University of Minnesota

Hon-Cheung Lee

Timothy F Walseth

Robert A Aarhus

Cyclic ADP-ribose (cADPR) analogs block cADPR from releasing Ca.sup.+2, and also inhibit cADPR from potentiating Ca.sup.+2 release induced by either divalent cations or by caffeine. 8-amino-cADPR and two other 8-substituted analogs were also synthesized. Both 8-Br- and 8-azido-cADPR were also antagonists, although with less potency than 8-amino-cADPR. These results show that alterations at the 8-position of the adenine group do not inhibit cADPR from binding to its receptor but do eliminate the ability of the metabolite to activate the Ca.sup.+2 release mechanism.

Growing community of inventors

Woodbury, MN, United States of America

Hon-Cheung Lee