Cyclic ADP ribose antagonists

Details Cyclic ADP ribose antagonists Cyclic ADP ribose antagonists

1993-11-01

1996-01-23

Robinson, Douglas W.

Organic compounds -- part of the class 532-570 series

Organic compounds

Carbohydrates or derivatives

536 262, 536 2621, 536 2623, 536 2624, C07H 1923, A61K 5100

Patent

active

054866049

ABSTRACT:
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.

REFERENCES:
patent: 5202426 (1993-04-01), Strumwasser et al.
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