Evidence that [Phe1 ψ (CH2-NH)Gly2]nociceptin-(1-13)-NH2, a peripheral ORL-1 receptor antagonist, acts as an agonist in the rat spinal cord

被引:55
作者
Carpenter, KJ [1 ]
Dickenson, AH [1 ]
机构
[1] Univ London Univ Coll, Dept Pharmacol, London WC1E 6BT, England
关键词
nociceptin; spinal cord; ORL-1; receptor; antinociception;
D O I
10.1038/sj.bjp.0702188
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
[Phe(1) psi(CH2-NH)Gly(2)]nociceptin-(1-13)-NH2, a pseudopeptide analogue of nociceptin is an antagonist in peripheral assays. Here, using in vivo electrophysiological recordings of dorsal horn neurones, [Phe(1) psi(CH2-NH)Gly(2)]nociceptin-(1-13)-NH2 appears to have agonist activity after spinal administration. The noxious evoked activity of the neurones was inhibited by [Phe(1) psi(CH2-NH)Gly(2)]nociceptin-(1-13)-NH2, which was as potent as nociceptin itself.
引用
收藏
页码:949 / 951
页数:3
相关论文
共 11 条
[1]  
Anton B, 1996, J COMP NEUROL, V368, P229
[2]  
BUTOR JL, 1998, IN PRESS EUR J PHARM
[3]  
DICKENSON AH, 1987, BRAIN RES, V413, P44
[4]   A new selective antagonist of the nociceptin receptor [J].
Guerrini, R ;
Calo, G ;
Rizzi, A ;
Bigoni, R ;
Bianchi, C ;
Salvadori, S ;
Regoli, D .
BRITISH JOURNAL OF PHARMACOLOGY, 1998, 123 (02) :163-165
[5]   Biochemical evidence for orphanin FQ/nociceptin receptor heterogeneity in mouse brain [J].
Mathis, JP ;
RyanMoro, J ;
Chang, A ;
Hom, JSH ;
Scheinberg, DA ;
Pasternak, GW .
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, 1997, 230 (02) :462-465
[6]   Nociceptin/orphanin FQ and the opioid receptor-like ORL1 receptor [J].
Meunier, JC .
EUROPEAN JOURNAL OF PHARMACOLOGY, 1997, 340 (01) :1-15
[7]   Distribution of nociceptin orphanin FQ receptor transcript in human central nervous system and immune cells [J].
Peluso, J ;
LaForge, KS ;
Matthes, HW ;
Kreek, MJ ;
Kieffer, BL ;
Gavériaux-Ruff, C .
JOURNAL OF NEUROIMMUNOLOGY, 1998, 81 (1-2) :184-192
[8]   ORPHANIN-FQ - A NEUROPEPTIDE THAT ACTIVATES AN OPIOID-LIKE G-PROTEIN-COUPLED RECEPTOR [J].
REINSCHEID, RK ;
NOTHACKER, HP ;
BOURSON, A ;
ARDATI, A ;
HENNINGSEN, RA ;
BUNZOW, JR ;
GRANDY, DK ;
LANGEN, H ;
MONSMA, FJ ;
CIVELLI, O .
SCIENCE, 1995, 270 (5237) :792-794
[9]   Inhibitory action of nociceptin on spinal dorsal horn neurones of the rat, in vivo [J].
Stanfa, LC ;
Chapman, V ;
Kerr, N ;
Dickenson, AH .
BRITISH JOURNAL OF PHARMACOLOGY, 1996, 118 (08) :1875-1877
[10]   ISOLATION OF A NOVEL CDNA-ENCODING A PUTATIVE MEMBRANE-RECEPTOR WITH HIGH HOMOLOGY TO THE CLONED MU-OPIOID, DELTA-OPIOID, AND KAPPA-OPIOID RECEPTORS [J].
WICK, MJ ;
MINNERATH, SR ;
LIN, XQ ;
ELDE, R ;
LAW, PY ;
LOH, HH .
MOLECULAR BRAIN RESEARCH, 1994, 27 (01) :37-44