[3H]A-81988, a potent, selective, competitive antagonist radioligand for angiotensin AT1 receptors

  • Eur J Pharmacol. 1994 Mar 15;267(1):49-54. doi: 10.1016/0922-4106(94)90223-2.
A A Hancock  1 ,  B W Surber ,  G Rotert ,  S Thomas ,  A S Tasker ,  B K Sorensen ,  A D Vodenlich ,  T J Opgenorth ,  D J Kerkman ,  J F DeBernardis
Affiliations
  • 1. Department 47C, AP-10, Abbott Laboratories, Abbott Park, IL 60064.
PMID: 8206129 DOI: 10.1016/0922-4106(94)90223-2
Abstract

Abbott-81988 (A-81988), 2-(N-n-Propyl-N-[(2'-[1H-tetrazol-5-yl]biphenyl-4- yl)methyl]amino)pyridine-3-carboxylic acid is a potent, competitive, non-peptidic antagonist of angiotensin AT1 receptors. A-81988 was labeled with tritium to high specific activity (16 Ci/mmol) and radioligand binding assays performed in rat liver membranes. [3H]A-81988 bound with high affinity (KD = 0.57 nM) and the KD determined from kinetics assays was similar. Non-specific binding (defined with 10(-6) M angiotensin-II) was very low (< 6% at the KD). The binding of [3H]A-81988 was competitive and exhibited appropriate pharmacological specificity for compounds acting at angiotensin AT1 receptors. These properties demonstrate that [3H]A-81988 will be a useful radioligand for studies of angiotensin AT1 receptors in various tissues.

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