European Journal of Medicinal Chemistry p. 433 - 440 (1988)
Update date:2022-07-29
Topics: Ligand Biological Evaluation Structure-Activity Relationship (SAR) Electrophysiology Dose-Response Curve Adenosine triphosphate (ATP) Radioligand Binding Assay
Howson, William
Taylor, Edwin Michael
Parsons, Michael Edward
Novelli, Riccardo
Wilczynska, Maria Aleksandra
Harris, Deborah Tracy
This paper describes studies carried out on a series of ATP analogues on the guinea pig bladder, a tissue reported to possess purinergic P2X-receptors.Optimisation of the pharmacological experimental technique enabled reproducible responses to ATP to be obtained in the 0.2-100 μM concentration range and the potencies of ATP analogues relative to ATP to be accurately determined.Alterations of the three main parts of the ATP molecule, i.e., the triphosphate, ribose and base, suggest that the triphosphate group is responsible for the efficacy of the agonist, whereas the ribose and adenine moieties are associated with affinity. quantitative analysis / ATP / purinergic / P2X-receptors / guinea pig bladder
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