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促肾上腺皮质激素释放因子(CRF)受体拮抗剂可阻断CRF在大鼠体内的激活作用和“致焦虑”作用。

Corticotropin releasing factor (CRF) receptor antagonist blocks activating and 'anxiogenic' actions of CRF in the rat.

作者信息

Britton K T, Lee G, Vale W, Rivier J, Koob G F

出版信息

Brain Res. 1986 Mar 26;369(1-2):303-6. doi: 10.1016/0006-8993(86)90539-1.

Abstract

The effectiveness of a recently synthesized corticotropin releasing factor (CRF) antagonist, alpha-helical CRF9-41, in reversing the locomotor activating and proconflict effects of CRF was evaluated. The CRF receptor antagonist (50, 100 and 200 micrograms, i.c.v.) produced a dose-related attenuation of the response-suppressing effects of CRF in a conflict model of anxiety. The antagonist also effectively suppressed the marked locomotor activation produced by CRF. No discernible intrinsic effects on behavior were noted when the antagonist was administered alone. These results suggest that the behavioral effects of CRF are receptor-mediated phenomena and point to the potential usefulness of a CRF antagonist in understanding the function of endogenous CRF in mediating responses to stressful stimuli.

摘要

评估了一种最近合成的促肾上腺皮质激素释放因子(CRF)拮抗剂α-螺旋CRF9-41在逆转CRF的运动激活和促冲突效应方面的有效性。在焦虑的冲突模型中,CRF受体拮抗剂(50、100和200微克,脑室内注射)产生了与剂量相关的对CRF反应抑制效应的减弱。该拮抗剂还有效抑制了CRF产生的明显运动激活。单独给予拮抗剂时,未观察到对行为有明显的内在影响。这些结果表明,CRF的行为效应是受体介导的现象,并指出CRF拮抗剂在理解内源性CRF在介导对压力刺激反应中的功能方面的潜在用途。

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