Abstract：
:The inhibitory effects of anion channel blockers were evaluated on aggregation, intracellular Ca2+ rises, and the production of arachidonic acid metabolites in human platelets. Inhibitors included five anion channel blockers: phloretin, probenecid, pyridoxal phosphate, 4,4'-diisothiocyano-2,2'-disulfonic acid stilbene (DIDS) and 4-acetamido-4'-isothiocyanostilbene-2,2'-disulfonic acid (SITS). The degree of inhibition by each of these agents was dose-dependent on thrombin-activated platelet function. These agents generally had no significant inhibitory effects on ionomycin-activated platelet functions. It is suggested that anion mobilization plays a major role in the receptor-mediated activation of platelet functions, but only a minor role in Ca2+ ionophore-induced platelet activation. It is also suggested that several agents may have properties unrelated to anion channel blockers. Phloretin may be a selective cyclooxygenase inhibitor, and probenecid may inhibit phospholipase A2. DIDS and SITS may interfere with certain aggregation-inducing mechanisms.
journal_name
Biochem Pharmacoljournal_title
Biochemical pharmacologyauthors
Ozaki Y,Matsumoto Y,Yatomi Y,Higashihara M,Kariya T,Shoji Kdoi
10.1016/0006-2952(89)90069-5subject
Has Abstractpub_date
1989-07-01 00:00:00pages
2147-52issue
13eissn
0006-2952issn
1873-2968pii
0006-2952(89)90069-5journal_volume
38pub_type
杂志文章abstract：:From routine in vitro drug-transporter inhibition assays, observed inhibition is typically assumed from direct interaction with the transporter. Other mechanisms that possibly reduce substrate uptake are not frequently fully examined. The objective of this study was to investigate the association of transporter inhibi...
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pub_type： 杂志文章
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journal_title：Biochemical pharmacology
pub_type： 杂志文章
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更新日期：1989-04-15 00:00:00
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更新日期：1987-01-01 00:00:00
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pub_type： 杂志文章
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