EVIDENCE THAT BETA-ENDORPHIN IS AN AGONIST AT BOVINE PINEAL DELTA-OPIOID RECEPTORS

被引:6
作者
ALOYO, VJ
PAZDALSKI, PS
机构
[1] Department of Pharmacology, Medical College of Pennsylvania, Philadelphia, PA
来源
EUROPEAN JOURNAL OF PHARMACOLOGY-MOLECULAR PHARMACOLOGY SECTION | 1995年 / 288卷 / 03期
关键词
PINEAL GLAND; BOVINE; BETA-ENDORPHIN; DELTA-OPIOID RECEPTOR; EPSILON-OPIOID RECEPTOR;
D O I
10.1016/0922-4106(95)90041-1
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Since beta-endorphin is the putative endogenous ligand for epsilon-opioid receptors, the previous demonstration of saturable, high affinity beta-endorphin binding sites on bovine pineal membranes suggests the possible presence of epsilon-opioid receptors. To determine the identity of pineal beta-endorphin binding sites, the inhibition of [I-125]beta-endorphin binding by ligands with varying affinities for epsilon-, mu-, delta- or kappa-opioid receptors was investigated. A high positive correlation was observed between the K-i values for these drugs to inhibit [I-125]beta-endorphin binding to pineal membranes and for these drugs to bind to delta-opioid receptors but not to mu-, kappa- or epsilon-opioid receptors, demonstrating that in the pineal beta-endorphin binds to delta-opioid receptors. Both NaCl and a GTP analogue were potent inhibitors of [I-125]beta-endorphin binding, providing evidence that beta-endorphin is an agonist at pineal delta-opioid receptors. These results suggest that endogenous bovine beta-endorphin may modulate pineal function.
引用
收藏
页码:295 / 301
页数:7
相关论文
共 40 条
  • [1] ALOYO VJ, 1992, J PHARMACOL EXP THER, V262, P292
  • [2] RECEPTOR-EFFECTOR COUPLING BY G-PROTEINS
    BIRNBAUMER, L
    ABRAMOWITZ, J
    BROWN, AM
    [J]. BIOCHIMICA ET BIOPHYSICA ACTA, 1990, 1031 (02) : 163 - 224
  • [3] DIFFERENTIAL REGULATION BY GUANINE-NUCLEOTIDES OF OPIATE AGONIST AND ANTAGONIST RECEPTOR INTERACTIONS
    CHILDERS, SR
    SNYDER, SH
    [J]. JOURNAL OF NEUROCHEMISTRY, 1980, 34 (03) : 583 - 593
  • [4] EHLERT FJ, 1988, MOL PHARMACOL, V33, P187
  • [5] CLONING OF A DELTA OPIOID RECEPTOR BY FUNCTIONAL EXPRESSION
    EVANS, CJ
    KEITH, DE
    MORRISON, H
    MAGENDZO, K
    EDWARDS, RH
    [J]. SCIENCE, 1992, 258 (5090) : 1952 - 1955
  • [6] BETA-ENDORPHIN - CHARACTERISTICS OF BINDING-SITES IN THE RAT-BRAIN
    FERRARA, P
    HOUGHTEN, R
    LI, CH
    [J]. BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, 1979, 89 (03) : 786 - 792
  • [7] GOLDSTEIN A, 1989, MOL PHARMACOL, V36, P265
  • [8] HAWKINS KN, 1989, J PHARMACOL EXP THER, V248, P73
  • [9] Hays WL, 1963, STAT PSYCHOLOGISTS
  • [10] SPECIFIC NON-OPIATE RECEPTORS FOR BETA-ENDORPHIN
    HAZUM, E
    CHANG, KJ
    CUATRECASAS, P
    [J]. SCIENCE, 1979, 205 (4410) : 1033 - 1035