（^3H）二氢埃托啡与大鼠脑膜阿片受体的结合  

Bindingof[3H]dihydroetorphinetoopioidrecep torsinratbrainmembrane

作　　者：王丹心[1] 秦伯益[1] 

机构地区：[1]军事医学科学院毒物药物研究所

出　　处：《中国药理学报》1996年第3期281-283,共3页Acta Pharmacologica Sinica

摘　　要：目的：观察二氢埃托啡（ＤＨＥ）与阿片受体的结合情况．方法：采用放射配体受体结合实验，观察了［３Ｈ］ＤＨＥ与大鼠脑膜阿片受体的结合．结果：饱和实验显示［３Ｈ］ＤＨＥ的结合呈高亲和力单一位点，Ｋｄ＝０１９±００５ｎｍｏｌ·Ｌ－１，Ｂｍａｘ＝１１５±２１ｐｍｏｌ／ｇｐｒｏｔｅｉｎ．动力学实验表明［３Ｈ］ＤＨＥ与阿片受体结合极快，解离很慢．ＮａＣｌ１００ｍｍｏｌ·Ｌ－１＋鸟苷三磷酸（ＧＴＰ）５０μｍｏｌ·Ｌ－１可使［３Ｈ］ＤＨＥ的Ｋｄ值提高为７８７ｎｍｏｌ·Ｌ－１，Ｂｍａｘ值不变．激动剂和拮抗剂的竞争抑制实验均表明［３Ｈ］ＤＨＥ与μ阿片受体的亲和力大于δ和κ受体．结论：ＤＨＥ对μ阿片受体具有一定选择性．IM:Tostudythebindingcharacteristicsofdihydroetorphine(DH E)toopioidreceptors.METHODS:Thebindingof[3H]DHEtoratbrainmembraneopio idreceptorswasobservedbyradioligandbindingstudy.RESULTS:Saturationstu dyshowedthebindingof[3H]DHEtoratbrainmembranepresentedasinglehigh afinityclassofbindingsiteswithKd=0 19nmol·L-1andBmax=115pmol/gprotein.Kineticsstudyshowedtheassociation rateof[3H]DHEtoopioidreceptorwasveryrapidanddissociationveryslow.NaCl 100mmol·L-1+guanosinetriphosphate(GTP)50μ mol·L-1inhibitedthebindingof[3H]DHEandmadeKdincreaseto7 87nmol·L-1,withoutefectonBmax.Competitiveinhibitionofagonistsandanta gonistsindicatedthattheafinityof[3H]DHEtoμ opioidreceptorwashigherthantoδandκ opioidreceptors.CONCLUSION:DHEisaselectiveagonistofμopioidreceptors.

关 键 词：二氢埃托啡 阿片受体 脑 放射配体 

分 类 号：R966[医药卫生—药理学] R971.1[医药卫生—药学]