PMID: 8220885Sep 1, 1993Paper

Pharmacological characterization of the novel nonpeptide angiotensin II receptor antagonist, BIBR 277

British Journal of Pharmacology
W WienenM Entzeroth

Abstract

1. The pharmacological profile of BIBR 277, 4'-[(1,4'-dimethyl-2'-propyl[2,6'-bi-1H-benzimidazol]-1'-yl)methyl ]- [1,1'-biphenyl]-2-carboxylic acid, a novel, nonpeptide angiotensin II receptor antagonist has been investigated by use of receptor binding studies, enzymatic assays, functional in vitro assays in rabbit aorta as well as in vivo experiments in pithed, anaesthetized and conscious rats. 2. BIBR 277 potently interacted with rat AT1 receptors (Ki 3.7 nM). Competitive receptor interaction was shown by radioligand saturation experiments performed in the presence of BIBR 277. The failure to inhibit radioligand binding to AT2 sites demonstrates the selectivity of BIBR 277 for AT1 receptors. This is further substantiated by the findings that BIBR 277 neither interacted with other receptor systems investigated nor affected the activity of components of the human renin-angiotensin system, such as plasma renin or serum converting enzyme. 3. In rabbit aorta, BIBR 277 had no agonistic properties and was shown to be an insurmountable antagonist of angiotensin II-induced contractions (KB 0.33 nM). The antagonistic effect persisted even after several wash-out procedures. However, this interaction was not irreversible since the insurm...Continue Reading

References

Apr 1, 1977·Physiological Reviews·M J Peach
Mar 25, 1991·European Journal of Pharmacology·M Entzeroth, S Hadamovsky
Jan 1, 1987·Journal of Cardiovascular Pharmacology·B JacksonC I Johnston
Jan 1, 1987·Journal of Cardiovascular Pharmacology·J I Robertson, D M Tillman
Nov 30, 1989·Biochemical and Biophysical Research Communications·A T ChiuA L Johnson
Aug 30, 1989·Biochemical and Biophysical Research Communications·S WhitebreadM de Gasparo
Dec 31, 1987·Biochemical and Biophysical Research Communications·H OkunishiN Toda
Jan 10, 1987·British Medical Journal·S M WoodM D Rawlins
Jan 1, 1987·Annual Review of Physiology·M I Phillips
Dec 1, 1971·Circulation Research·D T PalsD C Fessler
Mar 23, 1972·The New England Journal of Medicine·R ZacestJ Koch-Weser
Jan 1, 1984·Journal of Cardiovascular Pharmacology·K J CattG Aguilera
Mar 1, 1959·British Journal of Pharmacology and Chemotherapy·O ARUNLAKSHANA, H O SCHILD
Jun 1, 1959·British Journal of Pharmacology and Chemotherapy·R B BARLOW, I KHAN

❮ Previous
Next ❯

Citations

Jul 18, 1995·European Journal of Pharmacology·A R RenzettiA Subissi
Jul 8, 1999·European Journal of Pharmacology·F L FierensG Vauquelin
Nov 11, 1999·European Journal of Pharmacology·T NakaiK Ichihara
May 17, 2002·Journal of Diabetes and Its Complications·J RippinUNKNOWN DETAIL study
Sep 2, 2004·Nature Reviews. Drug Discovery·David C Swinney
Jul 19, 1994·Proceedings of the National Academy of Sciences of the United States of America·H T SchambyeT W Schwartz
Feb 2, 2000·Current Opinion in Nephrology and Hypertension·R T Gansevoort, D de Zeeuw
Nov 1, 2000·Critical Care : the Official Journal of the Critical Care Forum·H U StrohmengerP Radermacher
Jul 1, 2004·Nihon yakurigaku zasshi. Folia pharmacologica Japonica·Motohiko ChachinHisashi Satoh
May 8, 2010·Vascular Health and Risk Management·Domenico GalzeranoCarlo Gaudio
Feb 24, 2001·Clinical Therapeutics·F FreytagUNKNOWN Telmisartan Hypertension Experience in a Randomized European Study Versus Atenolol Study Group
Jun 1, 2010·Expert Opinion on Drug Metabolism & Toxicology·Sylvia DeppeRalf A Benndorf
Aug 9, 2011·Antiviral Research·Juan C ZapataMaria S Salvato
May 22, 2010·Journal of Ethnopharmacology·Enrique Jiménez-FerrerMaribel Herrera-Ruiz
Jul 1, 2008·Journal of the American Society of Hypertension : JASH·Gordon McInnes
Jul 16, 2008·Molecular and Cellular Endocrinology·I Van Liefde, G Vauquelin
Jun 21, 2008·Biochemical and Biophysical Research Communications·Tatsuya BadenYukio Hara
Nov 7, 2012·Pain Practice : the Official Journal of World Institute of Pain·Hisanao Akiyama, Yasuhiro Hasegawa
Dec 24, 2009·Chirality·Takateru KubotaChristopher J Welch
Dec 21, 2005·The Journal of Heart and Lung Transplantation : the Official Publication of the International Society for Heart Transplantation·Noriyoshi KajiharaShigeki Morita

❮ Previous
Next ❯

Related Concepts

Related Feeds

Anthelmintics

Anthelmintics or antihelminthics are a group of antiparasitic drugs that expel parasitic worms (helminths) and other internal parasites from the body by either stunning or killing them and without causing significant damage to the host. Discover the latest research on anthelmintics here.