Synthesis and P2Y receptor activity of a series of uridine dinucleoside 5'-polyphosphates

W Pendergast; B R Yerxa; J G Douglass 3rd; S R Shaver; R W Dougherty; C C Redick; I F Sims; J L Rideout

doi:10.1016/s0960-894x(00)00612-0

Synthesis and P2Y receptor activity of a series of uridine dinucleoside 5'-polyphosphates

Bioorg Med Chem Lett. 2001 Jan 22;11(2):157-60. doi: 10.1016/s0960-894x(00)00612-0.

Authors

W Pendergast¹, B R Yerxa, J G Douglass 3rd, S R Shaver, R W Dougherty, C C Redick, I F Sims, J L Rideout

Affiliation

¹ Inspire Pharmaceuticals, Inc., Durham, NC 27703, USA.

PMID: 11206448
DOI: 10.1016/s0960-894x(00)00612-0

Abstract

A series of dinucleoside 5-polyphosphates UpnU (n = 2-7) was synthesized. Their relative potencies as agonists at the G-protein-coupled receptors P2Y1, P2Y2, P2Y4, and P2Y6 were determined by intracellular calcium measurements using fluorescent imaging techniques. The correlation of phosphate chain length to activities at these receptors is discussed.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Calcium / metabolism
Dinucleoside Phosphates / chemical synthesis
Dinucleoside Phosphates / metabolism*
Humans
Protein Binding
Purinergic P2 Receptor Agonists*
Receptors, Purinergic P2 / metabolism
Spectrometry, Fluorescence
Structure-Activity Relationship
Transduction, Genetic
Tumor Cells, Cultured
Uracil Nucleotides / chemical synthesis
Uracil Nucleotides / metabolism*

Substances

Dinucleoside Phosphates
Purinergic P2 Receptor Agonists
Receptors, Purinergic P2
Uracil Nucleotides
Calcium