Inhibition of central neurotransmitter release by ω-conotoxin GVIA, a peptide modulator of the N-type voltage-sensitive calcium channel

Inhibition of central neurotransmitter release by ω-conotoxin GVIA, a peptide modulator of the N-type voltage-sensitive calcium channel
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ω-芋螺毒素 GVIA(N 型电压敏感钙通道的肽调节剂)抑制中枢神经递质释放

DOI:
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发表时间:
1987
期刊:
Naunyn-Schmiedeberg's Archives of Pharmacology
影响因子:
--
通讯作者:
G. Hertting
G. Hertting
中科院分区:
--
文献类型:
--
作者:
D. Dooley;A. Lupp;G. Hertting

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总结氚溢出,由电刺激诱发[3 H]多巴胺-、[3 H]-去甲肾上腺素-、[3 H]-5-羟色胺-和[3 H]-乙酰胆碱-标记的切片从兔中枢神经系统的不连续区域制备,共芋螺毒素GVIA抑制(2 min; 2 ms,3 Hz,5 V/cm和24 mA)39- 50(ω-CT; 5 nmol/l),一种N型电压敏感性钙通道(N-VSCC)的肽调节剂。使用ω-CT(5 nmol/l)和[3 H]-去甲肾上腺素标记的海马切片的其他实验表明,ω-CT诱导的抑制具有时间依赖性,缓冲液钙浓度与ω-CT之间存在竞争性拮抗作用,长时间电刺激(15 min; 0.4 Hz)对ω-CT诱导的抑制无影响。这些不同的结果表明:1)ω-CT与钙竞争N-VSCC,2)ω-CT的抑制作用与N-VSCC的门控状态无关,3)N-VSCC的分子性质在中枢神经递质系统中可能相似或相同。ω-CT在研究N-VSCC参与神经递质释放方面似乎是一种有用的药理学工具。
SummaryTritium overflows, evoked by electrical stimulation (2 min; 2 ms, 3 Hz, 5 V/cm, and 24 mA) of [3H]dopamine-, [3H]-noradrenaline-, [3H]-5-hydroxytrypt-amine, and [3H]-acetylcholine-labeled slices prepared from discrete regions of the rabbit central nervous system, were inhibited 39–50% by co-conotoxin GVIA (ω-CT; 5 nmol/l), a peptide modulator of the N-type voltage-sensitive calcium channel (N-VSCC). Additional experiments using ω-CT (5 nmol/l) and [3H]-noradrenaline-labeled hippocampal slices indicated the time dependence of ω-CT-induced inhibition, the competitive antagonism between buffer calcium concentration and ω-CT, and the lack of effect of prolonged electrical stimulation (15 min; 0.4 Hz) on ω-CT-induced inhibition. These various results suggest that 1) ω-CT competes with calcium for the N-VSCC, 2) the inhibitory effects of ω-CT are independent of the gating state of the N-VSCC, and 3) the molecular nature of the N-VSCC may be similar or identical across central neurotransmitter systems. ω-CT appears to be a useful pharmacological tool in studying the involvement of the N-VSCC in neurotransmitter release.
二氢吡啶结合位点是电压敏​​感的钙通道吗?
DOI: 10.1016/0024-3205(84)90543-5
发表时间: 1984
期刊: Life sciences
影响因子: 6.1
作者:
Miller,RJ;Freedman,SB
通讯作者: Freedman,SB
DOI: 10.1126/science.2432656
发表时间: 1987-01-02
期刊: SCIENCE
影响因子: 56.9
作者:
MILLER, RJ
通讯作者: MILLER, RJ
DOI: --
发表时间: 1987
期刊: The Journal of biological chemistry
影响因子: --
作者:
Rivier,J;Galyean,R;Gray,WR;Azimi-Zonooz,A;McIntosh,JM;Cruz,LJ;Olivera,BM
通讯作者: Olivera,BM