PD 123319 ditrifluoroacetate is a potent, selective, non-peptide angiotensin AT2 receptor antagonist with IC50 values of 34 and 210 nM in rat adrenal tissue and brain respectively. PD 123319 ditrifluoroacetate prevents the binding of angiotensin II to the receptor, which blocks signal transduction and causes vasodilation. Intravenous administration of PD 123319 to conscious hypertensive rats elicited an immediate dose-dependent increase in MAP that was sustained for approximately 7.4 min with 3 mg/kg PD123319.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
Induction of angiotensin II subtype 2 receptor-mediated blood pressure regulation in synthetic diet-fed rats.
Tamura M, et al. J Hypertens. 2000 Sep;18(9):1239-46. PMID: 10994755.
Receptor subtypes mediating spinal cardiovascular effects of angiotensin II in rat using losartan and PD 123319.
Park PD, et al. Eur J Pharmacol. 1997 May 20;326(2-3):139-45. PMID: 9196266.
|Related Angiotensin Receptor Products|
A-779 is a specific antagonist of G-protein coupled receptor (Mas receptor).
Angiotensin (1-7) is a synthetic heptapeptide identical to endogenous angiotensin-(1-7), inhibits purified canine angiotensin converting enzyme (ACE) activity with an IC50 of 0.65 μM.
Losartan is an angiotensin II receptor antagonist, competing with the binding of angiotensin II to AT1 receptors with IC50 of 20 nM.
EMA401 (also known as Olodanrigan and PD-126055) is a highly selective angiotensin AT2 antagonist.
|Angiotensin II human
Angiotensin II human is converted by Angiotensin I through removal of two C-terminal residues by the enzyme angiotensin-converting enzyme (ACE). Angiotensin II is mediated by AT1 and AT2 receptors, which are seven transmembrane glycoproteins with 30% sequence similarity.
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