Pharmacokinetics and Pharmacological Effect of a New Antiplatelet Agent, Ethyl 2-(4,5-bis(4-methoxyphenyl)thiazol-2-yl)pyrrol-1-ylacetate, after Administration in Guinea Pigs.

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  • 新規抗血小板薬Ｅｔｈｙｌ　２‐［４，５‐ｂｉｓ（４‐ｍｅｔｈｏｘｙｐｈｅｎｙｌ）ｔｈｉａｚｏｌ‐２‐ｙｌ］ｐｙｒｒｏｌ‐１‐ｙｌａｃｅｔａｔｅ（ＫＢＴ‐３０２２）のモルモットにおける体内動態および薬効
Published
1997
DOI
  • 10.2133/dmpk.12.275
Publisher
The Japanese Society for the Study of Xenobiotics

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The pharmacokinetics and pharmacological effect of ethyl 2-[4, 5-bis-(4-methoxyphenyl)thiazol-2-yl]pyrrol-1-ylacetate (KBT-3022), were studied after administration of KBT-3022 to guinea pigs.<BR> 1. The unchanged KBT-3022 was detected in plasma at only early phase after intravenous or oral administration of KBT-3022. KBT-3022 was readily metabolized to desethyl KBT-3022, 2-[4, 5-bis(4-methoxyphenyl)thiazol-2-yl]-pyrrol-1-ylacetic acid.<BR> 2. Both Cmax and AUC00-∞ of desethyl KBT-3022 increased approximately in proportion to the administerd dose over the dose range 5-20 mg/kg.<BR> 3. The levels of radioactivity in the pla telets were 9-44 times higher than those in plasma after oral administration of 14C-KBT-3022, and the level of desethyl KBT-3022 in the platelets was estimated to be about 75 times higher than that in plasma.<BR> 4. TXB2 production was almost completely inhibited by 48h after oral administration of KBT-3022 both at a dose of 1 and 5 mg/kg, but duration of this inhibitory effect at a dose of 5 mg/kg was longer than that at a dose of 1 mg/kg. IC50 value of desethyl KBT-3022 in plasma was estimated to be 1-2 ng/ml.

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