ANTINOCICEPTIVE EFFECTS OF CA2+ CHANNEL BLOCKERS

被引:114
作者
MIRANDA, HF
BUSTAMANTE, D
KRAMER, V
PELISSIER, T
SAAVEDRA, H
PAEILE, C
FERNANDEZ, E
PINARDI, G
机构
[1] Department of Pharmacology, Faculty of Medicine, Universidad de Chile, Santiago, 7
关键词
ANTINOCICEPTION; FORMALIN TEST; WRITHING TEST; HOT-PLATE TEST; CA2+ CHANNEL BLOCKERS;
D O I
10.1016/0014-2999(92)90833-P
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The antinociceptive action of four Ca2+ channel blockers, nifedipine, nimodipine, verapamil and diltiazem, was evaluated and compared to that of morphine using three algesiometric tests in mice and rats, namely, formalin, writhing and modified hot-plate test. Dose-response curves for all the drugs tested were similar and a significant dose-dependent antinociceptive action was evident in the formalin and writhing tests. However, in the hot-plate test, only nimodipine exhibited a significant analgesic effect, confirming the misleading results previously reported for this test. The findings suggest a pharmacological role of Ca2+ channel blockers in the modulation of antinociception under acute conditions. The analgesic action of Ca2+ channel blockers could be mediated by an increase in the nociceptive threshold resulting from interference with Ca2+ influx at opioid receptors, because Ca2+ influx is critical for the release of neurotransmitters and other substances implicated in nociception and inflammation. It is suggested that if a substance has a Ca2+ channel blocking effect, it should probably have some antinociceptive properties.
引用
收藏
页码:137 / 141
页数:5
相关论文
共 33 条
[1]   NEW HOT PLATE TESTS TO QUANTIFY ANTINOCICEPTIVE AND NARCOTIC-ANTAGONIST ACTIVITIES [J].
ANKIER, SI .
EUROPEAN JOURNAL OF PHARMACOLOGY, 1974, 27 (01) :1-4
[2]   POTENTIATION OF THERMOREGULATORY AND ANALGESIC EFFECTS OF MORPHINE BY CALCIUM-ANTAGONISTS [J].
BENEDEK, G ;
SZIKSZAY, M .
PHARMACOLOGICAL RESEARCH COMMUNICATIONS, 1984, 16 (10) :1009-1018
[3]   EFFECTS OF ELEVATED CALCIUM AND CALCIUM-ANTAGONISTS ON 6,7-BENZOMORPHAN-INDUCED ANALGESIA [J].
BENSRETI, MM ;
GONZALEZ, JP ;
SEWELL, RDE .
EUROPEAN JOURNAL OF PHARMACOLOGY, 1983, 90 (04) :385-391
[4]   ANALGESIC ACTION OF CLONIXIN, NIFEDIPINE AND MORPHINE USING THE FORMALIN TEST [J].
BUSTAMANTE, D ;
MIRANDA, HF ;
PELISSIER, T ;
PAEILE, C .
GENERAL PHARMACOLOGY, 1989, 20 (03) :319-322
[5]   MODIFICATION OF ENDORPHIN ENKEPHALIN ANALGESIA AND STRESS-INDUCED ANALGESIA BY DIVALENT-CATIONS, A CATION CHELATOR AND AN IONOPHORE [J].
CHAPMAN, DB ;
WAY, EL .
BRITISH JOURNAL OF PHARMACOLOGY, 1982, 75 (02) :389-396
[6]   CALCIUM-CHANNEL ANTAGONISTS INCREASE MORPHINE-INDUCED ANALGESIA AND ANTAGONIZE MORPHINE-TOLERANCE [J].
CONTRERAS, E ;
TAMAYO, L ;
AMIGO, M .
EUROPEAN JOURNAL OF PHARMACOLOGY, 1988, 148 (03) :463-466
[7]   ANALGESIC EFFECTS OF SEVERAL CALCIUM-CHANNEL BLOCKERS IN MICE [J].
DELPOZO, E ;
CARO, G ;
BAEYENS, JM .
EUROPEAN JOURNAL OF PHARMACOLOGY, 1987, 137 (2-3) :155-160
[8]   ANALGESIC EFFECTS OF DILTIAZEM AND VERAPAMIL AFTER CENTRAL AND PERIPHERAL ADMINISTRATION IN THE HOT-PLATE TEST [J].
DELPOZO, E ;
RUIZGARCIA, C ;
BAEYENS, JM .
GENERAL PHARMACOLOGY, 1990, 21 (05) :681-685
[9]   FORMALIN TEST - QUANTITATIVE STUDY OF ANALGESIC EFFECTS OF MORPHINE, MEPERIDINE, AND BRAIN-STEM STIMULATION IN RATS AND CATS [J].
DUBUISSON, D ;
DENNIS, SG .
PAIN, 1977, 4 (02) :161-174
[10]  
GILBERT R, 1989, BRIT J PHARMACOL, V96, pP240