Walczak S A, Wilkening D, Makman M H
Brain Res. 1979 Jan 5;160(1):105-16. doi: 10.1016/0006-8993(79)90604-8.
Adenylate cyclase activity (AC) of homogenates of monkey amygdaloid nucleus was approximately doubled in the presence of dopamine (10 micrometer). Morphine, etorphine, and several enkephalin analogs (met-enkephalin, D-ala2-met-enkephalin, and D-met2, pro5-enkephalinamide) were capable of inhibiting the stimulation of AC produced by dopamine (90-100% with etorphine or D-ala2-met-enkephalin). Unlike morphine and etorphine, the peptides exhibited bell-shaped dose-response curves for this inhibition with maximal effects at approximately 1 X 10(-7) M, but negligible effects at 1 X 10(-5) M. Under the conditions studied, only etorphine inhibited basal AC. Naloxone antagonized the inhibitory effects of each of the opioids tested, and dextrorphan, an inactive L-(+)-opiate, failed to inhibit the dopamine response. Together these data indicate that the effects were mediated via the classically described stereospecific opiate receptor. The relative order of potency (etorphine greater than enkephalins greater than morphine) was similar to that previously reported for the binding affinities of these drugs in rat brain homogenates. The influence of narcotic agents on dopamine stimulated AC was eliminated by either freezing the amygdaloid tissue or preincubating the homogenate at 4 degrees C; the dopamine responses, however, could still be elicited. The narcotic receptor interaction with the adenylate cyclase thus appears to be distinct from and more labile than that of the dopamine receptor. Gpp(NH)p-stimulated AC was not inhibited by morphine. It is postulated that the inhibition involves interaction of opiate receptors with catalytic units of dopamine-stimulated AC, but not with other cyclase species which may provide the major component of Gpp(NH)p-stimulated activity in amygdala.
在存在多巴胺(10微摩尔)的情况下,猴杏仁核匀浆的腺苷酸环化酶活性(AC)大约增加了一倍。吗啡、埃托啡和几种脑啡肽类似物(甲硫脑啡肽、D-丙氨酸2-甲硫脑啡肽和D-蛋氨酸2、脯氨酸5-脑啡肽酰胺)能够抑制多巴胺对AC的刺激(埃托啡或D-丙氨酸2-甲硫脑啡肽可抑制90%-100%)。与吗啡和埃托啡不同,这些肽对这种抑制作用呈现钟形剂量反应曲线,在约1×10⁻⁷M时具有最大效应,但在1×10⁻⁵M时效应可忽略不计。在所研究的条件下,只有埃托啡抑制基础AC。纳洛酮拮抗了所测试的每种阿片类药物的抑制作用,而右旋啡烷,一种无活性的L-(+)-阿片,未能抑制多巴胺反应。这些数据共同表明,这些效应是通过经典描述的立体特异性阿片受体介导的。效价的相对顺序(埃托啡>脑啡肽>吗啡)与先前报道的这些药物在大鼠脑匀浆中的结合亲和力顺序相似。通过冷冻杏仁核组织或将匀浆在4℃预孵育,可消除麻醉剂对多巴胺刺激的AC的影响;然而,多巴胺反应仍可被引发。因此,阿片受体与腺苷酸环化酶的相互作用似乎与多巴胺受体的相互作用不同,且更不稳定。Gpp(NH)p刺激的AC不受吗啡抑制。据推测,这种抑制涉及阿片受体与多巴胺刺激的AC的催化单元相互作用,但不与可能提供杏仁核中Gpp(NH)p刺激活性主要成分的其他环化酶种类相互作用。