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5-羟色胺1A受体的激活增加了大鼠间脑和端脑区域甘丙肽受体的亲和力。

Activation of 5-hydroxytryptamine1A receptors increases the affinity of galanin receptors in di- and telencephalic areas of the rat.

作者信息

Hedlund P, von Euler G, Fuxe K

机构信息

Department of Histology and Neurobiology, Karolinska Institutet, Stockholm, Sweden.

出版信息

Brain Res. 1991 Sep 27;560(1-2):251-9. doi: 10.1016/0006-8993(91)91240-2.

Abstract

Since galanin in vitro selectively increases the KD value of 5-HT1A receptors without altering the binding of 5-HT1B or 5-HT2 receptors, we have studied whether 5-HT1A receptor activation in turn may affect galanin binding in the ventral di- and telencephalon and the substantia nigra of the rat. As analyzed by autoradiography, the binding of 125I-galanin was increased by about 55% in the presence of 3-30 nM of 8-OH-2-(di-n-propylamino)-tetralin (DPAT) in the paraventricular thalamic nucleus, the nucleus reuniens and rhomboideus, the zona incerta, the medial and the lateral hypothalamus, and the medial and the lateral amygdaloid area, but not in the pars compacta of the substantia nigra, which lacks 5-HT1A binding sites. DPAT (10 nM) reduced the IC50 values of galanin at 125I-galanin binding sites by approximately 55% within all the analyzed di- and telencephalic regions. The overall increase in BO values was 50 +/- 11%. Using the filter wipe technique in cryostat sections at Bregma -2.8 mm covering all the brain regions at this level, DPAT (10 nM) decreased the IC50 values of galanin from 21.6 +/- 1.1 nM (control) to 15.5 +/- 0.9 nM, and increased the BO values by 19.4 +/- 4.1%. In membrane preparations from the ventral di- and telencephalon, DPAT decreased the IC50 values of galanin binding sites by 20 +/- 3% at 100 nM of DPAT. This effect could be completely blocked by the specific 5-HT1A receptor antagonist 1-(2-methoxyphenyl)-4-[4-(2-phthalimido)butyl]piperazine.(ABSTRACT TRUNCATED AT 250 WORDS)

摘要

由于甘丙肽在体外可选择性增加5-HT1A受体的KD值,而不改变5-HT1B或5-HT2受体的结合,我们研究了5-HT1A受体激活是否反过来会影响大鼠腹侧间脑和端脑以及黑质中甘丙肽的结合。通过放射自显影分析,在室旁丘脑核、 reunien核和菱形核、未定带、内侧和外侧下丘脑以及内侧和外侧杏仁核区域,存在3 - 30 nM的8-OH-2-(二正丙基氨基)-四氢萘(DPAT)时,125I-甘丙肽的结合增加了约55%,但在缺乏5-HT1A结合位点的黑质致密部则没有增加。DPAT(10 nM)在所有分析的间脑和端脑区域将甘丙肽在125I-甘丙肽结合位点的IC50值降低了约55%。BO值的总体增加为50±11%。在脑坐标-2.8 mm处使用冷冻切片机切片的滤膜擦拭技术覆盖该水平的所有脑区,DPAT(10 nM)将甘丙肽的IC50值从21.6±1.1 nM(对照)降至15.5±0.9 nM,并使BO值增加了19.4±4.1%。在腹侧间脑和端脑的膜制剂中,100 nM的DPAT使甘丙肽结合位点的IC50值降低了20±3%。这种作用可被特异性5-HT1A受体拮抗剂1-(2-甲氧基苯基)-4-[4-(2-邻苯二甲酰亚胺基)丁基]哌嗪完全阻断。(摘要截断于250字)

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