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甘丙肽(1-15)而非甘丙肽(1-29)可调节大鼠脑海马背侧的5-HT1A受体:可能存在甘丙肽受体亚型。

Galanin-(1-15), but not galanin-(1-29), modulates 5-HT1A receptors in the dorsal hippocampus of the rat brain: possible existence of galanin receptor subtypes.

作者信息

Hedlund P B, Finnman U B, Yanaihara N, Fuxe K

机构信息

Department of Neuroscience, Karolinska Institute, Stockholm, Sweden.

出版信息

Brain Res. 1994 Jan 14;634(1):163-7. doi: 10.1016/0006-8993(94)90271-2.

Abstract

The aim of the present study was to evaluate whether galanin-(1-29) and galanin-(1-15) can modulate the 5-hydroxytryptamine1A (5-HT1A) receptors using [3H]8-OH-2-(di-n-propylamino)-tetralin ([3H]8-OH-DPAT) as a radioligand. Membrane preparations of the dorsal hippocampus, an area having the recently described [125I]galanin-(1-15) fragment binding sites, but having very few porcine [125I]galanin-(1-29) binding sites, were used. Galanin-(1-15) produced a concentration-dependent increase in the Kd value of [3H]8-OH-DPAT with a maximum effect of approximately 65% at 3 nM of galanin-(1-15), whereas galanin-(1-29) had no effect. This increase of the Kd value of [3H]8-OH-DPAT could be completely counteracted by the putative galanin antagonist M35 (1 nM). The Bmax values of [3H]8-OH-DPAT were not affected in any experiment. In conclusion, the present results give further evidence for the existence of a galanin receptor subtype mainly recognizing N-terminal galanin fragments, also having the ability to reduce the affinity of 5-HT1A receptors.

摘要

本研究的目的是使用[3H]8-羟基-2-(二正丙基氨基)四氢萘([3H]8-OH-DPAT)作为放射性配体,评估甘丙肽-(1-29)和甘丙肽-(1-15)是否能调节5-羟色胺1A(5-HT1A)受体。使用了背侧海马体的膜制剂,该区域具有最近描述的[125I]甘丙肽-(1-15)片段结合位点,但猪[125I]甘丙肽-(1-29)结合位点极少。甘丙肽-(1-15)使[3H]8-OH-DPAT的Kd值呈浓度依赖性增加,在3 nM甘丙肽-(1-15)时最大效应约为65%,而甘丙肽-(1-29)无作用。[3H]8-OH-DPAT的Kd值增加可被假定的甘丙肽拮抗剂M35(1 nM)完全抵消。在任何实验中,[3H]8-OH-DPAT的Bmax值均未受影响。总之,本研究结果进一步证明存在一种主要识别N端甘丙肽片段的甘丙肽受体亚型,其也具有降低5-HT1A受体亲和力的能力。

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