3H-酪氨酸-D-丙氨酸-甘氨酸-N（甲基）苯丙氨酸氯甲基酮的合成——一种阿片样物质亲和标记物。

Synthesis of 3H-Tyr-D-Ala-Gly-N(Me)Phe chloromethyl ketone--an opioid affinity label.

作者信息

Varga E, Tóth G, Hepp J, Benyhe S, Simon J, Medzihradszky K, Borsodi A

机构信息

Institute of Biochemistry, Hungarian Academy of Sciences, Szeged.

出版信息

Neuropeptides. 1988 Oct;12(3):135-9. doi: 10.1016/0143-4179(88)90044-3.

DOI:10.1016/0143-4179(88)90044-3

PMID:2853836

Abstract

A radioactive enkephalin affinity reagent, selective for the mu opioid receptor subtype, was synthesized by a fragment condensation method. 3H-BOC-Tyr-D-Ala-Gly-OH was prepared by catalytic tritiation of the protected iodinated tripeptide. The protected tritiated tripeptide and N(Me)Phe-CH2Cl were condensed by the mixed anhydride method. The protecting group was removed by HCl/acetic acid. The tritiated tetrapeptide has a specific radioactivity of 56.8 Ci/mmole (2.1 TBq/mmole).

摘要

一种对μ阿片受体亚型具有选择性的放射性脑啡肽亲和试剂，通过片段缩合方法合成。通过对受保护的碘化三肽进行催化氚化制备了3H-BOC-Tyr-D-Ala-Gly-OH。受保护的氚化三肽和N(Me)Phe-CH2Cl通过混合酸酐法缩合。通过HCl/乙酸去除保护基团。该氚化四肽的比放射性为56.8 Ci/mmole（2.1 TBq/mmole）。