Thiocyanate stabilizes AMPA binding to the quisqualate receptor.

Thiocyanate stabilizes AMPA binding to the quisqualate receptor.
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硫氰酸盐可稳定 AMPA 与使君子酸受体的结合。

DOI:
10.1016/0014-2999(88)90383-4
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发表时间:
1988
影响因子:
5
通讯作者:
Young,AB
Young,AB
中科院分区:
医学2区
文献类型:
--
作者:
Nielsen,EO;Cha,JH;Honoré,T;Penney,JB;Young,AB

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钙离子和氯离子刺激[3 H]谷氨酸结合到使君子酸敏感的[3 H]谷氨酸结合位点4倍,通过定量放射自显影测量,而100 mM硫氰酸钾没有额外的效果。相反,钙和氯对[3 H](RS)-α-氨基-3-羟基-5-甲基异恶唑-4-丙酸([3 H]AMPA)的结合几乎没有影响,但100 mM硫氰酸盐刺激结合4倍。在没有硫氰酸盐的情况下,AMPA从小脑分子层中的使君子酸敏感结合位点置换很少的[3 H]谷氨酸结合。然而,在硫氰酸盐的存在下,AMPA成为一个更有效的置换剂,但仍然只置换了44%的使君子酸敏感的[3 H]谷氨酸结合。[~ 3 H]谷氨酸结合到使君子酸敏感位点的分布与[~ 3 H]AMPA结合的分布相似但不相同。而AMPA可置换的[3 H]谷氨酸结合的分布与[3 H]AMPA结合的分布高度相关(r = 0.97,P<0.0005)。结果表明,AMPA结合到使君子酸敏感的[3 H]谷氨酸盐结合位点的一个亚类,其高度受离子环境的影响,并且使君子酸敏感的结合位点以几种状态存在。
Calcium and chloride ions stimulated [3H]glutamate binding to quisqualate-sensitive [3H]glutamate binding sites 4-fold, as measured by quantitative autoradiography, whereas 100 mM potassium thiocyanate had no additional effect. In contrast, calcium and chloride had little effect on the binding of [3H](RS)-α-amino-3-hydroxy-5-methylisoxazole-4-proprionic acid ([3H]AMPA), but 100 mM thiocyanate stimulated binding 4-fold. AMPA displace little [3H]glutamate binding from quisqualate-sensitive binding sites in the molecular layer of the cerebellum in the absence of thiocyanate. However, in the presence of thiocyanate AMPA became a more effective displacer, but still displaced only 44% of the quisqualate-sensitive [3H]glutamate binding. The distribution of [3H]glutamate binding to quisqualate-sensitive sites was similar to but not identical with that of [3H]AMPA binding. However, the distribution of AMPA-displaceable [3H]glutamate binding correlated highly (r = 0.97, P<0.0005) with that of [3H]AMPA binding. The results suggest that AMPA binds to a subclass of quisqualate-sensitive [3H]glutamate binding sites that are highly influenced by ionic environment and that quisqualate-sensitive binding sites exist in several states.