Creese I, Snyder S H
J Pharmacol Exp Ther. 1975 Jul;194(1):205-19.
A comparison was made between the affinities of a wide range of opiate agonists, mixed agonist-antagonists and antagonists for opiate receptor binding sites in the guniea-pig intestine longitudinal muscle and myenteric plexus preparation, and their pharmacological potency in influencing the electrically induced contraction of this in vitro functional system. The relative affinities of drugs and the degree of stereospecificity for intestinal binding sites are closely similar to these properties in the brain. Receptor binding correlates extremely well with pharmacological potency, both for agonists and antagonists, indicating that binding involves pharmacologically relevant opiate receptors. Pharmacological activity correlates best with receptor binding assayed in the presence of sodium.
对一系列阿片类激动剂、混合激动-拮抗剂和拮抗剂与豚鼠肠纵肌和肠肌丛制剂中阿片受体结合位点的亲和力，以及它们影响该体外功能系统电诱导收缩的药理效力进行了比较。药物的相对亲和力和对肠道结合位点的立体特异性程度与大脑中的这些特性非常相似。受体结合与激动剂和拮抗剂的药理效力都高度相关，表明结合涉及药理学相关的阿片受体。药理活性与在有钠存在的情况下测定的受体结合相关性最佳。
