C. Muller, J. Sandoval-Ramirez, U. Schobert, U. Geis, W. Frobenius, and K. Klotz. Bioorg Med Chem, 6 (6):
707-19(June 1998)Muller, C E Sandoval-Ramirez, J Schobert, U Geis, U Frobenius, W
Klotz, K N England Bioorganic & medicinal chemistry Bioorg Med Chem.
1998 Jun;6(6):707-19..
Abstract
8-(Sulfostyryl)xanthine derivatives were synthesized as water-soluble
A2A-selective adenosine receptor (AR) antagonists. meta- and para-sulfostyryl-DMPX
(3,7-dimethyl-1-propargylxanthine) derivatives 11a and 11b exhibited
high affinity to rat A2A-AR in submicromolar concentrations, and
were 20- to 30-fold selective versus rat A1-AR. Styryl-DMPX derivatives
were inactive at human A2B- and A3-AR. 1,3-Dipropyl-8-p-sulfostyrylxanthine
(13) or only a 7-methyl derivative (14) showed similar (13) or higher
(14) A2A affinity than 11a and 11b but showed no (13) or only a low
degree (14) of selectivity versus A1-, A2B-, and A3-AR. The A2A-selective
sulfostyryl-DMPX derivatives exhibit high water-solubility and may
be useful research tools for in vivo studies.
Muller, C E Sandoval-Ramirez, J Schobert, U Geis, U Frobenius, W
Klotz, K N England Bioorganic & medicinal chemistry Bioorg Med Chem.
1998 Jun;6(6):707-19.
%0 Journal Article
%1 Muller1998
%A Muller, C. E.
%A Sandoval-Ramirez, J.
%A Schobert, U.
%A Geis, U.
%A Frobenius, W.
%A Klotz, K. N.
%D 1998
%J Bioorg Med Chem
%K & A2A Acids/*chemical Adenosine Animals Arylsulfonic Assay CHO Central Cerebral Concentration Cortex/metabolism Cricetinae Humans Hydrogen-Ion Magnetic Nervous P1/*antagonists Proteins/antagonists Purinergic Radioligand Rats Recombinant Relationship Resonance Solubility Spectroscopy Stimulants/*chemical Structure-Activity Styrenes/*chemical System Xanthines/*chemical inhibitors/biosynthesis synthesis/chemistry/metabolism/pharmacology Receptor Cell
%N 6
%P 707-19
%T 8-(Sulfostyryl)xanthines: water-soluble A2A-selective adenosine receptor
antagonists
%U http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&dopt=Citation&list_uids=9681137
%V 6
%X 8-(Sulfostyryl)xanthine derivatives were synthesized as water-soluble
A2A-selective adenosine receptor (AR) antagonists. meta- and para-sulfostyryl-DMPX
(3,7-dimethyl-1-propargylxanthine) derivatives 11a and 11b exhibited
high affinity to rat A2A-AR in submicromolar concentrations, and
were 20- to 30-fold selective versus rat A1-AR. Styryl-DMPX derivatives
were inactive at human A2B- and A3-AR. 1,3-Dipropyl-8-p-sulfostyrylxanthine
(13) or only a 7-methyl derivative (14) showed similar (13) or higher
(14) A2A affinity than 11a and 11b but showed no (13) or only a low
degree (14) of selectivity versus A1-, A2B-, and A3-AR. The A2A-selective
sulfostyryl-DMPX derivatives exhibit high water-solubility and may
be useful research tools for in vivo studies.
@article{Muller1998,
abstract = {8-(Sulfostyryl)xanthine derivatives were synthesized as water-soluble
A2A-selective adenosine receptor (AR) antagonists. meta- and para-sulfostyryl-DMPX
(3,7-dimethyl-1-propargylxanthine) derivatives 11a and 11b exhibited
high affinity to rat A2A-AR in submicromolar concentrations, and
were 20- to 30-fold selective versus rat A1-AR. Styryl-DMPX derivatives
were inactive at human A2B- and A3-AR. 1,3-Dipropyl-8-p-sulfostyrylxanthine
(13) or only a 7-methyl derivative (14) showed similar (13) or higher
(14) A2A affinity than 11a and 11b but showed no (13) or only a low
degree (14) of selectivity versus A1-, A2B-, and A3-AR. The A2A-selective
sulfostyryl-DMPX derivatives exhibit high water-solubility and may
be useful research tools for in vivo studies.},
added-at = {2010-12-14T18:12:02.000+0100},
author = {Muller, C. E. and Sandoval-Ramirez, J. and Schobert, U. and Geis, U. and Frobenius, W. and Klotz, K. N.},
biburl = {https://www.bibsonomy.org/bibtex/2e766b5c0ae2f5e10cb31e62c4e2f46f4/pharmawuerz},
endnotereftype = {Journal Article},
interhash = {435dcf05b9c795e90a14c6d07c0a5341},
intrahash = {e766b5c0ae2f5e10cb31e62c4e2f46f4},
issn = {0968-0896 (Print) 0968-0896 (Linking)},
journal = {Bioorg Med Chem},
keywords = {& A2A Acids/*chemical Adenosine Animals Arylsulfonic Assay CHO Central Cerebral Concentration Cortex/metabolism Cricetinae Humans Hydrogen-Ion Magnetic Nervous P1/*antagonists Proteins/antagonists Purinergic Radioligand Rats Recombinant Relationship Resonance Solubility Spectroscopy Stimulants/*chemical Structure-Activity Styrenes/*chemical System Xanthines/*chemical inhibitors/biosynthesis synthesis/chemistry/metabolism/pharmacology Receptor Cell},
month = Jun,
note = {Muller, C E Sandoval-Ramirez, J Schobert, U Geis, U Frobenius, W
Klotz, K N England Bioorganic \& medicinal chemistry Bioorg Med Chem.
1998 Jun;6(6):707-19.},
number = 6,
pages = {707-19},
shorttitle = {8-(Sulfostyryl)xanthines: water-soluble A2A-selective adenosine receptor
antagonists},
timestamp = {2010-12-14T18:20:40.000+0100},
title = {8-(Sulfostyryl)xanthines: water-soluble A2A-selective adenosine receptor
antagonists},
url = {http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&dopt=Citation&list_uids=9681137},
volume = 6,
year = 1998
}