Búzás B, Izenwasser S, Portoghese P S, Cox B M
Dept. of Pharmacology, Uniformed Services University, Bethesda, MD 20814.
Life Sci. 1994;54(7):PL101-6. doi: 10.1016/0024-3205(94)00412-9.
Opioid agonists selective for mu- or delta opioid receptors inhibit adenylyl cyclase in membranes from rat caudate-putamen and nucleus accumbens. The presence of subtypes of delta opioid receptors has been suggested. In both brain regions we have found that the inhibition of adenylyl cyclase by DPDPE was more readily antagonized by 7-benzylidenenaltrexone (BNTX), than by naltriben. In contrast, the inhibitory effects of deltorphin-II and DSLET were more readily antagonized by naltriben, than by BNTX. Neither naltriben nor BNTX significantly antagonized the effect of a mu selective agonist. These results suggest that inhibition of adenylyl cyclase in caudate-putamen and nucleus accumbens is regulated by two forms of delta-opioid receptor with ligand selectivities similar to those two forms proposed to mediate analgesic effect.
对μ或δ阿片受体有选择性的阿片类激动剂可抑制大鼠尾状核-壳核和伏隔核膜中的腺苷酸环化酶。有人提出存在δ阿片受体亚型。在这两个脑区,我们发现7-苄叉基纳曲酮(BNTX)比纳曲苄更易拮抗DPDPE对腺苷酸环化酶的抑制作用。相反,纳曲苄比BNTX更易拮抗强啡肽-II和DSLET的抑制作用。纳曲苄和BNTX均未显著拮抗μ选择性激动剂的作用。这些结果表明,尾状核-壳核和伏隔核中腺苷酸环化酶的抑制作用由两种δ阿片受体形式调节,其配体选择性类似于被认为介导镇痛作用的那两种形式。