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The following terms were not found in PubMed: Edonentan, Edonentan
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BMS-193884 and BMS-207940 Bristol-Myers Squibb.
Hulpke-Wette M, Buchhorn R. Hulpke-Wette M, et al. Curr Opin Investig Drugs. 2002 Jul;3(7):1057-61. Curr Opin Investig Drugs. 2002. PMID: 12186267 Review.
Structural modifications led to the development of a second-generation analog, BMS-207940, a biphenylsulfonamide endothelin A receptor-selective antagonist, and the probable discontinuation of the first clinical candidate, BMS-193884 [446511]. By April 2002, BMS …
Structural modifications led to the development of a second-generation analog, BMS-207940, a biphenylsulfonamide endothelin A …
(11)C-BMS-5p and (18)F-FBzBMS: radiolabeled analogs of BMS-207940, a potent and selective antagonist of endothelin receptor subtype A.
Chopra A. Chopra A. 2013 Mar 12 [updated 2013 Jun 27]. In: Molecular Imaging and Contrast Agent Database (MICAD) [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2004–2013. 2013 Mar 12 [updated 2013 Jun 27]. In: Molecular Imaging and Contrast Agent Database (MICAD) [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2004–2013. PMID: 23833790 Free Books & Documents. Review.
Synthesis and in vivo evaluation of novel PET radioligands for imaging the endothelin-A receptor.
Mathews WB, Murugesan N, Xia J, Scheffel U, Hilton J, Ravert HT, Dannals RF, Szabo Z. Mathews WB, et al. J Nucl Med. 2008 Sep;49(9):1529-36. doi: 10.2967/jnumed.108.051565. Epub 2008 Aug 14. J Nucl Med. 2008. PMID: 18703610 Free article.
The aim of this study was to synthesize and evaluate in vivo (11)C- and (18)F-labeled analogs of the potent and selective ETA antagonist N-[[2'-[[(4,5-dimethyl-3-isoxazolyl)amino]sulfonyl]-4-(2-oxazol …
The aim of this study was to synthesize and evaluate in vivo (11)C- and (18)F-labeled analogs of the potent and selective ETA antagonist …
Biphenylsulfonamide endothelin receptor antagonists. 4. Discovery of N-[[2'-[[(4,5-dimethyl-3-isoxazolyl)amino]sulfonyl]-4-(2-oxazolyl)[1,1'-biphenyl]- 2-yl]methyl]-N,3,3-trimethylbutanamide (BMS-207940), a highly potent and orally active ET(A) selective antagonist.
Murugesan N, Gu Z, Spergel S, Young M, Chen P, Mathur A, Leith L, Hermsmeier M, Liu EC, Zhang R, Bird E, Waldron T, Marino A, Koplowitz B, Humphreys WG, Chong S, Morrison RA, Webb ML, Moreland S, Trippodo N, Barrish JC. Murugesan N, et al. J Med Chem. 2003 Jan 2;46(1):125-37. doi: 10.1021/jm020289q. J Med Chem. 2003. PMID: 12502366
Following the discovery that a 3-amino-isoxazole group displays significantly improved metabolic stability in comparison to its 5-regioisomer, the 3-amino-isoxazole group was combined with the optimal 2'-substituent leading to 16a (BMS-207940). Compound 16a is an ex …
Following the discovery that a 3-amino-isoxazole group displays significantly improved metabolic stability in comparison to its 5-regioisome …
Simulation of the impact of atropisomer interconversion on plasma exposure of atropisomers of an endothelin receptor antagonist.
Zhou YS, Tay LK, Hughes D, Donahue S. Zhou YS, et al. J Clin Pharmacol. 2004 Jul;44(7):680-8. doi: 10.1177/0091270004266622. J Clin Pharmacol. 2004. PMID: 15199072
BMS-207940, a potent endothelin receptor antagonist, exists as rapidly interconverting atropisomers. The plasma interconversion t(1/2) is approximately 2.5 hours at 400 microg/mL under room temperature and decreases to < 0.1 hours at 20 microg/mL, making it extre …
BMS-207940, a potent endothelin receptor antagonist, exists as rapidly interconverting atropisomers. The plasma interconversio …
Targeting of endothelin receptors in the healthy and infarcted rat heart using the PET tracer 18F-FBzBMS.
Higuchi T, Rischpler C, Fukushima K, Isoda T, Xia J, Javadi MS, Szabo Z, Dannals RF, Mathews WB, Bengel FM. Higuchi T, et al. J Nucl Med. 2013 Feb;54(2):277-82. doi: 10.2967/jnumed.112.106096. Epub 2013 Jan 11. J Nucl Med. 2013. PMID: 23315664 Free article.
RESULTS: At autoradiography, intravenous pretreatment with the selective ET-A blocker BMS-207940 reduced myocardial FBzBMS uptake by 93% 0.7%. Oral pretreatment with the clinical blocker bosentan resulted in a dose-dependent partial blockade (5 mg/kg, 48% 6%; 50 mg/ …
RESULTS: At autoradiography, intravenous pretreatment with the selective ET-A blocker BMS-207940 reduced myocardial FBzBMS upt …
Characterization of the in vitro atropisomeric interconversion rates of an endothelin A antagonist by enantioselective liquid chromatography.
Shi Y, Huang MH, Macor JE, Hughes DE. Shi Y, et al. J Chromatogr A. 2005 Jun 17;1078(1-2):67-73. doi: 10.1016/j.chroma.2005.04.091. J Chromatogr A. 2005. PMID: 16007983
Substituted biphenyl I (BMS-207940), a selective antagonist of the endothelin A (ETA) receptor, has been proposed for the treatment of congestive heart failure. ...
Substituted biphenyl I (BMS-207940), a selective antagonist of the endothelin A (ETA) receptor, has been proposed for the trea …