Comparison between two classes of selective EP3 antagonists and their biological activities

Bioorganic and Medicinal Chemistry Letters

Volumn 16, Issue 21, 2006, Pages 5639-5642

  Belley, Michel ^a   Chan, Chi Chung ^a   Gareau, Yves ^a   Gallant, Michel ^a   Juteau, Hélène ^a   Houde, Karine ^a   Lachance, Nicolas ^a   Labelle, Marc ^a   Sawyer, Nicole ^a   Tremblay, Nathalie ^a   Lamontagne, Sonia ^a   Carrière, Marie Claude ^a   Denis, Danielle ^a   Greig, Gillian M ^a   Slipetz, Deborah ^a   Gordon, Robert ^a   Chauret, Nathalie ^a   Li, Chun ^a   Zamboni, Robert J ^a   Metters, Kathleen M ^a  

^a MERCK FROSST CENTRE FOR THERAPEUTIC RESEARCH   (Canada)

Author keywords

Acylsulfonamides; Analgesic; Anti inflammation; Cinnamic acids; EP3 antagonist; Metabolism; Rat paw edema; Rat paw hyperalgesia

Indexed keywords

CINNAMIC ACID DERIVATIVE; PROSTAGLANDIN E RECEPTOR; PROSTAGLANDIN RECEPTOR BLOCKING AGENT; SULFONAMIDE;

ANALGESIC ACTIVITY; ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; BINDING AFFINITY; BIOLOGICAL ACTIVITY; CONTROLLED STUDY; DOSE RESPONSE; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG METABOLISM; DRUG POTENCY; DRUG STRUCTURE; EMBRYO; HUMAN; HUMAN CELL; HYBRID; HYPERALGESIA; MALE; NONHUMAN; PAW EDEMA; RAT; SUBSTITUTION REACTION;

CINNAMATES; HUMANS; RECEPTORS, PROSTAGLANDIN E; SULFONAMIDES;

EID: 33748786846     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2006.08.025     Document Type: Article

References (12)

1. Belley M., Gallant M., Roy B., Houde K., Lachance N., Labelle M., Trimble L., Chauret N., Li C., Sawyer N., Tremblay N., Lamontagne S., Carrière M.-C., Denis D., Greig G.M., Slipetz D., Metters K.M., Gordon R., Chan C.C., and Zamboni R.J. Bioorg. Med. Chem. Lett. 15 (2005) 527
2. Juteau H., Gareau Y., Labelle M., Sturino C.F., Sawyer N., Tremblay N., Lamontagne S., Carrière M.-C., Denis D., and Metters K.M. Bioorg. Med. Chem. 9 (2001) 1977
3. Juteau H., Gareau Y., Labelle M., Lamontagne S., Tremblay N., Carrière M.-C., Denis D., Sawyer N., and Metters K.M. Bioorg. Med. Chem. Lett. 11 (2001) 747
4. 1 and the variation in the ratio of isomers should not significantly change the results described herein.
5. Pelletier J.C., and Hesson D.P. Synlett (1995) 1141
6. Boie Y., Stocco R., Sawyer N., Slipetz D.M., Ungrin M.D., Neuschäfer-Rube F., Püschel G.P., Metters K.M., and Abramovitz M. Eur. J. Pharmacol. 340 (1997) 227
7. Li C., Chauret N., Trimble L.A., Nicoll-Griffith D.A., Silva J.M., Macdonald D., Perrier H., Yergey J.A., Parton T., Alexander R.P., and Warrellow G.J. Drug Metab. Dispos. 29 (2001) 232
8. Chan C.-C., Boyce S., Brideau C., Ford-Hutchinson A.W., Gordon R., Guay D., Hill R.G., Li C.-S., Mancini J., Penneton M., Prasit P., Rasori R., Riendeau D., Roy P., Tagari P., Vickers P., Wong E., and Rodger I.W. J. Pharm. Exp. Ther. 274 (1995) 1531
9. Labelle M., Gareau Y., Dufresne C., Lau C.K., Belley M., Jones T.R., Leblanc Y., McAuliffe M., McFarlane C.S., Metters K.M., Ouimet N., Perrier H., Rochette C., Sawyer N., Slipetz D., Xiang Y.B., Wang Z., Pickett C.B., Ford-Hutchinson A.W., Young R.N., and Zamboni R.J. Bioorg. Med. Chem. Lett. 5 (1995) 2551
10. Jones T.R., Labelle M., Belley M., Champion E., Charette L., Evans J., Ford-Hutchinson A.W., Gauthier J.-Y., Lord A., Masson P., McAuliffe M., McFarlane C.S., Metters K.M., Pickett C., Piechuta H., Rochette C., Rodger I.W., Sawyer N., Young R.N., Zamboni R.J., and Abraham W.M. Can. J. Physiol. Pharmacol. 73 (1995) 191
11. i of 0.082 μM on the DP receptor.
12. Breyer R.M., Bagdassarian C.K., Myers S.A., and Breyer M.D. Annu. Rev. Pharmacol. Toxicol. 41 (2001) 661