BIBS 39 is a new nonpeptide angiotensin II (AII) receptor antagonist. Target: Angiotensin Receptor in vitro: BIBS 39 displaces [125I] AII from its specific binding sites with a Ki value of 29 7 nM for the AII subtype 1 (AT1) receptor and a Ki value of 480 110 nM for the AII subtype 2 (AT2) receptor. BIBS 222 shows a Ki value of 20 7 nM for the AT1 subtype and a Ki value of 730 170 nM for the AT2 subtype. BIBS 39 is 17 times more selective for the AT1 subtype and BIBS 222 37 times. BIBS 39 shifts the AII concentration-contractile response curves in isolated rabbit aorta to the right in a parallel fashion. [1] in vivo: In pithed rats, BIBS 39 dependently shifts the dose-response curve of AII to the right without affecting the maximal response. BIBS 222 also causes parallel shifts to the right but a significant reduction of the maximal responses was observed at 3 and 10 mg/kg i.v. These results show that the benzimidazole derivatives BIBS 39 is a potent and selective AII receptor antagonists. Substitution with a benzimidazole moiety results into a considerable loss of selectivity for the AT1 receptor subtype compared with an imidazole moiety as, for instance, in DuP 753.[1] BIBS 39 is a new nonpeptide angiotensin receptor blockers that has affinity for both AT1- and AT2-receptors, is also a potent antagonist of the cardiovascular effects of AII in pithed rabbits. [2]
Molekulargewicht:
524.65
Reinheit:
99.70
CAS Nummer:
[133085-33-3]
Formel:
C32H36N4O3
Target-Kategorie:
Angiotensin Receptor
Anwendungsbeschreibung:
Reference compound
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