Design and synthesis of sodium (.beta.R*,.gamma.S*)-4-[[3-(4-acetyl-3-hydroxy-2-propylphenoxy)propyl]thio]-.gamma.-hydroxy-.beta.-methylbenzenebutanoate: a novel, selective, and orally active receptor antagonist of leukotriene D4

1986 ◽  
Vol 29 (9) ◽  
pp. 1573-1576 ◽  
Author(s):  
R. N. Young ◽  
P. Belanger ◽  
E. Champion ◽  
R. N. DeHaven ◽  
D. Denis ◽  
...  
Keyword(s):  
Receptor Antagonist ◽  
Leukotriene D4 ◽  
Design And Synthesis ◽  
Orally Active

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.

ChemInform Abstract: Discovery of MK-0476, a Potent and Orally Active Leukotriene D4 Receptor Antagonist Devoid of Peroxisomal Enzyme Induction.

ChemInform ◽  
2010 ◽  
Vol 26 (27) ◽  
pp. no-no
Author(s):  
M. LABELLE ◽  
M. BELLEY ◽  
Y. GAREAU ◽  
J. Y. GAUTHIER ◽  
D. GUAY ◽  
...  
Keyword(s):  
Receptor Antagonist ◽  
Enzyme Induction ◽  
Leukotriene D4 ◽  
Peroxisomal Enzyme ◽  
D4 Receptor ◽  
Orally Active

The discovery of L-699,392, a novel potent and orally active leukotriene D4 receptor antagonist

1994 ◽  
Vol 4 (3) ◽  
pp. 463-468 ◽  
Author(s):  
M. Labelle ◽  
M. Belley ◽  
E. Champion ◽  
R. Gordon ◽  
K. Hoogsteen ◽  
...  
Keyword(s):  
Receptor Antagonist ◽  
Leukotriene D4 ◽  
D4 Receptor ◽  
Orally Active

Design and Synthesis of Selurampanel, a Novel Orally Active and Competitive AMPA Receptor Antagonist

ChemMedChem ◽  
2016 ◽  
Vol 12 (3) ◽  
pp. 197-201 ◽  
Author(s):  
David Orain ◽  
Engin Tasdelen ◽  
Samuel Haessig ◽  
Manuel Koller ◽  
Anne Picard ◽  
...  
Keyword(s):  
Receptor Antagonist ◽  
Ampa Receptor ◽  
Design And Synthesis ◽  
Ampa Receptor Antagonist ◽  
Orally Active

scholarly journals Cover Picture: Design and Synthesis of Selurampanel, a Novel Orally Active and Competitive AMPA Receptor Antagonist (ChemMedChem 3/2017)

ChemMedChem ◽  
2017 ◽  
Vol 12 (3) ◽  
pp. 196-196
Author(s):  
David Orain ◽  
Engin Tasdelen ◽  
Samuel Haessig ◽  
Manuel Koller ◽  
Anne Picard ◽  
...  
Keyword(s):  
Receptor Antagonist ◽  
Ampa Receptor ◽  
Design And Synthesis ◽  
Ampa Receptor Antagonist ◽  
Orally Active

ChemInform Abstract: The Discovery of L-699,392, a Novel Potent and Orally Active Leukotriene D4 Receptor Antagonist.

ChemInform ◽  
2010 ◽  
Vol 25 (31) ◽  
pp. no-no
Author(s):  
M. LABELLE ◽  
M. BELLEY ◽  
E. CHAMPION ◽  
R. GORDON ◽  
K. HOOGSTEEN ◽  
...  
Keyword(s):  
Receptor Antagonist ◽  
Leukotriene D4 ◽  
D4 Receptor ◽  
Orally Active
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