|Description||Bosentan inhibits the presser response to big ET-1 both after i.v. and oral administration, with a long duration of action and no intrinsic agonist activity.|
Endothelin 1 swine, human
Endothelin 1 (swine, human), a vasoconstrictor increased in plasma and explants of patients with uterine leiomyomas, is a synthetic peptide with the sequence of...
Zibotentan (ZD4054)is an orally administered, potent and specific ETA-receptor (endothelin A receptor) antagonist (IC50 = 21 nM).
Fandosentan potassium is an endothelin A antagonist developed for the treatment of pulmonary hypertension.
Enrasentan, an indene derivative, has been found to be an endothelin receptor antagonist that was once studied in reperfusion injury and heart failure therapy.
BMS-248360 is a first orally active generation dual action receptor antagonist. BMS-248360 antagonized both Ang II AT1 and endothelin ETA receptors (AT1 IC50 = ...
Sitaxentan sodium inhibits ET-1-induced stimulation of phosphoinositide turnover with a Ki of 0.69 nM and a pA2 of 8.0.
RO462005 is an endothelin receptor selective agonist.
FR 139317 is a selective Endothelin A receptor antagonist originated by Fujisawa. (Ki values are 1 nM and 7.3 μM at ETA and ETB subtypes respectively). No devel...
IRL-2500, an indol derivative, has been found to be an endothelin B receptor antagonist that was once studied in hypertension.
Bosentan is an endothelin (ET) receptor antagonist for ET-A and ET-B with Ki of 4.7 nM and 95 nM, respectively.
Bosentan inhibits the presser response to big ET-1 both after i.v. and oral administration, with a long duration of action and no intrinsic agonist activity.
BMS-187308, a sulfonamide derivative, has been found to be an endothelin-A (ETA) antagonist that was once studied about its activity against pressor effect in r...
atrasentan hydrochloride is the orally available hydrochloride salt of pyrrolidine-3-carboxylic acid with potential antineoplastic activity. As a selective anta...
Tak-044 has been found to be an endothelin receptor antagonist that was once studied against some sort of liver disorders and subarachnoid haemorrhage.
Edonentan, also known as BMS-207940, is a very potent and selective ETA endothelin receptor antagonist (Ki= 10 pM) that shows 80000-fold selective for ETA vs ET...
Clazosentan, also called as AXV 034, Ro 61-1790 or VML 588, a novel endothelin A antagonist, improves cerebral blood flow and behavior after traumatic brain inj...
Ambrisentan, a highly selective antagonist of the endothelin-1 type A receptor with IC50 of 18 nM, is indicated for the treatment of pulmonary arterial hyperten...
Macitentan is an orally available dual endothelin receptor (ETR) antagonist with potential antihypertensive and antineoplastic activity.
Tezosentan, also known as RO 610612 and Veletri, is a potent dual endothelian (ETA/ETB) receptor antagonist optimized from Bosentan (B675900). It acts as a vaso...
The sodium salt form of T-0201 which has been found to be an Endothelin A receptor antagonist that could be used as as anti-ischaemic agent and was once studied...