Plasma drug profiles and tolerability of MK-571 (L-660,711), a leukotriene D4 receptor antagonist, in man

1992 ◽  
Vol 43 (4) ◽  
pp. 427-430 ◽  
Author(s):  
M. Depré ◽  
D. J. Margolskee ◽  
J. Y. K. Hsieh ◽  
A. Van Hecken ◽  
A. Buntinx ◽  
...  
Keyword(s):  
Receptor Antagonist ◽  
Plasma Drug ◽  
Leukotriene D4 ◽  
D4 Receptor

Treatment of interstitial cystitis with montelukast, a leukotriene D4 receptor antagonist

Urology ◽  
2001 ◽  
Vol 57 (6) ◽  
pp. 118 ◽  
Author(s):  
K Bouchelouche ◽  
J Nordling ◽  
T Hald ◽  
P Bouchelouche
Keyword(s):  
Receptor Antagonist ◽  
Interstitial Cystitis ◽  
Leukotriene D4 ◽  
D4 Receptor

scholarly journals Oral pharmacokinetics and food interaction of the leukotriene D4 receptor antagonist verlukast

1993 ◽  
Vol 36 (5) ◽  
pp. 464-466 ◽  
Author(s):  
JULES I. SCHWARTZ ◽  
DOROTHY J. MARGOLSKEE ◽  
THORIR D. BJORNSSON ◽  
VANESSA C. WILLIAMS ◽  
JOHN Y. HSIEH ◽  
...  
Keyword(s):  
Receptor Antagonist ◽  
Food Interaction ◽  
Leukotriene D4 ◽  
Oral Pharmacokinetics ◽  
D4 Receptor

Pharmacology of L-660,711 (MK-571): a novel potent and selective leukotriene D4 receptor antagonist

1989 ◽  
Vol 67 (1) ◽  
pp. 17-28 ◽  
Author(s):  
T. R. Jones ◽  
R. Zamboni ◽  
M. Belley ◽  
E. Champion ◽  
L. Charette ◽  
...  
Keyword(s):  
Guinea Pig ◽  
Receptor Antagonist ◽  
Guinea Pigs ◽  
Competitive Inhibitor ◽  
Dose Ratio ◽  
Leukotriene D4 ◽  
Small Component ◽  
Human Trachea ◽  
D4 Receptor ◽  
Orally Active

L-660,711 (3-(3-(2-(7-chloro-2-quinolinyl)ethenyl)phenyl) ((3-dimethyl amino-3-oxo propyl)thio)methyl)thio)propanoic acid is a potent and selective competitive inhibitor of [3H]leukotriene D4 binding in guinea pig (Ki value, 0.22 nM) and human (Ki value, 2.1 nM) lung membranes but is essentially inactive versus [3H]leukotriene C4 binding (IC50 value in guinea pig lung, 23 μM). Functionally it competitively antagonized contractions of guinea pig trachea and ileum induced by leukotriene (LT) D4 (respective pA2 values, 9.4 and 10.5) and LTE4 (respective pA2 values, 9.1 and 10.4) and contractions of human trachea induced by LTD4 (pA2 value, 8.5). L-660,711 (5.8 × 10−8 M) antagonized contractions of guinea pig trachea induced by LTC4 in the absence (dose ratio = 28) but not in the presence of 45 mM L-serine borate (dose ratio <2). L-660,711 (1.9 × 10−5 M) did not block contractions of guinea pig trachea induced by histamine, acetylcholine, 5-hydroxytryptamine, PGF2α, U-44069, or PGD2. In the presence of atropine, mepyramine, and indomethacin, L-660,711 (1.9 × 10−5 M) inhibited a small component of the response to antigen on guinea pig trachea but completely blocked anti-IgE-induced contractions of human trachea. L-660,711 (i.v.) antagonized bronchoconstriction induced in anesthetized guinea pigs by i.v. LTC4, LTD4, and LTE4 but did not block bronchoconstriction to arachidonic acid, U-44069, 5-hydroxytryptamine, histamine, or acetylcholine. Intraduodenal L-660,711 antagonized LTD4 (0.2–12.8 μg/kg) -induced bronchoconstriction in guinea pigs, and p. o. L-660,711 blocked LTD4- and Ascaris-induced bronchoconstriction in conscious squirrel monkeys and ovalbumin-induced bronchoconstriction in conscious sensitized rats treated with methysergide (3 μg/kg). The pharmacological profile of L-660,711 indicates that it is a potent, selective, orally active leukotriene receptor antagonist which is well suited to determine the role played by LTD4 and LTE4 in asthma and other pathophysiologic conditions.

Increased sensitivity to vincristine of MDR cells by the leukotriene D4 receptor antagonist, ONO-1078

1998 ◽  
Vol 130 (1-2) ◽  
pp. 175-182 ◽  
Author(s):  
Shuichi Nagayama ◽  
Zhe-Sheng Chen ◽  
Masaki Kitazono ◽  
Yuji Takebayashi ◽  
Kiyoshi Niwa ◽  
...  
Keyword(s):  
Receptor Antagonist ◽  
Leukotriene D4 ◽  
Increased Sensitivity ◽  
D4 Receptor

Inhibition of Exercise-Induced Bronchoconstriction by MK-571, a Potent Leukotriene D4–Receptor Antagonist

1990 ◽  
Vol 323 (25) ◽  
pp. 1736-1739 ◽  
Author(s):  
Patrick J. Manning ◽  
Richard M. Watson ◽  
Dorothy J. Margolskee ◽  
Vanessa C. Williams ◽  
Jules I. Schwartz ◽  
...  
Keyword(s):  
Receptor Antagonist ◽  
Leukotriene D4 ◽  
D4 Receptor ◽  
Exercise Induced
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