EMD 66684

EMD 66684 is an antagonist of Angiotensin II Type 1 (AT1) receptor. EMD 66684 shows potent binding affinities for the AT1 subtype Ang II receptor with an IC₅₀ value of 0.7 nM. EMD 66684 also serves as an antiischemic cytoprotectant ^[1]-[5]. IC50 & Target:IC50: 0.7 nM (Angiotensin II type 1)^[1] In Vitro: Ang II is known to activate at least two receptor subtypes, namely, AT1 and AT2 receptors^[1].
EMD 66684 (0.1 μM) decreases Ang II (0.1 mM)-induced in basal and NS-induced NPY overflow, attenuates the NS-induced stimulation of both NE and NPY release^[1].
EMD 66684 (0.01 nM-1 μM; 0, 30, 60 min) exhibits a time-dependent inhibition against Ang II in DMR (dynamic mass redistribution) responses, with IC₅₀s of 181.97 nM (0 min), 0.22 nM (30 min), 0.17 nM (60 min), respectively^[2].
EMD 66684 exhibits binding affinities for the AT1 subtype Ang II receptor with an IC₅₀ value of 0.7 nM in rat adrenal cortical membranes, and inhibits Ang II-Induced contraction in rabbit aortic rings with an IC₅₀ value of 0.2 nM^[3]. In Vivo: EMD 66684 (0.1, 0.3, 1 mg/kg; i.v.; once) results in a long lasting fall in blood pressure^[3].
EMD 66684 (0.1 μM; 45 min) decreases the NS-induced overflow of NE and NPY from preparations from SHRs at 10-12 weeks old^[4].