CAPSAZEPINE AS A SELECTIVE ANTAGONIST OF CAPSAICIN-INDUCED ACTIVATION OF C-FIBERS IN GUINEA-PIG BRONCHI

被引:49
作者
BELVISI, MG
MIURA, M
STRETTON, D
BARNES, PJ
机构
[1] Department of Thoracic Medicine, National Heart and Lung Institute, London, SW3 6LY, Dovehouse Street, Chelsea
关键词
CAPSAZEPINE; NONADRENERGIC NONCHOLINERGIC (NANC) EXCITATORY NERVES; CAPSAICIN; ELECTRICAL FIELD STIMULATION; TETRODOTOXIN;
D O I
10.1016/0014-2999(92)90054-8
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
We investigated the action of capsazepine, an antagonist of the actions of capsaicin on sensory neurones, on the contractile responses evoked by capsaicin or by electrical field stimulation (EFS) in guinea-pig bronchi. Capsazepine (10(-5) M) selectively inhibited responses to capsaicin, producing a significant change in EC50 values but not the Hill coefficient (n(H)), suggesting that capsazepine acts as a competitive antagonist (apparent pK(B) = 5.12) whereas ruthenium red is a non-competitive antagonist. Capsazepine and ruthenium red were without effect on EFS-induced responses.
引用
收藏
页码:341 / 344
页数:4
相关论文
共 9 条
[1]   RUTHENIUM RED SELECTIVELY INHIBITS CAPSAICIN-INDUCED RELEASE OF CALCITONIN GENE-RELATED PEPTIDE FROM THE ISOLATED PERFUSED GUINEA-PIG LUNG [J].
AMANN, R ;
DONNERER, J ;
LEMBECK, F .
NEUROSCIENCE LETTERS, 1989, 101 (03) :311-315
[2]  
BEVAN S, 1990, TRENDS PHARMACOL SCI, V11, P330
[3]  
Bevan S., 1991, BRIT J PHARMACOL, V102
[4]   SELECTIVE ANTAGONISM OF CAPSAICIN BY CAPSAZEPINE - EVIDENCE FOR A SPINAL RECEPTOR-SITE IN CAPSAICIN-INDUCED ANTINOCICEPTION [J].
DICKENSON, AH ;
DRAY, A .
BRITISH JOURNAL OF PHARMACOLOGY, 1991, 104 (04) :1045-1049
[5]  
Dray A., 1991, BRIT J PHARMACOL, V102
[6]   SELECTIVITY OF RUTHENIUM RED IN INHIBITING BRONCHOCONSTRICTION AND CGRP RELEASE INDUCED BY AFFERENT C-FIBER ACTIVATION IN THE GUINEA-PIG LUNG [J].
LOU, YP ;
KARLSSON, JA ;
FRANCOCERECEDA, A ;
LUNDBERG, JM .
ACTA PHYSIOLOGICA SCANDINAVICA, 1991, 142 (02) :191-199
[7]  
LUNDBERG JM, 1987, ANNU REV PHYSIOL, V49, P557
[8]   BRONCHIAL SMOOTH-MUSCLE CONTRACTION INDUCED BY STIMULATION OF CAPSAICIN-SENSITIVE SENSORY NEURONS [J].
LUNDBERG, JM ;
SARIA, A .
ACTA PHYSIOLOGICA SCANDINAVICA, 1982, 116 (04) :473-476
[9]   THE EFFERENT FUNCTION OF CAPSAICIN-SENSITIVE NERVES - RUTHENIUM RED DISCRIMINATES BETWEEN DIFFERENT MECHANISMS OF ACTIVATION [J].
MAGGI, CA ;
PATACCHINI, R ;
SANTICIOLI, P ;
GIULIANI, S ;
DELBIANCO, E ;
GEPPETTI, P ;
MELI, A .
EUROPEAN JOURNAL OF PHARMACOLOGY, 1989, 170 (03) :167-177