酪氨酸-1取代且具有荧光性的丙氨酸-1-脑啡肽能强烈且选择性地与μ和δ阿片受体结合。
Tyr1-substituted and fluorescent Pya1-enkephalins bind strongly and selectively to mu and delta opiate receptors.
作者信息
Mihara H, Lee S, Shimohigashi Y, Aoyagi H, Kato T, Izumiya N, Costa T
出版信息
Biochem Biophys Res Commun. 1986 May 14;136(3):1170-6. doi: 10.1016/0006-291x(86)90457-2.
The fluorescent enkephalins in which an essential Tyr1 residue is replaced by L-1-pyrenylalanine (Pya) were synthesized and examined in the receptor binding assays. [Pya1, Leu5]Enkephalin and its methyl ester showed binding characteristics specific for the opiate receptors, exhibiting a potent inhibition of Tyr1-containing enkephalins. Surprisingly, the methyl ester displayed almost the same potencies to those of DAGO-enkephalin. This analog bound 24-fold more strongly to mu than to delta-receptors. C-terminal free analog Pya1-Enk-OH was delta-preferential with a fairly good affinity. These results indicate that Tyr1 in enkephalin is not necessary to recognition of the opiate receptors.
合成了其中必需的Tyr1残基被L-1-芘基丙氨酸（Pya）取代的荧光脑啡肽，并在受体结合试验中进行了检测。[Pya1，Leu5]脑啡肽及其甲酯显示出对阿片受体具有特异性的结合特性，对含Tyr1的脑啡肽表现出强效抑制作用。令人惊讶的是，甲酯显示出与DAGO-脑啡肽几乎相同的效力。该类似物与μ受体的结合强度比与δ受体的结合强度高24倍。C末端游离类似物Pya1-Enk-OH对δ受体具有优先选择性，亲和力相当好。这些结果表明，脑啡肽中的Tyr1对于阿片受体的识别并非必需。
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