PD123319 shows inhibition potency in both rat adrenal and brain binding assay with IC50 values of 34nM and 210nM. At high concentrations PD123319 blocks the beneficial effects of the AT2-agonist LP2-3 on RVH. At low concentrations PD123319 attenuates cardiopulmonary injury by reducing pulmonary inflammation and fibrosis and preventing PAH-induced RVH but does not affect alveolar and vascular development in newborn rats with experimental BPD. Administration of PD123319 can suppress the generation of cyclic guanosine monophosphate and increase the production of prostaglandin E2. Besides that, administration of PD-123319 does not inﬂuence the effect of Ang II on protein tyrosine phosphorylation or thymidine incorporation.
|Animal models||spontaneously hypertensive rats|
|Dosages||0.36 and 1 mg/kg/min|
|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.
|Solubility||DMSO 100 mg/mL
Water 100 mg/mL
|Source||Br J Pharmacol (2015). Figure 3. PD 123319|
|Cell Lines||male Sprague Dawley rats|
|Incubation Time||2 weeks|
|Results||Remarkably, C21 treatment of MCT rats reversed both interstitial and perivascular fibrosis, an effect that was blocked by PD-123319|
Angiotensin II type 2 receptor ligand PD123319 attenuates hyperoxia-induced lung and heart injury at a low dose in newborn rats.
Wagenaar GT, et al. Am J Physiol Lung Cell Mol Physiol. 2014 Aug 1;307(3):L261-72. PMID: 24951776.
Effects of acid challenges on type 2 angiotensin II receptor-sensitive ammonia production by the proximal tubule.
Nagami GT, et al. Am J Physiol Renal Physiol. 2014 Jul 1;307(1):F53-7. PMID: 24829505.
Angiotensin II receptor blockers: review of the binding characteristics.
Siragy H. Am J Cardiol. 1999 Nov 18;84(10A):3S-8S. PMID: 10588088.
Synthesis and structure-activity relationships of a novel series of non-peptide angiotensin II receptor binding inhibitors specific for the AT2 subtype.
Blankley CJ, et al. J Med Chem. 1991 Nov;34(11):3248-60. PMID: 1956044.
|Related Angiotensin Receptor Products|
Tranilast is an antiallergic agent.
Olmesartan Medoxomil is a compound which is hydrolyzed to olmesartan that is a selective AT1 subtype angiotensin II receptor antagonist.
Olmesartan is an angiotensin II receptor antagonist with an IC50 of 7.7 nM.
Losartan potassium is a selective non-peptide angiotensin AT1 receptor antagonist.
|PD 123319 ditrifluoroacetate
PD 123319 ditrifluoroacetate is a potent, selective, non-peptide angiotensin AT2 receptor antagonist.
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