NONSPECIFIC ACTIVITY OF (+/-)-CP-96,345 IN MODELS OF PAIN AND INFLAMMATION

被引:53
作者
NAGAHISA, A
ASAI, R
KANAI, Y
MURASE, A
TSUCHIYANAKAGAKI, M
NAKAGAKI, T
SHIEH, TC
TANIGUCHI, K
机构
[1] Department of Medicinal Biology, Central Research Division, Pfizer Inc., Taketoyo, Aichi, 470-23
关键词
CP-96,345; NONPEPTIDE NK1-RECEPTOR ANTAGONIST; PAIN; INFLAMMATION;
D O I
10.1111/j.1476-5381.1992.tb12737.x
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The non-peptide NK1 receptor antagonist, CP-96,345, and its 2R,3R enantiomer CP-96,344, which is not an NK1 receptor antagonist (IC50 > 10 muM), were evaluated for antinociceptive and anti-inflammatory activities in several classical models of pain and inflammation in the rat. Both CP-96,345 and CP-96,344 reduced carrageenin-induced paw oedema and hyperalgesia, and attenuated the second phase of formalin-induced paw licking with equal potency. These results indicate that NK1 antagonism is not responsible for the activity of (+/-)-CP-96,345 in the above animal models.
引用
收藏
页码:273 / 275
页数:3
相关论文
共 9 条
[1]   THE NONPEPTIDE NK1 RECEPTOR ANTAGONIST, (+/-)-CP-96,345, PRODUCES ANTINOCICEPTIVE AND ANTI-EDEMA EFFECTS IN THE RAT [J].
BIRCH, PJ ;
HARRISON, SM ;
HAYES, AG ;
ROGERS, H ;
TYERS, MB .
BRITISH JOURNAL OF PHARMACOLOGY, 1992, 105 (03) :508-510
[2]  
CONSTANTINE JW, 1991, N-S ARCH PHARMACOL, V344, P471
[3]   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
[4]   ROLE OF NK1 TACHYKININ RECEPTORS IN THERMONOCICEPTION - EFFECT OF (+/-)-CP 96,345, A NONPEPTIDE SUBSTANCE-P ANTAGONIST, ON THE HOT PLATE TEST IN MICE [J].
LECCI, A ;
GIULIANI, S ;
PATACCHINI, R ;
VITI, G ;
MAGGI, CA .
NEUROSCIENCE LETTERS, 1991, 129 (02) :299-302
[5]   THE NONPEPTIDE TACHYKININ ANTAGONIST, CP-96,345, IS A POTENT INHIBITOR OF NEUROGENIC INFLAMMATION [J].
LEMBECK, F ;
DONNERER, J ;
TSUCHIYA, M ;
NAGAHISA, A .
BRITISH JOURNAL OF PHARMACOLOGY, 1992, 105 (03) :527-530
[6]  
LOWE JA, 1990, J MED CHEM, V35, P2591
[7]   ANTIINFLAMMATORY AND ANALGESIC ACTIVITY OF A NONPEPTIDE SUBSTANCE-P RECEPTOR ANTAGONIST [J].
NAGAHISA, A ;
KANAI, Y ;
SUGA, O ;
TANIGUCHI, K ;
TSUCHIYA, M ;
LOWE, JA ;
HESS, HJ .
EUROPEAN JOURNAL OF PHARMACOLOGY, 1992, 217 (2-3) :191-195
[8]   THE SUBSTANCE-P RECEPTOR ANTAGONIST CP-96,345 INTERACTS WITH CA2+ CHANNELS [J].
SCHMIDT, AW ;
MCLEAN, S ;
HEYM, J .
EUROPEAN JOURNAL OF PHARMACOLOGY, 1992, 215 (2-3) :351-352
[9]   A POTENT NONPEPTIDE ANTAGONIST OF THE SUBSTANCE-P (NK1) RECEPTOR [J].
SNIDER, RM ;
CONSTANTINE, JW ;
LOWE, JA ;
LONGO, KP ;
LEBEL, WS ;
WOODY, HA ;
DROZDA, SE ;
DESAI, MC ;
VINICK, FJ ;
SPENCER, RW ;
HESS, HJ .
SCIENCE, 1991, 251 (4992) :435-437