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可乐定和强啡肽A-(1-13)可降低突触体游离[Ca2+]水平,而咪唑克生则可使其升高。

Synaptosomal free [Ca2+] is reduced by clonidine and dynorphin A-(1-13) and increased by idazoxan.

作者信息

Adamson P, McWilliam J R, Brammer M J, Campbell I C

机构信息

Department of Biochemistry, Institute of Psychiatry, De Crespigny Park, London, U.K.

出版信息

Eur J Pharmacol. 1987 Oct 13;142(2):261-6. doi: 10.1016/0014-2999(87)90115-4.

Abstract

Intrasynaptosomal free calcium concentrations measured in rat cortical synaptosomes using the calcium sensitive fluorescent dye quin 2, were found to be 0.107-0.122 microM (n = 33). Stimulation of alpha 2-adrenoceptors or kappa-opiate receptors with clonidine (0.1-100 microM) or dynorphin A fragment (1-13) (0.2-5.0 microM) respectively, produced a dose dependent reduction in the intrasynaptosomal free calcium concentration. The alpha 2-adrenoceptor mediated reduction produced by clonidine (100 microM) was antagonised by the selective alpha 2-antagonist idazoxan (RX781094) (200 microM). Dynorphin A-(1-13) (1 microM) caused a reduction which was antagonised by a high (20 microM) but not low (2.0 microM) concentration of naloxone. We conclude that unlike the mu- and delta-opiate receptor, stimulation of alpha 2-adrenoceptors or kappa-opiate receptors elicits changes in intrasynaptosomal free calcium concentration which are independent of the voltage sensitive calcium channel. This does not preclude the possibility that the alpha 2-adrenoceptor and kappa-opiate receptor also have an effect at the voltage sensitive calcium channel.

摘要

用钙敏荧光染料喹啉2在大鼠皮质突触体中测得的突触体内游离钙浓度为0.107 - 0.122微摩尔(n = 33)。分别用可乐定(0.1 - 100微摩尔)或强啡肽A片段(1 - 13)(0.2 - 5.0微摩尔)刺激α2 - 肾上腺素能受体或κ - 阿片受体,可使突触体内游离钙浓度呈剂量依赖性降低。可乐定(100微摩尔)介导的α2 - 肾上腺素能受体介导的降低被选择性α2 - 拮抗剂咪唑克生(RX781094)(200微摩尔)拮抗。强啡肽A - (1 - 13)(1微摩尔)引起的降低被高浓度(20微摩尔)而非低浓度(2.0微摩尔)的纳洛酮拮抗。我们得出结论,与μ - 和δ - 阿片受体不同,刺激α2 - 肾上腺素能受体或κ - 阿片受体引起突触体内游离钙浓度的变化,这些变化独立于电压敏感性钙通道。这并不排除α2 - 肾上腺素能受体和κ - 阿片受体也对电压敏感性钙通道有影响的可能性。

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