A81988

Mice^[2]
B₂^-/- mice and wild-type J129Sv controls (B₂^+/+) are used. Pregnant mice are administered the nonpeptidic antagonist of Ang II AT₁ receptors, A81988 (1.7 mg/kg BW per day in drinking water) or vehicle. At the dose indicated above, A81988 (A-81988) is able to antagonize the vasopressor effect of 10 pmol intravenous Ang II by 75% in mice. At 2 days after birth, the gender of the pups is determined, and each litter is culled to 5 male pups. Mice whose mother is treated during pregnancy continued to receive the antagonist until 180 days of age (treated B₂^+/+ and B₂^-/-, n=25 each group). Untreated controls of each strain (n=25 per group) are provided regular tap water. The animals are housed at a constant room temperature (24±1°C) and humidity (60±3%).
Rats^[3]
Animals are randomly assigned to a normal (0.12 mmol/g chow, n=8 each group), a low (0.02 mmol/g chow, n=8 each group), or a high (0.84 mmol/g chow, n=8 each group) sodium diet. After 15 days, they received the antagonist A81988 (A-81988) for 10 days at the dose of 170 μg/100 g body wt per day orally. In the rat, the antagonist potency of A81988 on the vasopressor response to intravenous angiotensin II is greater than that of losartan by a factor of at least 10. A81988 has no affinity for adrenergic, cholinergic, endothelin, or PAF receptors, and it is >1000-fold more selective for AT1- versus AT₂-receptors. In preliminary experiments, A81988 is able to antagonize the vasopressor effect of 10 pmol intravenous angiotensin II by 75%. Tail-cuff BP is measured twice under basal conditions, every 5 days during A81988 administration, and then after discontinuation of the compound.

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