INHIBITION OF CUTANEOUS AND PLATELET RESPONSES TO PLATELET-ACTIVATING-FACTOR BY ORAL WEB 2086 IN MAN

被引:11
|
作者
HAYES, JP
RIDGE, SM
GRIFFITH, S
BARNES, PJ
CHUNG, KF
机构
[1] ROYAL BROMPTON & NATL HEART HOSP,NATL HEART & LUNG INST,DEPT THORAC MED,DOVEHOUSE ST,LONDON SW3 6LY,ENGLAND
[2] BOEHRINGER INGELHEIM,BRACKNELL,ENGLAND
关键词
PAF; PAF ANTAGONIST; WEB; 2086; HISTAMINE;
D O I
10.1016/0091-6749(91)90304-7
中图分类号
R392 [医学免疫学];
学科分类号
100102 ;
摘要
WEB 2086, an antagonist of platelet-activating factor (PAF), was assessed against the cutaneous response in vivo and the aggregation of platelets ex vivo induced by PAF in a double-blind, placebo-controlled, crossover study in 12 normal male volunteers. Wheal-and-flare responses to intradermal PAF (200 ng) and histamine (1-mu-g) were measured 1 hour after placebo or control administration. Wheal volumes were significantly reduced by 66% +/- 8.7% (mean +/- SEM), 86% +/- 8.3%, and 90% +/- 6.0% after 10, 40, and 100 mg of WEB 2086 compared to placebo administration (p < 0.005). Flare responses were correspondingly inhibited by 66% +/- 8.3%, 82% +/- 8.7%, and 84% +/- 7.8% at 10, 40, and 100 mg of WEB 2086, respectively. Cutaneous responses to histamine were unaffected. Ex vivo platelet responses to PAF were significantly inhibited at all three doses of WEB 2086. Oral WEB 2086 is a potent and specific inhibitor of cutaneous and platelet responses to PAF in man.
引用
收藏
页码:83 / 88
页数:6
相关论文
共 50 条
  • [1] USE OF WEB-2086 AND WEB-2170 AS PLATELET-ACTIVATING-FACTOR ANTAGONISTS
    CASALSSTENZEL, J
    HEUER, HO
    METHODS IN ENZYMOLOGY, 1990, 187 : 455 - 465
  • [2] EFFECT OF A PLATELET-ACTIVATING-FACTOR ANTAGONIST, WEB-2086, ON ALLERGEN-INDUCED ASTHMATIC RESPONSES
    FREITAG, A
    WATSON, RM
    MATSOS, G
    EASTWOOD, C
    OBYRNE, PM
    THORAX, 1993, 48 (06) : 594 - 598
  • [3] MODIFICATION OF ANTIGEN-INDUCED LATE RESPONSES WITH AN ANTAGONIST OF PLATELET-ACTIVATING-FACTOR (WEB-2086)
    STEVENSON, JS
    TALLENT, M
    BLINDER, L
    ABRAHAM, WM
    FEDERATION PROCEEDINGS, 1987, 46 (04) : 1461 - 1461
  • [4] PHARMACOLOGICAL ACTIONS OF WEB-2086, A NEW SPECIFIC ANTAGONIST OF PLATELET-ACTIVATING-FACTOR
    CASALSSTENZEL, J
    MUACEVIC, G
    WEBER, KH
    JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS, 1987, 241 (03): : 974 - 981
  • [5] PLATELET-ACTIVATING-FACTOR AND WEB-2086 DIRECTLY MODULATE RAT CARDIOMYOCYTE CONTRACTILITY
    DELBRIDGE, LM
    STEWART, AG
    GOULTER, CM
    MORGAN, TO
    HARRIS, PJ
    JOURNAL OF MOLECULAR AND CELLULAR CARDIOLOGY, 1994, 26 (02) : 185 - 193
  • [6] WEB-2086 - AN INHIBITOR OF PLATELET ACTIVATING FACTOR
    WEINTRAUB, M
    EVANS, P
    HOSPITAL FORMULARY, 1989, 24 (07): : 367 - 369
  • [7] THE INTRADERMAL RESPONSES TO INJECTION OF PLATELET-ACTIVATING-FACTOR (PAF) IN MAN
    SCIBBERAS, DGJ
    FOX, J
    JAMES, I
    BABER, NS
    BRITISH JOURNAL OF CLINICAL PHARMACOLOGY, 1987, 23 (01) : P116 - P116
  • [8] AIRWAY RESPONSES TO PLATELET-ACTIVATING-FACTOR
    SCHELLENBERG, RR
    AMERICAN REVIEW OF RESPIRATORY DISEASE, 1987, 136 (04): : S28 - S32
  • [9] EFFECT OF A PLATELET-ACTIVATING-FACTOR ANTAGONIST, WEB-2086, ON INHIBITION OF ACTIVE OXYGEN GENERATION IN HUMAN POLYMORPHONUCLEAR LEUKOCYTES
    SUZUKI, S
    SUGAI, K
    SATO, H
    ARAKAWA, M
    PHARMACOLOGY, 1994, 48 (02) : 111 - 118
  • [10] EFFECTS OF WEB-2086, A NOVEL ANTAGONIST OF PLATELET-ACTIVATING-FACTOR, IN ACTIVE AND PASSIVE ANAPHYLAXIS
    CASALSSTENZEL, J
    IMMUNOPHARMACOLOGY, 1987, 13 (02): : 117 - 124