Chain-branched acyclic phenethylthiocarbamates as vanilloid receptor antagonists

被引:18
作者
Yoon, J
Choi, H
Lee, HJ
Ryu, CH
Park, HG
Suh, YG
Oh, U
Jeong, YS
Choi, JK
Park, YH
Kim, HD
机构
[1] Sookmyung Womens Univ, Coll Pharm, Yongsan Ku, Seoul 140742, South Korea
[2] Seoul Natl Univ, Coll Pharm, Seoul 151742, South Korea
[3] AmorePacific R & D Ctr, Youngin Si 449900, Kyounggi Do, South Korea
关键词
D O I
10.1016/S0960-894X(03)00178-1
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A series of acyclic phenethylthiocarbamate derivatives have been synthesized, and their antagonist effect against vanilloid receptor tested. Chain branching led to a significant change in antagonist activity of the parent molecule. Ethyl-branched le showed a 6.3 muM Of IC50 value in Ca-45(2+)-influx assay. (C) 2003 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:1549 / 1552
页数:4
相关论文
共 21 条
[1]   The capsaicin receptor: a heat-activated ion channel in the pain pathway [J].
Caterina, MJ ;
Schumacher, MA ;
Tominaga, M ;
Rosen, TA ;
Levine, JD ;
Julius, D .
NATURE, 1997, 389 (6653) :816-824
[2]  
CULSHAW AJ, 2002, Patent No. 0276946
[3]   Capsazepine block of voltage-activated calcium channels in adult rat dorsal root ganglion neurones in culture [J].
Docherty, RJ ;
Yeats, JC ;
Piper, AS .
BRITISH JOURNAL OF PHARMACOLOGY, 1997, 121 (07) :1461-1467
[4]   NE-19550 AND NE-21610, ANTINOCICEPTIVE CAPSAICIN ANALOGS - STUDIES ON NOCICEPTIVE FIBERS OF THE NEONATAL RAT TAIL INVITRO [J].
DRAY, A ;
BETTANEY, J ;
RUEFF, A ;
WALPOLE, C ;
WRIGGLESWORTH, R .
EUROPEAN JOURNAL OF PHARMACOLOGY, 1990, 181 (03) :289-293
[5]   ACTIONS OF CAPSAICIN ON PERIPHERAL NOCICEPTORS OF THE NEONATAL RAT SPINAL CORD-TAIL INVITRO - DEPENDENCE OF EXTRACELLULAR IONS AND INDEPENDENCE OF 2ND MESSENGERS [J].
DRAY, A ;
BETTANEY, J ;
FORSTER, P .
BRITISH JOURNAL OF PHARMACOLOGY, 1990, 101 (03) :727-733
[6]   DIRECT EVIDENCE FOR NEUROGENIC INFLAMMATION AND ITS PREVENTION BY DENERVATION AND BY PRETREATMENT WITH CAPSAICIN [J].
JANCSO, N ;
JANCSOGA.A ;
SZOLCSANYI, J .
BRITISH JOURNAL OF PHARMACOLOGY AND CHEMOTHERAPY, 1967, 31 (01) :138-+
[7]  
Lee Buyean, 1994, Archives of Pharmacal Research (Seoul), V17, P304, DOI 10.1007/BF02974166
[8]   Capsazepine, a vanilloid receptor antagonist, inhibits nicotinic acetylcholine receptors in rat trigeminal ganglia [J].
Liu, L ;
Simon, SA .
NEUROSCIENCE LETTERS, 1997, 228 (01) :29-32
[9]  
LIU L, 1997, J NEUROSCI, V17, P101
[10]   THE EFFECT OF CAPSAICIN APPLICATION TO A PERIPHERAL-NERVE ON IMPULSE CONDUCTION IN FUNCTIONALLY IDENTIFIED AFFERENT NERVE-FIBERS [J].
PETSCHE, U ;
FLEISCHER, E ;
LEMBECK, F ;
HANDWERKER, HO .
BRAIN RESEARCH, 1983, 265 (02) :233-240