Cyclic ADP ribose antagonists
US5486604A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | Nov 1, 1993 |
| Grant date | Jan 23, 1996 |
| Priority date | — |
| Expiry date | Nov 1, 2013 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07H19/207
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
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.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.