, Obraztsova O G, Zin'kovskaia L Ia
Biull Eksp Biol Med. 1990 Mar;109(3):275-7.
The hypothermic activity of 8-OH-DRAT, 1-(2-pyrimidinyl) piperazine (1-PP), buspirone and its structure analogues tightly correlates with the degree of inhibition of 3H-serotonine release by electrically stimulated dorsal raphe slices (r = 0.84), but not cerebral cortex slices (r = 0.66). The pretreatment of mice with p-chlorphenylalanine decreased the hypothermic effects evoked by 8-OH-DRAT, buspirone, campirone (but not 1-PP) only in first 30 min after there injection. It was concluded that hypothermic effects of 8-OH-DRAT, buspirone and its structure analogues were bound with preferable influence as partial agonists on the postsynaptic serotonine 1A receptors. Ipsapirone as a partial agonist has maximal antagonistic activity.
8-羟基-二苯并氮杂卓(8-OH-DRAT)、1-(2-嘧啶基)哌嗪(1-PP)、丁螺环酮及其结构类似物的降温活性与电刺激中缝背核切片对3H-血清素释放的抑制程度紧密相关(r = 0.84),但与大脑皮层切片的抑制程度相关性较差(r = 0.66)。用对氯苯丙氨酸预处理小鼠,仅在注射后最初30分钟内可降低8-OH-DRAT、丁螺环酮、坎吡隆(但不包括1-PP)引起的降温作用。得出的结论是,8-OH-DRAT、丁螺环酮及其结构类似物的降温作用与作为部分激动剂对突触后血清素1A受体的优先影响有关。伊沙匹隆作为部分激动剂具有最大的拮抗活性。