S 8308

S 8308 (CV 2961) is a non-peptide angiotensin II (Angiotensin II receptor) receptor antagonist with transient oral activity and short-acting intravenous activity, and exhibits an IC₅₀ of 15 μM in rats. S 8308 competitively blocks the binding of angiotensin II to its receptor, thereby inhibiting vasoconstriction and pressor responses. S 8308 can be used in the research of hypertension and renal hypertension^{[1][2][3][4][5][6][7]}. In Vitro:S 8308 (CV 2961) is a specific competitive angiotensin II receptor antagonist that inhibits the binding of radioligands, with an IC₅₀ of 15 μM in rat adrenal cortex microsomes and an IC₅₀ of 4.5 μM in rat aortic smooth muscle cells ^[3].
S 8308 inhibits the binding of ³H-AII to rat adrenal cortex microsomes with an IC₅₀ of 15 μM, and is a weak angiotensin II receptor antagonist^[6].
S 8308 (60 min) competitively inhibits the binding of angiotensin II to its receptor in rat adrenal cortex microsomes, with an IC₅₀ of 15 μM^[1].
S 8308 (30 min) competitively inhibits the binding of angiotensin II to its receptors on cultured rat aortic smooth muscle cells, with an IC₅₀ of 4.5 μM^[1].
S 8308 (1-30 µM; 15 min) inhibits angiotensin II-induced ⁴⁵Ca²⁺ influx in rat aortic rings in a concentration-dependent manner, with an IC₅₀ of 7 μM, and does not affect norepinephrine- or KCl-induced influx ^[1].
S 8308 (3-100 μM) competitively inhibits angiotensin II-induced contraction of isolated rabbit aortic strips, with a pA₂ value of 5.74, and does not affect the contractions induced by norepinephrine or KCl ^[1].
S 8308 (up to 100 μM) does not inhibit rabbit angiotensin-converting enzyme or rat renin activity^[2].
S 8308 is a non-selective ligand that binds with equal affinity to the AT₁ and AT₂ angiotensin II receptor subtypes in rat adrenal cortical tissue^[7]. In Vivo:S 8308 (CV 2961) (100 mg/kg; p.o. or i.v.; single administration) reduces blood pressure in rats with renal hypertension, and transient oral activity is observed only at the high dose of 100 mg/kg^[3].
S 8308 (30-100 mg/kg; intravenous administration, oral administration; single-dose administration) produces a rapid and transient hypotensive effect in hypertensive rats with renal artery ligation. Both the 30 mg/kg intravenous dose and the 100 mg/kg oral dose reduce the mean arterial pressure by 20 mmHg, with the durations of action being 30 minutes and less than 30 minutes, respectively^[1].
S 8308 (30 mg/kg; intravenous injection) exhibits antihypertensive activity in renal artery ligation-induced hypertensive rats, with an intravenous ED₃₀ of 30 mg/kg^[4].
S 8308 (100 mg/kg; intravenous injection; single bolus administration) is a selective angiotensin II receptor antagonist in spinalized normotensive rats, which significantly blocks the pressor response induced by angiotensin II and does not attenuate the response to norepinephrine or isoprenaline^[5].