Full metadata record
DC Field | Value | Language |
---|---|---|
dc.contributor.author | 유혜현 | - |
dc.date.accessioned | 2019-06-24T07:28:34Z | - |
dc.date.available | 2019-06-24T07:28:34Z | - |
dc.date.issued | 2007-08 | - |
dc.identifier.citation | ACTA PHARMACOLOGICA SINICA, v. 28, No. 8, Page. 1247-1253 | en_US |
dc.identifier.issn | 1671-4083 | - |
dc.identifier.issn | 1745-7254 | - |
dc.identifier.uri | https://onlinelibrary.wiley.com/doi/abs/10.1111/j.1745-7254.2007.00611.x | - |
dc.identifier.uri | https://repository.hanyang.ac.kr/handle/20.500.11754/106838 | - |
dc.description.abstract | Aim: To investigate the pharmacokinetic profile and tissue distribution of a novel phosphodiesterase type 5 inhibitor, 5-ethyl-2-{5-[4-(2-hydroxy-ethyl)-piperazine-1-sulfonyl]-2-propoxy-phenyl}-7-propyl-3,5-dihydro-pyrrolo(3,2-d)pyrimidin-4-one (SK-3530), in rats after administration of the C-14-labeled compound. Methods: The pharmacokinetic parameters of SK-3530 were measured based on the total radioactivity and parent SK-3530 concentration in rat plasma after intravenous and oral administration. The tissue distribution of total radioactivity after a single oral administration of [C-14]SK-3530 at a dose of 40 mg/kg was assayed. The plasma protein binding rates of SK-3530 were assessed by in vitro and ex vivo assay. Results: The total radioactivity profiles showed linear pharmacokinetics. The maximum plasma concentration and area under the curve of the parent SK3530 were 10%-20% compared to those of the total radioactivity. After the oral administration of [C-14]SK-3530, the radioactivity was widely distributed in all tissues, and the tissue/plasma ratio of the radioactivity 1 h after administration was calculated as 0.5-2.6 with the exception of excretory organs. Arelatively high penetration was shown in the adrenal glands, liver, and lung. In vitro and ex vivo plasma protein binding assay by ultrafiltration showed a considerably high binding rate of more than 97%. Conclusion: SK-3530 was relatively well absorbed in the gastrointestinal tract and showed linear pharmacokinetics over the investigated dose range. SK-3530 had low oral bioavailability due to a high, first-pass metabolism. | en_US |
dc.language.iso | en_US | en_US |
dc.publisher | BLACKWELL PUBLISHING | en_US |
dc.subject | SK-3530 | en_US |
dc.subject | PDE5 inhibitor | en_US |
dc.subject | pharmacokinetics | en_US |
dc.subject | tissue distribution | en_US |
dc.subject | rats | en_US |
dc.title | Pharmacokinetics and tissue distribution of a novel PDE5 inhibitor, SK-3530, in rats | en_US |
dc.type | Article | en_US |
dc.relation.volume | 28 | - |
dc.identifier.doi | 10.1111/j.1745-7254.2007.00611.x | - |
dc.relation.page | 1247-1253 | - |
dc.relation.journal | ACTA PHARMACOLOGICA SINICA | - |
dc.contributor.googleauthor | Yoo, Hye-hyun | - |
dc.contributor.googleauthor | Kim, Nam-sun | - |
dc.contributor.googleauthor | Im, Guang-jin | - |
dc.contributor.googleauthor | Kim, Dong-hyun | - |
dc.relation.code | 2007200143 | - |
dc.sector.campus | E | - |
dc.sector.daehak | COLLEGE OF PHARMACY[E] | - |
dc.sector.department | DEPARTMENT OF PHARMACY | - |
dc.identifier.pid | yoohh | - |
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