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Discovery of a potent atrial natriuretic peptide antagonist for ANPA receptors in the human neuroblastoma NB-OK-1 cell line

par Delporte, Christine ;Winand, Jacques ;Poloczek, Piotr ;Von Geldern, Thomas W.;Christophe, Jean
Référence European journal of pharmacology, 224, 2-3, page (183-188)
Publication Publié, 1992-12

Article révisé par les pairs

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Résumé :

The effects of seven competitive atrial natriuretic peptide (ANP) receptor antagonists were compared on cultured human neuroblastoma NB-OK-1 cells expressing exclusively ANPA receptors, by evaluating their capacity to inhibit [125I]ANP binding and to suppress ANP-stimulated cyclic GMP elevation. In ANP analogues with a shortened Cys7-Cys18 bridge, Asp13 and a hydrophobic Tic residue at position 16 expressed antagonistic activity, while Ala16 provoked lower antagonistic potency and Phe16 induced receptor activation. The binding affinity of A71915 ([Arg6,Chs8]ANP-(6-15)-D-Tic-Arg-Cya-NH2), the most potent antagonist (with a pKi of 9.18 and a pA2 of 9.48) was only 22 times less lower than that of the agonist ANP-(1-28). © 1992.