Bamifylline similar to theophylline and caffeine is a competitive inhibitor of the cyclic nucleotide phosphodiesterase V

被引:5
作者
Berardi, S
Papponetti, M
Conti, P
Spoto, G
机构
[1] UNIV G DANNUNZIO,IST SCI BIOCHIM,I-66013 CHIETI,ITALY
[2] UNIV G DANNUNZIO,DIV IMMUNOL,INST EXPTL MED,I-66013 CHIETI,ITALY
关键词
bamifylline; theophylline; caffeine; cyclic nucleotide phosphodiesterase V;
D O I
10.1177/039463209600900106
中图分类号
R392 [医学免疫学]; Q939.91 [免疫学];
学科分类号
100102 ;
摘要
Bamifylline was found to be a poor inhibitor of 3',5'-cyclic GMP phosphodiesterase (PDE V) as other methylxanthines such as teophylline and caffeine, The IC50 was respectively 3.24, 2.91, 1.69 mM. Inhibition decreased at higher cGMP concentrations. Lineweaver-Burk plots were linear or nearly linear, Differences in the actions of these inhibitors presumably reflect differences in the molecular requirements for effective interaction at the catalytic site on phosphodiesterase.
引用
收藏
页码:29 / 32
页数:4
相关论文
共 23 条
[1]  
BEAVO JA, 1994, MOL PHARMACOL, V46, P399
[2]   PRIMARY SEQUENCE OF CYCLIC-NUCLEOTIDE PHOSPHODIESTERASE ISOZYMES AND THE DESIGN OF SELECTIVE INHIBITORS [J].
BEAVO, JA ;
REIFSNYDER, DH .
TRENDS IN PHARMACOLOGICAL SCIENCES, 1990, 11 (04) :150-155
[3]   PHARMACOLOGICAL ACTIVITY OF BAMIFYLLINE ON LUNG ANAPHYLAXIS - INVITRO STUDIES [J].
BERTI, F ;
MAGNI, F ;
ROSSONI, G ;
BONGRANI, S ;
SCHIANTARELLI, P .
PHARMACOLOGICAL RESEARCH, 1990, 22 (02) :143-150
[4]  
BERTI F, 1988, ARZNEIMITTEL-FORSCH, V38-1, P40
[5]  
CERU MP, 1989, INT J IMMUNOPATH PH, V2, P9
[6]   RECENT PROGRESS IN UNDERSTANDING THE HORMONAL-REGULATION OF PHOSPHODIESTERASES [J].
CONTI, M ;
NEMOZ, G ;
SETTE, C ;
VICINI, E .
ENDOCRINE REVIEWS, 1995, 16 (03) :370-389
[7]  
FRANCIS SH, 1994, J BIOL CHEM, V269, P22477
[8]   CHARACTERIZATION OF A CALMODULIN-DEPENDENT HIGH-AFFINITY CYCLIC-AMP AND CYCLIC-GMP PHOSPHODIESTERASE FROM MALE-MOUSE GERM-CELLS [J].
GEREMIA, R ;
ROSSI, P ;
MOCINI, D ;
PEZZOTTI, R ;
CONTI, M .
BIOCHEMICAL JOURNAL, 1984, 217 (03) :693-700
[9]  
JIN SLC, 1992, J BIOL CHEM, V267, P18929
[10]   MOLECULAR-CLONING AND EXPRESSION OF HUMAN MYOCARDIAL CGMP-INHIBITED CAMP PHOSPHODIESTERASE [J].
MEACCI, E ;
TAIRA, M ;
MOOS, M ;
SMITH, CJ ;
MOVSESIAN, MA ;
DEGERMAN, E ;
BELFRAGE, P ;
MANGANIELLO, V .
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1992, 89 (09) :3721-3725