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人们已经知道在脑内至少有两种类吗啡肽的受体存在。能够与吗啡、呐咯酮(naloxone)或呐曲酮(naltrexone)结合的受体称μ-受体。能与脑啡肽结合的称δ-受体。人们常用豚鼠回肠和小白鼠输精管作为测定这两种受体的药理学模型。我们在研究脑啡肽的结构与功能关系工作中,用经典的液相方法合成了一系列脑啡肽类似物。发现其中有两个类似物——[D-丙~2-O-苯甲基-丝~5]脑啡肽和[D-丙~2-S-苯甲基-半胱~5]脑啡肽具有对δ-受体特别强的亲合能力。它们的合成路线见图1,合成肽的物理常数列于
It is known that there are at least two receptors for morphin in the brain. Receptors that are capable of binding morphine, naloxone, or naltrexone are called μ-receptors. Δ-receptor that binds enkephalin. Guinea pig ileum and mouse vas deferens are commonly used as pharmacological models for determining these two receptors. We studied the structure and function of enkephalin in a series of enkephalin analogues synthesized by classical liquid phase method. Two of the analogues were found - enkephalin and [D-prop-2-S-benzyl-cysteine-5] Peptides have particularly strong affinity for delta-receptors. Their synthetic routes are shown in Figure 1, and the physical constants of the synthetic peptides are listed