Neurokinin receptor antagonists

被引:28
作者
Leroy, V [1 ]
Mauser, P [1 ]
Gao, ZL [1 ]
Peet, NP [1 ]
机构
[1] Aventis Pharmaceuts, Bridgewater, NJ 08807 USA
关键词
asthma; depression; emesis; migraine; neurokinin; neurokinin receptor antagonist; substance P;
D O I
10.1517/13543784.9.4.735
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Studies on tachykinin peptides and the corresponding neurokinin receptors (NKr) have increased dramatically recently due to the discovery of selective, orally-active, metabolically stable and sometimes CNS penetrating NKr antagonists. After demonstrating the potential use for NKr antagonists in animal models, some compounds have recently progressed into clinical trials and a few results have been published. NKr antagonists have demonstrated efficacy for the treatment of emesis and depression, while results in other areas have been disappointing. Nonetheless, this area is coming to the exciting time of proof of concept in humans. Demonstration of the: involvement of tachykinin peptides in biological functions continues to grow, as do the potential indications for NKr antagonists. More drug candidates are undergoing clinical trials for various conditions and these results could widen the potential use for NKr antagonists.
引用
收藏
页码:735 / 746
页数:12
相关论文
共 68 条
  • [61] Schuiling M, 1999, CLIN EXP ALLERGY, V29, P48
  • [62] Neurokinin receptor antagonists
    Seward, EM
    Swain, CJ
    [J]. EXPERT OPINION ON THERAPEUTIC PATENTS, 1999, 9 (05) : 571 - 582
  • [63] A POTENT NONPEPTIDE ANTAGONIST OF THE SUBSTANCE-P (NK1) RECEPTOR
    SNIDER, RM
    CONSTANTINE, JW
    LOWE, JA
    LONGO, KP
    LEBEL, WS
    WOODY, HA
    DROZDA, SE
    DESAI, MC
    VINICK, FJ
    SPENCER, RW
    HESS, HJ
    [J]. SCIENCE, 1991, 251 (4992) : 435 - 437
  • [64] Sorbera L. A., 1999, Drugs of the Future, V24, P254, DOI 10.1358/dof.1999.024.03.482256
  • [65] Suzuki R, 1999, J IMMUNOL, V163, P2410
  • [66] Swain C, 1999, ANNU REP MED CHEM, V34, P51
  • [67] Swain CJ, 1998, PROGR MED CHEM, V35, P57, DOI 10.1016/S0079-6468(08)70034-1
  • [68] The effect of the NK2 tachykinin receptor antagonist SR 48968 (saredutant) on neurokinin A-induced bronchoconstriction in asthmatics
    Van Schoor, J
    Joos, GF
    Chasson, BL
    Brouard, RJ
    Pauwels, RA
    [J]. EUROPEAN RESPIRATORY JOURNAL, 1998, 12 (01) : 17 - 23