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＝０１９±００５ｎｍｏｌ·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７８７ｎｍｏｌ·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.
出处
《中国药理学报》
CSCD
1996年第3期281-283,共3页
Acta Pharmacologica Sinica
关键词
二氢埃托啡
阿片受体
脑
放射配体
dihydroetorphine
opioidreceptors
brain
radioligandassay
