Document Detail


Substitution at the 8-position of 3''-deoxy-cyclic ADP-carbocyclic-ribose, a highly potent Ca2+-mobilizing agent, provides partial agonists.
MedLine Citation:
PMID:  17317189     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
We previously showed that 3''-deoxy-cyclic ADP-carbocyclic-ribose (3''-deoxy-cADPcR, 4) is a stable and highly potent analogue of cyclic ADP-ribose (cADPR, 1), a Ca(2+)-mobilizing second messenger. From these results, we designed and synthesized other 3''-modified analogues of cADPcR having a substituent at the 8-position and found that this modification at the 8-position made them partial agonists. Among these compounds, 8-NH(2)-3''-deoxy-cADPcR (10) was identified as a potent partial agonist with an EC(50) value of 17 nM.
Authors:
Takashi Kudoh; Takashi Murayama; Akira Matsuda; Satoshi Shuto
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't     Date:  2007-02-04
Journal Detail:
Title:  Bioorganic & medicinal chemistry     Volume:  15     ISSN:  0968-0896     ISO Abbreviation:  Bioorg. Med. Chem.     Publication Date:  2007 Apr 
Date Detail:
Created Date:  2007-03-19     Completed Date:  2007-05-18     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9413298     Medline TA:  Bioorg Med Chem     Country:  England    
Other Details:
Languages:  eng     Pagination:  3032-40     Citation Subset:  IM    
Affiliation:
Faculty of Pharmaceutical Sciences, Hokkaido University, Kita-12, Nishi-6, Kita-ku, Sapporo 060-0812, Japan.
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MeSH Terms
Descriptor/Qualifier:
Animals
Calcium / agonists*
Cyclic ADP-Ribose / analogs & derivatives*,  chemical synthesis,  pharmacology
Dose-Response Relationship, Drug
Indicators and Reagents
Ovum / metabolism
Sea Urchins
Spectrometry, Mass, Fast Atom Bombardment
Spectrophotometry, Ultraviolet
Structure-Activity Relationship
Chemical
Reg. No./Substance:
0/3''-deoxy-cyclic ADP-carbocyclic-ribose; 0/Indicators and Reagents; 119340-53-3/Cyclic ADP-Ribose; 7440-70-2/Calcium

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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