-
1
-
-
0037405120
-
Biological characterization of a novel, orally active small molecule gonadotropin-releasing hormone (GnRH) antagonist using castrated and intact rats
-
Anderes KL, Luthin DR, Castillo R, Kraynov EA, Castro M, Nared-Hood K,, et al. Biological characterization of a novel, orally active small molecule gonadotropin-releasing hormone (GnRH) antagonist using castrated and intact rats. J Pharmacol Exp Ther 2003 ; 305: 688-695.
-
(2003)
J Pharmacol Exp Ther
, vol.305
, pp. 688-695
-
-
Anderes, K.L.1
Luthin, D.R.2
Castillo, R.3
Kraynov, E.A.4
Castro, M.5
Nared-Hood, K.6
-
2
-
-
17544401468
-
A novel synthesis of 7-aryl-8-fluoro-pyrrolo[1,2-a]pyrimid-4-ones as potent, stable GnRH receptor antagonists
-
Tucci FC, Zhu YF, Guo Z, Gross TD, Connors PJ Jr, Struthers RS,, et al. A novel synthesis of 7-aryl-8-fluoro-pyrrolo[1,2-a]pyrimid-4-ones as potent, stable GnRH receptor antagonists. Bioorg Med Chem Lett 2002 ; 12: 3491-3495.
-
(2002)
Bioorg Med Chem Lett
, vol.12
, pp. 3491-3495
-
-
Tucci, F.C.1
Zhu, Y.F.2
Guo, Z.3
Gross, T.D.4
Connors Jr., P.J.5
Struthers, R.S.6
-
3
-
-
33748510561
-
Nonpeptide gonadotropin releasing hormone antagonists
-
Doherty AM (ed): Paris France: Elsevier
-
Yun-Fei Zhu CC, Struthers RS: Nonpeptide gonadotropin releasing hormone antagonists. In Doherty AM (ed): Annual Reports in Medicinal Chemistry. Paris France: Elsevier, 2004: 99-108.
-
(2004)
Annual Reports in Medicinal Chemistry
, pp. 99-108
-
-
Yun-Fei Zhu, C.C.1
Struthers, R.S.2
-
4
-
-
0033391893
-
A comparison of the efficacy and duration of action of candesartan cilexetil and losartan as assessed by clinic and ambulatory blood pressure after a missed dose, in truly hypertensive patients: A placebo controlled, forced titration study. Candesartan/Losartan study investigators
-
Lacourciere Y, Asmar R: A comparison of the efficacy and duration of action of candesartan cilexetil and losartan as assessed by clinic and ambulatory blood pressure after a missed dose, in truly hypertensive patients: a placebo controlled, forced titration study. Candesartan/Losartan study investigators. Am J Hypertens 1999 ; 12: 1181-1187.
-
(1999)
Am J Hypertens
, vol.12
, pp. 1181-1187
-
-
Lacourciere, Y.1
Asmar, R.2
-
5
-
-
33646122469
-
Biochemical mechanisms of new molecular entities (NMEs) approved by United States FDA during 2001-2004: Mechanisms leading to optimal efficacy and safety
-
Swinney DC: Biochemical mechanisms of new molecular entities (NMEs) approved by United States FDA during 2001-2004: mechanisms leading to optimal efficacy and safety. Curr Top Med Chem 2006 ; 6: 461-478.
-
(2006)
Curr Top Med Chem
, vol.6
, pp. 461-478
-
-
Swinney, D.C.1
-
6
-
-
0034959207
-
Antihypertensive efficacy of candesartan in comparison to losartan: The CLAIM study
-
Bakris G, Gradman A, Reif M, Wofford M, Munger M, Harris S,, et al. Antihypertensive efficacy of candesartan in comparison to losartan: the CLAIM study. J Clin Hypertens (Greenwich) 2001 ; 3: 16-21.
-
(2001)
J Clin Hypertens (Greenwich)
, vol.3
, pp. 16-21
-
-
Bakris, G.1
Gradman, A.2
Reif, M.3
Wofford, M.4
Munger, M.5
Harris, S.6
-
7
-
-
0034571320
-
Angiotensin II type 1 receptor antagonists: Why do some of them produce insurmountable inhibition?
-
Vanderheyden PM, Fierens FL, Vauquelin G: Angiotensin II type 1 receptor antagonists: why do some of them produce insurmountable inhibition? Biochem Pharmacol 2000 ; 60: 1557-1563.
-
(2000)
Biochem Pharmacol
, vol.60
, pp. 1557-1563
-
-
Vanderheyden, P.M.1
Fierens, F.L.2
Vauquelin, G.3
-
8
-
-
4544381198
-
Biochemical mechanisms of drug action: What does it take for success?
-
Swinney DC: Biochemical mechanisms of drug action: what does it take for success? Nat Rev Drug Discov 2004 ; 3: 801-808.
-
(2004)
Nat Rev Drug Discov
, vol.3
, pp. 801-808
-
-
Swinney, D.C.1
-
9
-
-
33745511768
-
Slow antagonist dissociation and long-lasting in vivo receptor protection
-
Vauquelin G, Van Liefde I: Slow antagonist dissociation and long-lasting in vivo receptor protection. Trends Pharmacol Sci 2006 ; 7: 355-359.
-
(2006)
Trends Pharmacol Sci
, vol.7
, pp. 355-359
-
-
Vauquelin, G.1
Van Liefde, I.2
-
10
-
-
33748325882
-
Drug-target residence time and its implications for lead optimization
-
Copeland RA, Pompliano DL, Meek TD: Drug-target residence time and its implications for lead optimization. Nat Rev Drug Discov 2006 ; 5: 730-739.
-
(2006)
Nat Rev Drug Discov
, vol.5
, pp. 730-739
-
-
Copeland, R.A.1
Pompliano, D.L.2
Meek, T.D.3
-
11
-
-
33748074796
-
Kinetics of nonpeptide antagonist binding to the human gonadotropinreleasing hormone receptor: Implications for structure-activity relationships and insurmountable antagonism
-
Sullivan SK, Hoare SR, Fleck BA, Zhu YF, Heise CE, Struthers RS,, et al. Kinetics of nonpeptide antagonist binding to the human gonadotropinreleasing hormone receptor: implications for structure-activity relationships and insurmountable antagonism. Biochem Pharmacol 2006 ; 72: 838-849.
-
(2006)
Biochem Pharmacol
, vol.72
, pp. 838-849
-
-
Sullivan, S.K.1
Hoare, S.R.2
Fleck, B.A.3
Zhu, Y.F.4
Heise, C.E.5
Struthers, R.S.6
-
12
-
-
0021336303
-
The kinetics of competitive radioligand binding predicted by the law of mass action
-
Motulsky HJ, Mahan LC: The kinetics of competitive radioligand binding predicted by the law of mass action. Mol Pharmacol 1984 ; 25: 1-9.
-
(1984)
Mol Pharmacol
, vol.25
, pp. 1-9
-
-
Motulsky, H.J.1
Mahan, L.C.2
-
13
-
-
20444499347
-
Measurement of radioligand binding by scintillation proximity assay
-
Berry J, Price-Jones M: Measurement of radioligand binding by scintillation proximity assay. Methods Mol Biol 2005 ; 306: 121-138.
-
(2005)
Methods Mol Biol
, vol.306
, pp. 121-138
-
-
Berry, J.1
Price-Jones, M.2
-
14
-
-
0024404456
-
Determination of the association and dissociation rate constants of muscarinic antagonists on rat pancreas: Rank order of potency varies with time
-
Waelbroeck M, Camus J, Christophe J: Determination of the association and dissociation rate constants of muscarinic antagonists on rat pancreas: rank order of potency varies with time. Mol Pharmacol 1989 ; 36: 405-411.
-
(1989)
Mol Pharmacol
, vol.36
, pp. 405-411
-
-
Waelbroeck, M.1
Camus, J.2
Christophe, J.3
-
15
-
-
0018859931
-
Kinetics of the hormone-receptor interaction: Competition experiments with slowly equilibrating ligands
-
Aranyi P: Kinetics of the hormone-receptor interaction: competition experiments with slowly equilibrating ligands. Biochim Biophys Acta 1980 ; 628: 220-227.
-
(1980)
Biochim Biophys Acta
, vol.628
, pp. 220-227
-
-
Aranyi, P.1
-
16
-
-
0037334023
-
Mechanism of corticotropin-releasing factor type I receptor regulation by nonpeptide antagonists
-
Hoare SR, Sullivan SK, Ling N, Crowe PD, Grigoriadis DE: Mechanism of corticotropin-releasing factor type I receptor regulation by nonpeptide antagonists. Mol Pharmacol 2003 ; 63: 751-765.
-
(2003)
Mol Pharmacol
, vol.63
, pp. 751-765
-
-
Hoare, S.R.1
Sullivan, S.K.2
Ling, N.3
Crowe, P.D.4
De, G.5
-
17
-
-
33751183557
-
Determining the potency and molecular mechanism of action of insurmountable antagonists
-
Kenakin T, Jenkinson S, Watson C: Determining the potency and molecular mechanism of action of insurmountable antagonists. J Pharmacol Exp Ther 2006 ; 319: 710-723.
-
(2006)
J Pharmacol Exp Ther
, vol.319
, pp. 710-723
-
-
Kenakin, T.1
Jenkinson, S.2
Watson, C.3
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