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磷酸丝氨酸对代谢型谷氨酸受体IV型有亲和力,但对I型没有。

Serine-O-phosphate has affinity for type IV, but not type I, metabotropic glutamate receptor.

作者信息

Thomsen C, Suzdak P D

机构信息

Department of Receptor Neurochemistry, Novo Nordisk A/S, Måløv, Denmark.

出版信息

Neuroreport. 1993 Sep;4(9):1099-101.

PMID:8106006
Abstract

L-serine-O-phosphate (L-SOP) has been reported to antagonize phosphoinositide (PI) hydrolysis in slices of rat brain as stimulated by agonists of the metabotropic glutamate receptor (mGluR). In the present study, the affinity of L-SOP was examined in a baby hamster kidney (BHK) cells expressing subtype mGluR1 or mGluR4 of the mGluR family. L-SOP or D-SOP (3 mM) did not inhibit PI-hydrolysis as stimulated by 10 microM glutamate in BHK cells expressing mGluR1. However, L-SOP was a potent agonist at the mGluR4 subtype (IC50 = 4.4 +/- 1.4 microM), which is negatively coupled to adenylate cyclase, while D-SOP was weakly active (IC50 = 1260 +/- 190 microM).

摘要

据报道,L-丝氨酸-O-磷酸(L-SOP)可拮抗代谢型谷氨酸受体(mGluR)激动剂刺激大鼠脑切片中的磷酸肌醇(PI)水解。在本研究中,检测了L-SOP对表达mGluR家族mGluR1或mGluR4亚型的幼仓鼠肾(BHK)细胞的亲和力。在表达mGluR1的BHK细胞中,L-SOP或D-SOP(3 mM)不抑制10 microM谷氨酸刺激的PI水解。然而,L-SOP是mGluR4亚型的强效激动剂(IC50 = 4.4 +/- 1.4 microM),mGluR4与腺苷酸环化酶负偶联,而D-SOP活性较弱(IC50 = 1260 +/- 190 microM)。

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