Activity of novel adenine nucleotide derivatives as agonists and antagonists at recombinant rat P2X receptors

Abstract

Strategy, Management and Health PolicyVenture Capital Enabling TechnologyPreclinical ResearchPreclinical Development Toxicology, Formulation Drug Delivery, PharmacokineticsClinical Development Phases I-III Regulatory, Quality, ManufacturingPostmarketing Phase IVThe effects of structural modifications of adenine nucleotides previously shown to enhance either agonist (2-thioether groups) or antagonist (additional phosphate moieties at the 3'- or 2'-position) properties at P2Y(1) receptors were examined at recombinant rat P2X(1), P2X(2), P2X(3), and P2X(4) receptors expressed in Xenopus oocytes. The potency of P2Y(1) agonists HT-AMP (2-(hexylthio)adenosine-5'-monophosphate) and PAPET (2-[2-(4-a..