| Description: |
Ro 46-2005 is a novel synthetic non-peptide endothelin receptor antagonist, inhibits the specific binding of 125I-ET-1 to human vascular smooth muscle cells (ETA receptor) with IC50 of 220 nM. |
| Target: |
IC50 value: 220 nM (ETA) [2]
Target: Endothelin |
| In Vitro: |
Ro 46-2005 proves to be equipotent (IC50 200-500 nM) for inhibition of [125I]ET-1 binding on the two known ET receptor subtypes (ETA and ETB). Ro 46-2005 also inhibits the functional consequences of ET-1 stimulation: the ET-l-induced release of arachidonic acid from rat mesangial cells was inhibited with an IC50 of 1.8 μM.[1] |
| References: |
[1]. Breu V, et al. In vitro characterization of Ro 46-2005, a novel synthetic non-peptide endothelin antagonist of ETA and ETBreceptors. FEBS Lett. 1993 Nov 15;334(2):210-214.
[2]. Clozel M, et al. Pathophysiological role of endothelin revealed by the first orally active endothelin receptor antagonist. Nature. 1993 Oct 21;365(6448):759-761.
[3]. N.R. Sibson, et al. MRI Determination of the Mechanisms Underlying TNF-a-induced Changes in Cerebral Blood Volume, Tissue Water Diffusion and BBB Permeability. Proc. Intl. Soc. Mag. Reson. Med. 10 (2002) |
