Affinity of neuropeptide FF analogs to opioid receptors in the rat spinal cord

被引:35
作者
Gouardères, C
Tafani, JAM
Zajac, JM
机构
[1] CNRS, Inst Pharmacol & Biol Struct, F-31077 Toulouse, France
[2] CHU Purpan, Serv Biophys & Med Nucl, Toulouse, France
关键词
neuropeptide FF; opioid; receptor; spinal cord; autoradiography; rat;
D O I
10.1016/S0196-9781(98)00015-1
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
Several high-affinity analogs of neuropeptide FF (Phe-Leu-Phe-Gln-Pro-Gln-Arg-Phe-NH2, NPFF) exhibiting both supraspinal anti-opioid and spinal analgesic activities were studied for their abilities to interact with specific mu, delta, and kappa opioid binding in the rat spinal cord. Measurements by quantitative receptor autoradiography in the superficial layers of the spinal cord revealed that NPFF analogs tested have only a low affinity for opioid receptors since K-i values ranged from 5 to 400 mu M. Taking into account the high efficacy of NPFF after intrathecal injection, these results indicate that analgesic effects of NPFF did not result from opioid receptor stimulation. (C) 1998 Elsevier Science Inc.
引用
收藏
页码:727 / 730
页数:4
相关论文
共 20 条
[1]   AUTORADIOGRAPHIC DISTRIBUTION OF RECEPTORS TO FLFQPQRFAMIDE, A MORPHINE-MODULATING PEPTIDE, IN RAT CENTRAL-NERVOUS-SYSTEM [J].
ALLARD, M ;
ZAJAC, JM ;
SIMONNET, G .
NEUROSCIENCE, 1992, 49 (01) :101-116
[2]   OPIOID AND ANTI-OPIOID PEPTIDES [J].
CESSELIN, F .
FUNDAMENTAL & CLINICAL PHARMACOLOGY, 1995, 9 (05) :409-433
[3]   ONTOGENY OF NEUROPEPTIDE FF PHARMACOLOGY AND RECEPTORS IN MOUSE-BRAIN [J].
DESPRAT, C ;
ZAJAC, JM .
DEVELOPMENTAL BRAIN RESEARCH, 1994, 82 (1-2) :118-126
[4]   (I-125)[D-ALA2]DELTORPHIN-I - A HIGH-AFFINITY, DELTA-SELECTIVE OPIOID RECEPTOR LIGAND [J].
DUPIN, S ;
TAFANI, JAM ;
MAZARGUIL, H ;
ZAJAC, JM .
PEPTIDES, 1991, 12 (04) :825-830
[5]  
Dupouy V, 1996, SYNAPSE, V24, P282, DOI 10.1002/(SICI)1098-2396(199611)24:3<282::AID-SYN11>3.0.CO
[6]  
2-Z
[7]   EFFECTS OF NEUROPEPTIDE FF ANALOGS ON MORPHINE ANALGESIA IN THE NUCLEUS RAPHE DORSALIS [J].
DUPOUY, V ;
ZAJAC, JM .
REGULATORY PEPTIDES, 1995, 59 (03) :349-356
[8]   Neuropeptide FF receptors control morphine-induced analgesia in the parafascicular nucleus and the dorsal raphe nucleus [J].
Dupouy, V ;
Zajac, JM .
EUROPEAN JOURNAL OF PHARMACOLOGY, 1997, 330 (2-3) :129-137
[9]   ANALOGS OF F8FAMIDE RESISTANT TO DEGRADATION, WITH HIGH-AFFINITY AND INVIVO EFFECTS [J].
GICQUEL, S ;
MAZARGUIL, H ;
ALLARD, M ;
SIMONNET, G ;
ZAJAC, JM .
EUROPEAN JOURNAL OF PHARMACOLOGY, 1992, 222 (01) :61-67
[10]   Autoradiographic characterization of rat spinal neuropeptide FF receptors by using [I-125][D.Tyr(1), (NMe)Phe(3)]NPFF [J].
Gouarderes, C ;
Tafani, JAM ;
Mazarguil, H ;
Zajac, JM .
BRAIN RESEARCH BULLETIN, 1997, 42 (03) :231-238