Ferkany J, Zaczek R, Markl A, Coyle J T
Neurosci Lett. 1984 Feb 24;44(3):281-6. doi: 10.1016/0304-3940(84)90036-3.
The dipeptide, L-phenylalanyl-L-glutamate (PG), augments the specific binding of the excitatory amino acid receptor antagonist, [3H]2-amino-7-phosphonoheptanoic acid (APH), to rat forebrain membranes by 5-fold at 100 microM with an EC50 of 4.9 microM. The increase in the specific binding of [3H]AHP induced by PG results exclusively from an increase in Bmax. In contrast, PG inhibits the specific binding of [3H]kainic acid to forebrain membranes with a Ki of 6.8 microM. Of several related peptides examined, active ones affected the two receptor sites in a reciprocal fashion. The results suggest an allosteric interaction between [3H]APH and kainate receptors modulated by glutamate-containing peptides.
二肽L-苯丙氨酰-L-谷氨酸（PG）可使兴奋性氨基酸受体拮抗剂[3H]2-氨基-7-磷酸庚酸（APH）与大鼠前脑细胞膜的特异性结合在100微摩尔浓度下增强5倍，半数有效浓度（EC50）为4.9微摩尔。PG诱导的[3H]AHP特异性结合增加完全是由于最大结合容量（Bmax）的增加。相比之下，PG抑制[3H] kainic酸与前脑细胞膜的特异性结合，抑制常数（Ki）为6.8微摩尔。在所检测的几种相关肽中，有活性的肽以相反的方式影响这两个受体位点。结果表明，[3H]APH和由含谷氨酸肽调节的海人藻酸受体之间存在变构相互作用。
