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포스포디에스테라제 III의 저해물인 KR-30075의 흰쥐에서의 약물속도론
이광표(Kwang Pyo Lee),김효진(Hyo Jin Kim),권광일(Kwnag Il Kwon),조송자(Song Ja Cho) 대한약학회 1992 약학회지 Vol.36 No.3
A procedure for the determination of KR-30075 and its metabolites in plasma and urine by high performance liquid chromatography is described. For the study of pharmacokinetic properties of KR-30075, a new PDE III inhibitor, the plasma concentration and urinary excretion after an oral administration of KR-30075 (4mg/kg) in the male rat (Sprague Dawley) were determined by high performance liquid chromatography. The best extraction efficiency of KR-30075 and KR-30072 is obtained with ethyl ether adjusted to pH 4.0. Retention times of both KR-30072 and KR-30075 were within 5 min and resolution was complete at the flow rate of 1.0ml/min. The sensitivity and specificity of this HPLC assay appears to be satisfactory for the pharmacokinetic study of KR-30075 and its metabolites. One-compartment open model with first-order absorption was applied to evaluate the pharmacokinetic parameters of KR-30075 according to Minimum AIC Estimation. Tmax was 1 hr, Cmax was 0.789 +/- 0.31 mcg/ml and elimination half T1/2 was 6.31 min after oral administration of 4mg/kg KR-30075 to male rats.
Kwon, Kwnag-Il,Lee, Sun-Kyung,Yoo, Sung-Eun 충남대학교 약학대학 의약품개발연구소 1992 藥學論文集 Vol.8 No.-
β-Adrenoceptor binding study of β-agonist ((-)NE), β-antagonists ((±)propanolol, labetalol) and PDE inhibitors (imazodan, KR-30045, KR-30075 etc.) was performed using(-)-[^3H]-DHA, as a non-β_1/β_2 selective radioligand. In saunation studies, K_α B_max of(-)-[^3H]-DHA to β-adrenoceptors in rat left ventricle in which both β_1 and β_2 receptors coexist were determined to be 1.5±0.43 nM and 22.0土0.9 fmol/㎎ protein, respectively. (±)Propranolol, labetalol and(-)NE competed for(-)-[^3H]-DHA binding sites in an essentialy monophasic manner with Ki=l7.0±0.40 nM, 57.3±l.30 nM and 1.57±0.95 μM, respectively. All of PDE inhibitors inhibited the(-)-[^3H]-DHA binding by only below l0% even at the high concentration of l0 ^3M. The present results suggest that propranolol, labetalol and NE are non-β_1/β_2 selective antagonists and agonist, respectively. Additionally, this study shows that imazodan and new synthesized PDE inhibitors may hardly have the affinities to β-adrenocetors in cardiac muscle.