Abstract：
:Theophylline, caffeine, isobutylmethylxanthine, papaverine, N6-cyclohexyladenosine, N6-allyl-N6-cyclohexyladenosine ( ACHA ) and N6-L-phenylisopropyladenosine (L-PIA) inhibited the transport of adenosine, uridine and hypoxanthine in Novikoff rat hepatoma cells. The IC50 values for the inhibition of uridine transport ranged from 5 microM for ACHA to 3200 microM for caffeine and were inversely proportional to the lipid solubility of the inhibitors. L-PIA and papaverine inhibited uridine influx in a non-competitive manner, having a greater influence on the Michaelis-Menten constant than on maximum velocity, just as observed previously for the inhibition of nucleoside transport by dipyridamole and hypoxanthine. [3H]L-PIA rapidly accumulated in Novikoff cells at 25 degrees to about five times higher levels than present extracellularly. The initial rates of L-PIA uptake were directly proportional to its extracellular concentration between 0.01 and 240 microM and not affected by structurally related analogs, methylxanthines, papaverine, dipyridamole, or 2 mM uridine, but were dependent on temperature. We conclude that L-PIA inhibits nucleoside transport in these cells without being significantly transported by the carrier, that it equilibrates rapidly across the plasma membrane without carrier mediation consistent with its lipophilicity, and that it accumulates concentratively in cells due to partitioning into membrane lipids and binding to intracellular components.
journal_name
Biochem Pharmacoljournal_title
Biochemical pharmacologyauthors
Plagemann PG,Wohlhueter RMdoi
10.1016/0006-2952(84)90350-2subject
Has Abstractpub_date
1984-06-01 00:00:00pages
1783-8issue
11eissn
0006-2952issn
1873-2968pii
0006-2952(84)90350-2journal_volume
33pub_type
杂志文章abstract：:The metabolism of (1R)[1-3H]ethanol, [2-3H]lactate or [2-3H]xylitol was studied in hepatocytes from fed or T3-treated rats in the presence or absence of fructose or xylitol. The yields of tritium in ethanol, lactate, water, glycerol and glucose were determined. A simple model, describing the metabolic fate of tritium ...
journal_title：Biochemical pharmacology
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doi：10.1016/0006-2952(85)90260-6
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doi：10.1016/s0006-2952(02)01615-5
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doi：10.1016/j.bcp.2018.04.002
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journal_title：Biochemical pharmacology
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journal_title：Biochemical pharmacology
pub_type： 杂志文章
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pub_type： 杂志文章,评审
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doi：10.1016/0006-2952(87)90464-3
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pub_type： 杂志文章
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pub_type： 杂志文章
doi：10.1016/j.bcp.2006.10.002
更新日期：2007-01-15 00:00:00
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journal_title：Biochemical pharmacology
pub_type： 杂志文章
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pub_type： 杂志文章
doi：10.1016/0006-2952(96)84544-8
更新日期：1995-10-26 00:00:00
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更新日期：1987-07-15 00:00:00
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journal_title：Biochemical pharmacology
pub_type： 杂志文章
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更新日期：2005-02-15 00:00:00
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pub_type： 杂志文章
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更新日期：2000-06-01 00:00:00
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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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pub_type： 杂志文章
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更新日期：1994-05-18 00:00:00
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journal_title：Biochemical pharmacology
pub_type： 杂志文章
doi：10.1016/0006-2952(94)90544-4
更新日期：1994-04-29 00:00:00
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journal_title：Biochemical pharmacology
pub_type： 杂志文章
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更新日期：1991-02-01 00:00:00
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journal_title：Biochemical pharmacology
pub_type： 杂志文章
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更新日期：2009-09-01 00:00:00
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journal_title：Biochemical pharmacology
pub_type： 杂志文章
doi：10.1016/s0006-2952(98)00205-6
更新日期：1998-11-15 00:00:00
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journal_title：Biochemical pharmacology
pub_type： 杂志文章,评审
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更新日期：1999-01-15 00:00:00
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journal_title：Biochemical pharmacology
pub_type： 杂志文章
doi：10.1016/0006-2952(84)90179-5
更新日期：1984-04-15 00:00:00
abstract：:Dichlorodi[U-14C]phenyltrichloroethane ( [14C]DDT), incubated with rat hepatic microsomes and NADPH, produced reactive intermediates which covalently bound to microsomal protein and lipids. In atmospheric oxygen, DDT bound to microsomal protein; however, binding was increased up to approximately 70% by oxygen depletio...
journal_title：Biochemical pharmacology
pub_type： 杂志文章
doi：10.1016/0006-2952(84)90483-0
更新日期：1984-01-15 00:00:00
