5-羟色胺7受体刺激对培养的大鼠视交叉上核神经元中GABAA受体激活电流的抑制作用。
Inhibition by 5-HT7 receptor stimulation of GABAA receptor-activated current in cultured rat suprachiasmatic neurones.
作者信息
Kawahara F, Saito H, Katsuki H
机构信息
Department of Chemical Pharmacology, Faculty of Pharmaceutical Sciences, University of Tokyo, Japan.
出版信息
J Physiol. 1994 Jul 1;478 ( Pt 1)(Pt 1):67-73. doi: 10.1113/jphysiol.1994.sp020230.
Abstract
- Whole-cell voltage-clamp recordings were made from postnatal rat suprachiasmatic (SCN) neurones to investigate possible modulation by 5-hydroxytryptamine (5-HT) of gamma-aminobutyric acid (GABA)-activated current (IGABA). 2. 5-HT reversibly inhibited IGABA in a concentration-dependent manner (10(-10) to 10(-6) M). (+/-)-8-Hydroxy-2-N,N-dipropylaminotetralin (8-OH-DPAT, 10(-10) to 10(-5) M) and 5-carboxamidotryptamine (10(-6) M) also inhibited IGABA, whereas 1-(2,5-dimethyl-4-iodophenyl)-2-aminopropane (DOI, 10(-6) M) had no significant effect. 3. The effect of 8-OH-DPAT (10(-7) M) was blocked by ritanserin (10(-7) M), but not by pindolol (10(-7) M). The effect of 5-HT was also suppressed by ritanserin, but not by pindolol, ketanserin (10(-7) M) or ICS 205-930 (10(-6) M). 4. 8-Bromo-cAMP (10(-3) M) or forskolin (5 x 10(-5) M) suppressed IGABA. The effects of forskolin and 5-HT were not additive. Furthermore, the effect of 5-HT (10(-7) M) was significantly reduced by N-[2-(methylamino)ethyl]-5-isoquinoline sulphonamide (H-8, 10(-6) M). 5. It is concluded that 5-HT inhibits IGABA in the SCN neurones, which involves the activation of 5-HT7 receptors and cAMP-coupled systems.
摘要
- 采用全细胞膜片钳记录技术，对出生后大鼠视交叉上核（SCN）神经元进行记录，以研究5-羟色胺（5-HT）对γ-氨基丁酸（GABA）激活电流（IGABA）的可能调节作用。2. 5-HT以浓度依赖性方式（10^(-10)至10^(-6) M）可逆性抑制IGABA。（±）-8-羟基-2-N，N-二丙基氨基四氢萘（8-OH-DPAT，10^(-10)至10^(-5) M）和5-羧基色胺（10^(-6) M）也抑制IGABA，而1-（2,5-二甲基-4-碘苯基）-2-氨基丙烷（DOI，10^(-6) M）无显著作用。3. 8-OH-DPAT（10^(-7) M）的作用被利坦色林（10^(-7) M）阻断，但不被吲哚洛尔（10^(-7) M）阻断。5-HT的作用也被利坦色林抑制，但不被吲哚洛尔、酮色林（10^(-7) M）或ICS 205-930（10^(-6) M）抑制。4. 8-溴-cAMP（10^(-3) M）或福斯可林（5×10^(-5) M）抑制IGABA。福斯可林和5-HT的作用无相加性。此外，5-HT（10^(-7) M）的作用被N-[2-（甲氨基）乙基]-5-异喹啉磺酰胺（H-8，10^(-6) M）显著减弱。5. 得出结论：5-HT抑制SCN神经元中的IGABA，这涉及5-HT7受体和cAMP偶联系统的激活。
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