Venn R F, Barnard E A
J Biol Chem. 1981 Feb 25;256(4):1529-32.
The synthesis and characterization of a novel enkephalin analogue, Tyr-D-Ala-Gly-Phe-Leu-chloromethyl ketone, is described. The biological potency of the compound in various assays has been determined to be very high. The compound is an alkylating affinity reagent and irreversibly inactivates a defined population of enkephalin receptors in rat brain membrane preparations, as well as irreversibly inhibiting electrically stimulated contractions in the mouse vas deferens tissue preparation.
描述了一种新型脑啡肽类似物Tyr-D-Ala-Gly-Phe-Leu-氯甲基酮的合成与表征。已确定该化合物在各种测定中的生物活性非常高。该化合物是一种烷基化亲和试剂，可不可逆地使大鼠脑膜制剂中特定群体的脑啡肽受体失活，也可不可逆地抑制小鼠输精管组织制剂中的电刺激收缩。
