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ω-阿加毒素IVA可识别单一的钙通道亚型,该亚型参与钾离子诱导的大鼠脑片乙酰胆碱、5-羟色胺、多巴胺、γ-氨基丁酸和谷氨酸的释放。

omega-Agatoxin IVA identifies a single calcium channel subtype which contributes to the potassium-induced release of acetylcholine, 5-hydroxytryptamine, dopamine, gamma-aminobutyric acid and glutamate from rat brain slices.

作者信息

Harvey J, Wedley S, Findlay J D, Sidell M R, Pullar I A

机构信息

Eli Lilly and Company, Lilly Research Centre Ltd., Windlesham, Surrey, UK.

出版信息

Neuropharmacology. 1996 Apr;35(4):385-92. doi: 10.1016/0028-3908(96)00010-x.

Abstract

The voltage-dependent calcium channels (VDCCs) involved in K(+)-induced transmitter release have been studied. A maximally effective concentration of the N-type VDCC inhibitor, omega-conotoxin GVIA (GVIA) blocked the release of 5-HT (30%), DA (30%) and ACh (60%) but not that of GABA or glutamate. The O, P and Q-type VDCC inhibitor, omega-agatoxin IVA (Aga IVA, 1 microM), blocked 100% of GABA and glutamate, 70% of DA and about 50% of 5-HT and ACh release. The slopes of the inhibiton curves indicate that it acts on the same, single type of VDCC in all cases. omega-Conotoxin MVIIC (MVIIC) completely inhibited the release of all the transmitters. It is concluded that a single GVIA-insensitive type of VDCC is involved in the K(+)-induced release of all the transmitters and, in addition, N-type VDCCs, with a higher affinity for GVIA than MVIIC, are required for the release of 5-HT, DA and ACh. The non-N-type VDCC is not the O-type as it is not blocked by low (< 10 nM) concentrations of MVIIC. Further resolution of this VDCC into P or Q-type requires more selective antagonists.

摘要

对参与钾离子诱导递质释放的电压依赖性钙通道(VDCCs)进行了研究。N型VDCC抑制剂ω-芋螺毒素GVIA(GVIA)的最大有效浓度可阻断5-羟色胺(5-HT,30%)、多巴胺(DA,30%)和乙酰胆碱(ACh,60%)的释放,但不影响γ-氨基丁酸(GABA)或谷氨酸的释放。O、P和Q型VDCC抑制剂ω-阿加毒素IVA(Aga IVA,1微摩尔)可阻断100%的GABA和谷氨酸、70%的DA以及约50%的5-HT和ACh释放。抑制曲线的斜率表明,在所有情况下它作用于同一种单一类型的VDCC。ω-芋螺毒素MVIIC(MVIIC)完全抑制了所有递质的释放。得出的结论是,一种对GVIA不敏感的单一类型VDCC参与了钾离子诱导的所有递质释放,此外,对GVIA的亲和力高于MVIIC的N型VDCC是5-HT、DA和ACh释放所必需的。非N型VDCC不是O型,因为它不受低浓度(<10纳摩尔)MVIIC的阻断。要将这种VDCC进一步区分为P型或Q型需要更具选择性的拮抗剂。

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