Waglerin-1 inhibits GABA(A) current of neurons in the nucleus accumbens of neonatal rats.
Waglerin-1 inhibits GABA(A) current of neurons in the nucleus accumbens of neonatal rats.
复制标题
Waglerin-1 抑制新生大鼠伏核神经元的 GABA(A) 电流。
DOI：
10.1016/s0006-8993(99)01668-6
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发表时间：
1999
期刊：
影响因子：
2.9
通讯作者：
McArdle,JJ
中科院分区：
文献类型：
--
作者：
Ye,JH;Ren,J;McArdle,JJ
用3 ~ 7日龄大鼠延髓核分离的神经元，观察了Waglerin-1对γ-氨基丁酸（GABA）诱发的全细胞电流反应（IGABA）的影响。Waglerin-1抑制GABA亚饱和浓度诱导的IGABA; 10 μM GABA诱导的IGABA的IC 50为2.5 μM Waglerin-1。该浓度的Waglerin-1以平行方式使GABA浓度-反应曲线向右移动，使GABA EC 50从12±3 μ M增加至27±5 μM。Waglerin-1的抑制作用在负保持电位下更大。Zn ~（2+）对IGABA也有抑制作用，IC_（50）为0.3 μM。磷酸化状态似乎调节GABA A受体对Waglerin-1抑制作用的敏感性，因为用蛋白激酶A抑制剂N-[2-（（p-溴肉桂基）氨基）乙基]-5-异喹啉磺酰胺盐酸盐（H-89）透析神经元可阻止抑制。的数据进行了讨论，在发育的影响，GABAA受体的亚基组成的神经元的核神经元。
The effect of Waglerin-1, a 22-amino acid peptide purified from the venom of Wagler's pit viper on the whole cell current response (IGABA) to γ-aminobutyric acid (GABA) was examined for neurons freshly isolated from the nucleus accumbens of 3- to 7-day-old rats. Waglerin-1 depressed IGABAinduced by subsaturating concentrations of GABA; the IC50for IGABAinduced by 10 μM GABA was 2.5 μM Waglerin-1. This concentration of Waglerin-1 shifted the GABA concentration–response curve to the right in a parallel manner, increasing the GABA EC50from 12±3 to 27±5 μM. The depressant effect of Waglerin-1 was greater at negative holding potentials. Zn2+also inhibited IGABAwith an IC50of 0.3 μM. Phosphorylation state appeared to modulate GABAAreceptor sensitivity to the inhibitory effect of Waglerin-1 since dialysis of neurons with N-[2-((p-bromocinnamyl)amino)ethyl]-5-isoquinolinesulfonamide HCl (H-89), an inhibitor of protein kinase A, prevented inhibition. The data are discussed in terms of developmental influences on the subunit composition of GABAAreceptors in neurons of the nucleus accumbens.