Pharmacology of cizolirtine:: A new analgesic agent

被引:16
作者
Alvarez, I [1 ]
Andreu, F [1 ]
Buxens, J [1 ]
Colombo, M [1 ]
Dordal, A [1 ]
Fort, M [1 ]
Gutiérrez, B [1 ]
Farré, AJ [1 ]
机构
[1] Labs Dr Esteve SA, Dept Res, Barcelona 08026, Spain
来源
METHODS AND FINDINGS IN EXPERIMENTAL AND CLINICAL PHARMACOLOGY | 2000年 / 22卷 / 04期
关键词
nonopioid analgesic;
D O I
10.1358/mf.2000.22.4.584453
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Cizolirtine citrate (E-4018) is a new analgesic agent with antinociceptive activity against phenylquinone (ED50 33.7 mg/kg) and acetic acid (ED50 24.4 mg/kg) in mice, against acetic acid in rats (ED50 21.3 mg/kg) and in the plantar test (ED50 26.8 mg/kg). It demonstrated antinociceptive activity in the mil-pinch and rail-Slick tests (ED(50)s of 68.0 and 46.0 mg/kg, respectively), in both phases of the formalin lest (ED50 13.8 and 2.31 mg/kg), and in the capsaicin rest (ED50 7.14 mg/kg). Cizolirtine does not inhibit prostaglandin biosynthesis, it is not a ligand for opioid receptors, it does not have antiinflammatory or ulcerogenic activity ii has some antipyretic activity and shows no affinity for alpha(2)-adrenergic receptors, but its analgesic effect Mas modified by idazoxan and by desipramine. Recent studies have shown that the analgesic effect of cizolirtine could be related at least partially, to an inhibition of spinal substance P release. (C)2000 Prous Science. All rights reserved.
引用
收藏
页码:211 / 221
页数:11
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