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.
 |
Source | Br J Pharmacol (2015). Figure 3. PD 123319 |
| Method | s.c. injection | |
| Cell Lines | male Sprague Dawley rats | |
| Concentrations | 3 mg/kg | |
| 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 |
| Cell Experiment | |
|---|---|
| Cell lines | |
| Preparation method | |
| Concentrations | |
| Incubation time | |
| Animal Experiment | |
|---|---|
| Animal models | spontaneously hypertensive rats |
| Formulation | saline |
| Dosages | 0.36 and 1 mg/kg/min |
| Administration | intravenous |
| Molecular Weight | 508.61 |
| Formula | C31H32N4O3 |
| CAS Number | 130663-39-7 |
| Solubility (25°C) | DMSO 90 mg/mL Water 90 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.
[3] Siragy H. Am J Cardiol. Angiotensin II receptor blockers: review of the binding characteristics.
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