Action of AD6 (8-monochloro-3-beta-diethylaminoethyl-4-methyl-7-ethoxycarbonylmethoxy coumarin) on human platelets in vitro

Prosdocimi, Marco; Zatta, A.; Gorio, A.; Zanetti, Adrians; Dejana, Elisabetta

doi:10.1007/bf00504872

Cited by 27 publications

(11 citation statements)

References 17 publications

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“…These substances, mainly localized in the (Y granules, are P-thromboglobulin, platelet factor 4, and platelet-derived growth factor (PDGF). Cloricromene has been found to inhibit the release of thromboxane A, in platelets induced by several platelet-aggregating agents (15,21,25). This effect is likely to be caused by inhibition of arachidonic acid release from the cellular membranes.…”

Section: Effects On Plateletsmentioning

confidence: 99%

“…Platelet aggregation induced by several aggregating agents such as arachidonic acid, collagen, and ADP was significantly reduced by cloricromene in a dose-dependent manner. The lowest concentration of cloricromene, able to inhibit platelet aggregation, is 1 pmol/L and the overall effects on platelets are more evident when threshold concentrations (minimal concentrations capable of inducing aggregation in untreated platelets) of aggregating substances are used (15,20,21,24,25). Furthermore, cloricromene also inhibits washed platelet aggregation induced by platelet-activating factor (PAF) in combination with epinephrine.…”

Section: Effects On Plateletsmentioning

confidence: 99%

“…This effect is likely to be caused by inhibition of arachidonic acid release from the cellular membranes. Furthermore, following platelet activation, induced either spontaneously or by plateletaggregating agents, the drug blocks the release of a protein from (Y granules (25,35,39,40).…”

Section: Effects On Plateletsmentioning

confidence: 99%

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Cloricromene

Squadrito

Prosdocimi

Altavilla

et al. 1991

Cardiovascular Drug Reviews

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Section: Effects On Plateletsmentioning

confidence: 99%

Section: Effects On Plateletsmentioning

confidence: 99%

See 1 more Smart Citation

Cloricromene

Squadrito

Prosdocimi

Altavilla

et al. 1991

Cardiovascular Drug Reviews

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“…(a vasoconstrictor) synthesis from platelets [23], Platelets. Cloricromene inhibits platelet aggregation [24] and secretion [25], reduces thromboxane B2 formation by incubated platelets [23] and inhibits the activation of human platelets by ADP alone or in combina tion with adrenaline [26].…”

Section: Neutrophils and Endothelial Adhesionmentioning

confidence: 99%

Effects of Cloricromene on Ischemia-Reperfusion Myocardial Damage in the Rabbit

Milei¹,

Ferreira²,

Grana³

et al. 1992

Cardiology

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Cloricromene, a compound with several biological activities which suggest a therapeutic role in thrombosis or ischemic disease, has been studied for its effects on the extension of myocardial damage and the production of oxygen free radicals during periods of ischemia and reperfusion. In twenty rabbits the left anterior descending coronary artery (LAD) was occluded and cloricromene (3.6 µg /kg /min; n = 10) or placebo (n = 10) were continuously infused. After 50 min the artery was reopened and after 20 min of reperfusion a biopsy was obtained from the anterior wall of the heart in the LAD area and from the posterior wall (control myocardium) prior to sacrifice. Both samples were used for chemiluminescence measurement (free-radical production) and ultrastructural studies. In the placebo group all rabbits showed ST-segment changes during ischemia and reperfusion arrhythmias, while in the cloricromene group there were transient ST elevations in 4 animals which reverted at higher infusion rates of the drug. The chemiluminescence values were 18,017 ± 1,956 and 8,583 ± 918 cpm/mg protein (p < 0.001) in the anterior and posterior walls of the left ventricle, respectively, for the placebo group, and 7,767 ± 992 and 8,333 ± 832 cpm/mg protein (NS), respectively, for the cloricromene group. The ratio between the anterior and posterior wall was 2.27 ± 0.37 for the placebo group versus 0.95 ± 0.11 for the cloricromene group (p < 0.001). In ultrastructural studies, the anterior wall in the placebo group showed irreversible myocyte injury and infarction as well as mitochondrial damage. Samples from the cloricromene-treated group showed, in general, preservation of myocyte architecture or minor signs of injury. These results illustrate clearly the protective effect of cloricromene during damage induced by ischemia and reperfusion in the rabbit.

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“…This compound has been shown to inhibit platelet function in vitro and in vivo (Prosdocimi et al, 1985(Prosdocimi et al, , 1986 and to cause vasodilation in vivo (Aporti et al, 1978). In platelets and neutrophils it reduces arachidonic acid release from membrane phospholipids by interfering with phopholipase A2 activation resulting in an inhibition of platelet-activating-factor synthesis (Ribaldi et al, 1996).…”

Section: Discussionmentioning

confidence: 98%