Indobufen, a new inhibitor of platelet aggregation. Studies in guinea pigs

Bergamaschi, M.; Ceserani, R.; Pierucci, L.; Pogliani, E; A, Spelta

doi:10.1016/s0031-6989(79)80090-9

Cited by 13 publications

(2 citation statements)

References 14 publications

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“…indobufen thesized drug has shown in in vitro and ex vivo animal experiments to inhibit APD-and collagen-induced release reaction of platelets.12J3 The drug inhibits prostaglandin and thromboxane synthesis and collagen-induced 14C-serotonin release from guinea pig platelets without affecting 14C-serotonin uptake. 12 Rats are protected from endotoxin shock: both platelet decrease and mortality induced by endotoxins are significantly inhibited by previous administration of indob~fen. '~ Acute toxicity of indobufen is low: L D~o by the oral route is about 380 mg/kg in the rat and between 700 and 850 mg/kg in the mouse.…”

mentioning

confidence: 99%

Clinical Pharmacology Studies with Indobufen (K 3920): Inhibitor of Platelet Aggregation

Vinazzer¹,

Fuccella²

1980

The Journal of Clinical Pharma

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confidence: 99%

Clinical Pharmacology Studies with Indobufen (K 3920): Inhibitor of Platelet Aggregation

Vinazzer¹,

Fuccella²

1980

The Journal of Clinical Pharma

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“…The drugs to be compared with standard PGEg were tested with at least two doses, chosen in order to obtain good centering, i.e., a nonsignificant difference between preparations,24 When a drug was inactive, the dose was raised to a maximum of 20 Mg/kg iv. Six animals were used for each dose.…”

Section: Methodsmentioning

confidence: 99%

Azaprostaglandin analogs. Synthesis and biological properties of 11-azaprostaglandin derivatives

Barco¹,

Benetti²,

Pollini³

et al. 1981

J. Med. Chem.

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New nitrogen analogues of prostaglandins (11, 11a, 12, and 12a) have been synthesized starting from a 4,5-disubstituted 2-pyrrolidinone nucleus (5 and 5a) containing one side chain and a suitable functionality for elaborating the second one. These analogues had no better activity than natural prostaglandins in vitro [guinea pig ileum and trachea, rat stomach fundus strip, uterus and portal vein, ADP-induced guinea pig platelet-rich plasma (PRP) aggregation]. They similarly lacked any interesting activity in vivo [anesthetized rat blood pressure, stress, and acetylsalycilic acid (ASA) induced gastric lesions in rat].

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Different sensitivities of prostaglandin-cyclooxygenases in blood platelets and coronary arteries against non-steroidal antiinflammatory drugs

Schrör

Sauerland

Kühn

et al. 1980

Naunyn-Schmiedeberg's Arch. Pharmacol.

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The action of the non-steroidal antiinflammatory drugs indomethacin, tiaprofenic acid, diclofenac and meclofenamate on vascular and platelet-cyclooxygenases was studied by measuring the arachidonic acid-induced thromboxane A2 (TXA2)-formation of washed human platelets and prostacyclin (PGI2)-formation of bovine coronary artery rings. TXA2 was bioassayed as RCS on rabbit aorta strips, PGI2 in terms of its antiaggregatory activity on ADP-induced aggregation of human platelet-rich plasma. All of the substances studied produced concentration-dependent inhibition of PGI2- and RCS-release. The IC50 [micrometer] in inhibition of RCS-formation was 0.019 for indomethacin, 0.070 for tiaprofenic acid but 44.9 for meclofenamate and 63.2 for diclofenac. The IC50 [micrometer] in inhibition of PGI2-release was 0.42 for diclofenac, 0.63 for indomethacin and 0.99 for tiaprofenic acid. The data suggest (1) high sensitivity of human platelet-cyclooxygenase against indomethacin and tiaprofenic acid, (2) different sequence of the substances studied in inhibiting arachidonic acid-induced TXA2- and PGI2-formation. The possible therapeutic value of selective inhibition of platelets and vascular cyclooxygenases is discussed.

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Indobufen, a new inhibitor of platelet aggregation. Studies in guinea pigs

Cited by 13 publications

References 14 publications

Clinical Pharmacology Studies with Indobufen (K 3920): Inhibitor of Platelet Aggregation

Clinical Pharmacology Studies with Indobufen (K 3920): Inhibitor of Platelet Aggregation

Azaprostaglandin analogs. Synthesis and biological properties of 11-azaprostaglandin derivatives

Different sensitivities of prostaglandin-cyclooxygenases in blood platelets and coronary arteries against non-steroidal antiinflammatory drugs

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