Effect of KBT-3022, a New Diphenylthiazole Derivative, on Platelet Functions
| Autor: | Koichi Yokota, Noriko Yamamoto, Akira Yamashita, Minoru Oda, Yasuo Morimoto |
|---|---|
| Rok vydání: | 1995 |
| Předmět: |
Blood Platelets
Serotonin Ultraviolet Rays Metabolite Guinea Pigs Administration Oral Pharmaceutical Science Biology Pharmacology Ticlopidine Hydrochloride Mice chemistry.chemical_compound Thrombin Species Specificity medicine Animals Edema Humans Pyrroles Platelet Platelet activation Arachidonic Acid Aspirin Biological activity Rats Adenosine Diphosphate Thiazoles Adenosine diphosphate chemistry Biochemistry Erythema Gastric Mucosa Arachidonic acid Collagen Rabbits Platelet Aggregation Inhibitors medicine.drug |
| Zdroj: | Journal of Pharmacy and Pharmacology. 47:768-774 |
| ISSN: | 2042-7158 0022-3573 |
| Popis: | The effects of KBT-3022 and its metabolite desethyl KBT-3022 on platelet aggregation were determined in rat, guinea-pig, rabbit and human platelets in-vitro and ex-vivo. KBT-3022 and desethyl KBT-3022 inhibited platelet aggregation induced by arachidonic acid and collagen in-vitro more potently than aggregation induced by adenosine diphosphate, platelet-activating factor or thrombin, as well as by acetylsalicylic acid, and their effects were approximately 100 times more potent than those of acetylsalicylic acid. Desethyl KBT-3022, but not KBT-3022 or acetylsalicylic acid, inhibited thrombin-induced aggregation and 5-hydroxytryptamine release from platelets more potently than ticlopidine hydrochloride at higher concentrations. Oral administration of KBT-3022 inhibited both arachidonic acid- and collagen-induced platelet aggregation and reduced platelet retention in a glass-bead column approx. 100 times more potently than acetylsalicylic acid. KBT-3022 showed little or no anti-inflammatory effect on either ultraviolet-induced erythema or arachidonic acid induced ear oedema, and had lower gastro-ulcerogenicity than acetylsalicylic acid. These results suggest that KBT-3022 is a potent inhibitor of platelet activation with weak side-effects. |
| Databáze: | OpenAIRE |
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