Mechanism of action of two new pyrimidoquinoline and isoquinoline derivatives in human platelets

Thrombosis Research

Volumn 87, Issue 5, 1997, Pages 483-492

  Leoncini, Giuliana ^a   Signorello, Maria Grazia ^a   Grossi, Gian Carlo ^b   Di Braccio, Mario ^b  

^a UNIVERSITY OF GENOA   (Italy)

^b UNIVERSITY OF GENOA   (Italy)

Author keywords

Antiplatelet activity; CAMP; CAMP phosphodiesterase; Pyrimidoquinoline and isoquinoline derivatives

Indexed keywords

2 (1 PIPERAZINYL) 4H PYRIMIDO[2,1 A]ISOQUINOLIN 4 ONE; 3 (1 PIPERAZINYL) 1H PYRIMIDO[1,2 A]QUINOLIN 1 ONE; ADENOSINE DIPHOSPHATE; ANTITHROMBOCYTIC AGENT; AQ 11; CALCIMYCIN; CYCLIC AMP; IQ 3B; PHORBOL 12 ACETATE 13 MYRISTATE; UNCLASSIFIED DRUG;

ARTICLE; CALCIUM CELL LEVEL; DOSE RESPONSE; DRUG EFFECT; DRUG POTENCY; ENZYME INHIBITION; HUMAN; HUMAN CELL; PHOSPHATE METABOLISM; PRIORITY JOURNAL; THROMBOCYTE AGGREGATION INHIBITION;

EID: 0030812291     PISSN: 00493848     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0049-3848(97)00165-5     Document Type: Article

References (14)

1. ROMA, G., DI BRACCIO, M., LEONCINI, G, and APRILE, B. 1,2- Fused pyrimidines VI. Substituted 2-amino-4H-pyrido[1,2-a]pyrimidin-4-ones with antiplatelet activity, II Farmaco 48, 1225-1238, 1993.
2. DI BRACCIO, M., ROMA, G. and LEONCINI, G. 1,2-Fused pyrimidines VII. 3-(Dialkylamino)-1H-pyrimido[1,2-a]quinolin-1-ones and 2-(dialkylamino)-4H-pyrimido[2,1-a]isoquinolin-4-ones as antiplatelet compounds. Eur J Med Chem 30, 27-38, 1995.
3. LEONCINI, G., SIGNORELLO, M.G, ROMA, G. and DI BRACCIO, M. Effect of 2-(1-piperazinyl)-4H-pyrido[1,2-a]pyrimidin-4-one (AP155) on human platelets "in vitro". Biochem Pharmacol, 1997 in press.
4. LEONCINI, G., MARESCA, M., BUZZI, E., PIANA, A. and ARMANI, U. Platelet of patients affected with essential thrombocytemia are abnormal in plasma membrane and adenine nucleotide content. Eur J Hemat 44, 115-119, 1990.
5. BORN, G.V.R. Aggregation of blood platelets by adenosine diphosphate and its reversal. Nature 194, 927-929, 1962.
6. LEONCINI, G., MARESCA, M., COLAO, C., BUZZI, E., MAZZEI, M. and BALBI, A. Antiplatelet effect of 2-(diethylamino)-7-hydroxychromone. Phamacol Res 23, 139-148, 1991.
7. YAMAGUCHI, A., SUZUKI, H., TANOUE, K. and YAMAZAKI, H. Simple method of aequorin loading into platelets using dimethyl sulfoxide. Tromb Res 44, 165-174, 1986.
8. SCATCHARD, G. The attractions of proteins for small molecules and ions. Ann NY Acad Sci 57, 543-548, 1949.
9. LEREA, K.M., GLOMSET, J.A. and KREBS, E.G. Agents that elevate cAMP levels in platelets decrease thrombin binding. J Biol Chem 262, 282-288, 1987.
10. SIESS, W., GRUNBERG, B. and LUBER, K. Functional relationship between cyclic AMP-dependent protein phosphorylation and platelet inhibition. In: Mechanisms of platelet activation and control. K.S. Authi, S.P. Watson and V.V. Kakkar (eds.) pp. 229-235, Plenum Press, New York (1993).
11. CATTANEO, M., AKKAWAT, B., LECCHI, A., CIMMINIELLO, C., CAPITANIO, A.M. and MANNUCCI, P.M. Ticlopidine selectively inhibits human platelet responses to adenosine diphosphate. Thromb Haemostasis 66, 694-699, 1991.
12. HAWIGER, J., PARKINSON, S. and TIMMONS, S. Prostacyclin inhibits mobilization of fibrinogen-binding sites on human ADP and thrombin-treated platelets. Nature 283, 195-197, 1980.
13. 2+ influx in platelets: Activation by thrombin and by the depletion of the stores. Effect of cyclic nucleotides. Biochem J 303, 599-605, 1994.
14. 3 subunit. Biochem J 314, 769-79, 1996.