HUMAN DELTA-OPIOID RECEPTOR - A STABLE CELL-LINE FOR FUNCTIONAL-STUDIES OF OPIOIDS

被引:28
作者
MALATYNSKA, E
WANG, Y
KNAPP, RJ
SANTORO, G
LI, XP
WAITE, S
ROESKE, WR
YAMAMURA, HI
机构
[1] UNIV ARIZONA,DEPT BIOCHEM,TUCSON,AZ 85724
[2] UNIV ARIZONA,DEPT MED,TUCSON,AZ 85724
[3] UNIV ARIZONA,DEPT PSYCHIAT,TUCSON,AZ 85724
[4] UNIV ARIZONA,ARIZONA HLTH SCI CTR,TUCSON,AZ 85724
关键词
STABLE EXPRESSION; TRANSFECTION; CHO CELLS; HUMAN DELTA OPIOID RECEPTOR; NALTRINDOLE; DPDPE; RADIOLIGAND BINDING; CAMP; ADENYLYL CYCLASE;
D O I
10.1097/00001756-199503000-00007
中图分类号
Q189 [神经科学];
学科分类号
071006 ;
摘要
A HUMAN delta opioid receptor cDNA clone (pREP10/hDOR) was transfected into Chinese hamster ovary (CHO) cells. The stable cell line expressed a high density of delta opioid receptors (137 000 +/- 21 600 receptors/cell). DPDPE inhibited 90% of the forskolin-stimulated cAMP accumulation in these cells with high potency (EC(50) = 1.3 nM). This effect of DPDPE was antagonized by naltrindole. The pseudo-pA(2) value (K-e) of 155 pM for naltrindole is consistent with that measured for delta receptor antagonism in the mouse vas deferens. This is the first detailed characterization of DPDPE activity on forskolin-stimulated cAMP accumulation mediated through a human delta opioid receptor. The data support the use of the recombinant cell line for functional studies of opioid drugs.
引用
收藏
页码:613 / 616
页数:4
相关论文
共 14 条
  • [1] CHARACTERIZATION OF [H-3][ 2-D-PENICILLAMINE, 5-D-PENICILLAMINE] ENKEPHALIN BINDING TO DELTA-OPIATE RECEPTORS IN THE RAT-BRAIN AND NEUROBLASTOMA-GLIOMA HYBRID CELL-LINE (NG-108-15)
    AKIYAMA, K
    GEE, KW
    MOSBERG, HI
    HRUBY, VJ
    YAMAMURA, HI
    [J]. PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1985, 82 (08) : 2543 - 2547
  • [2] OPIOID RECEPTOR-COUPLED 2ND MESSENGER SYSTEMS
    CHILDERS, SR
    [J]. LIFE SCIENCES, 1991, 48 (21) : 1991 - 2003
  • [3] ICI-174864 - A HIGHLY SELECTIVE ANTAGONIST FOR THE OPIOID DELTA-RECEPTOR
    COTTON, R
    GILES, MG
    MILLER, L
    SHAW, JS
    TIMMS, D
    [J]. EUROPEAN JOURNAL OF PHARMACOLOGY, 1984, 97 (3-4) : 331 - 332
  • [4] FANG L, 1994, J PHARMACOL EXP THER, V268, P836
  • [6] KENAKIN T, 1993, PHARM ANAL DRUG RECE, P46
  • [7] IDENTIFICATION OF A HUMAN DELTA-OPIOID RECEPTOR - CLONING AND EXPRESSION
    KNAPP, RJ
    MALATYNSKA, E
    FANG, L
    LI, XP
    BABIN, E
    NGUYEN, M
    SANTORO, G
    VARGA, EV
    HRUBY, VJ
    ROESKE, WR
    YAMAMURA, HI
    [J]. LIFE SCIENCES, 1994, 54 (25) : PL463 - PL469
  • [8] AMPLIFICATION OF THE RAT M2 MUSCARINIC RECEPTOR GENE BY THE POLYMERASE CHAIN-REACTION - FUNCTIONAL EXPRESSION OF THE M2 MUSCARINIC RECEPTOR
    LAI, J
    BLOOM, JW
    YAMAMURA, HI
    ROESKE, WR
    [J]. LIFE SCIENCES, 1990, 47 (12) : 1001 - 1013
  • [9] CLONING, EXPRESSION AND PARTIAL CHARACTERIZATION OF A HUMAN DELTA-OPIOID RECEPTOR
    MALATYNSKA, E
    KNAPP, RJ
    FANG, L
    LI, X
    WANG, Y
    SANTORO, G
    DELEON, I
    WAITE, S
    ROESKE, WR
    YAMAMURA, HI
    [J]. REGULATORY PEPTIDES, 1994, 54 (01) : 173 - 174
  • [10] MEI L, 1989, J PHARMACOL EXP THER, V248, P661