title: Inhibition by 2- or/and 8-substituted adenosine derivatives of adenosine deaminase and calmodulin-dependent phosphodiesterase.
abstract: Several 2- or/and 8-substituted adenosine derivatives were tested for their ability to inhibit the adenosine deaminase activity in hog heart and Ca++, calmodulin-dependent phosphodiesterase activity in hog brain. Among these derivatives, 2-piperidyladenosine competitively inhibited not only the adenosine deaminase activity but also the phosphodiesterase activity. Further substitution of this compound with a bulky group at 8-position, 2-piperidyl-8-(8-aminooctylamino)-adenosine, abolished its ability to inhibit the adenosine deaminase activity, but progressively increased in the ability to inhibit the phosphodiasterase activity. On the other hand, 8-monosubstituted adenosine derivatives did not inhibit the adenosine deaminase activity.
mesh_terms: D015105:3',5'-Cyclic-AMP Phosphodiesterases / Q000037:antagonists & inhibitors*; D000241:Adenosine / Q000031:analogs & derivatives* / Q000494:pharmacology; D058892:Adenosine Deaminase Inhibitors; D000818:Animals; D002135:Calcium-Binding Proteins / Q000494:pharmacology*; D002147:Calmodulin / Q000494:pharmacology*; D054677:Cyclic Nucleotide Phosphodiesterases, Type 1; D009206:Myocardium / Q000201:enzymology; D009700:Nucleoside Deaminases / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship; D013552:Swine
chemical_list: D058892:Adenosine Deaminase Inhibitors; D002135:Calcium-Binding Proteins; D002147:Calmodulin; D015105:3',5'-Cyclic-AMP Phosphodiesterases; D054677:Cyclic Nucleotide Phosphodiesterases, Type 1; D009700:Nucleoside Deaminases; D000241:Adenosine