Abstract:
:Bernserazide (D,L-serine 2-[2,3,4-trihydroxybenzyl]-hydrazide) as been shown to inhibit the clorgyline-resistant amine oxidase (CRAO) activities which metabolize benzylamine in homogenates of rat aorta, heart and brown adipose tissue. In vitro studies showed a concentration- and time-dependent inhibition of CRAO in heart and aorta which was reversed by dialysis for 18hr. At high concentrations (10(-4)-10(-3)M) benserazide appeared to increase enzyme activity towards and occasionally above control value. These increases became more prominent after long periods of preincubation (especially in the presence of saturating benzylamine concentrations) and remained after dialysis of those homogenates preincubated with benserazide. The administration of benserazide for one or seven days in daily doses of 5-150 mg/kg also inhibited CRAO activity in vivo in a dose-dependent manner, with greater inhibition after seven days treatment. Reversal of inhibition, by dialysis of tissue homogenates from benserazide-treated rats, was much slower than was found with homogenates incubated in vitro with the drug. After benserazide administration to rats, MAO-A activity towards 5-hydroxytryptamine was generally not inhibited, and in fact was significantly increased in some cases. The administration of L-DOPA (250 mg/kg) together with benserazide (40 mg/kg) resulted in a similar degree of CRAO inhibition in aorta and heart to that seen after benserazide alone. These findings are discussed with regard to the use of these drugs in the therapy of Parkinson's Disease, although the paucity of information about the physiological function of CRAO makes the significance of its inhibition by benserazide unclear.
journal_name
Biochem Pharmacoljournal_title
Biochemical pharmacologyauthors
Lyles GA,Callingham BAdoi
10.1016/0006-2952(82)90037-5subject
Has Abstractpub_date
1982-04-01 00:00:00pages
1417-24issue
7eissn
0006-2952issn
1873-2968pii
0006-2952(82)90037-5journal_volume
31pub_type
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journal_title:Biochemical pharmacology
pub_type: 杂志文章
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更新日期:2004-01-01 00:00:00
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journal_title:Biochemical pharmacology
pub_type: 杂志文章
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journal_title:Biochemical pharmacology
pub_type: 杂志文章
doi:10.1016/0006-2952(85)90598-2
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journal_title:Biochemical pharmacology
pub_type: 杂志文章
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journal_title:Biochemical pharmacology
pub_type: 杂志文章
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pub_type: 杂志文章
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更新日期:1983-12-15 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:1983-07-01 00:00:00
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pub_type: 杂志文章
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更新日期:2015-09-01 00:00:00
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journal_title:Biochemical pharmacology
pub_type: 杂志文章
doi:10.1016/0006-2952(85)90614-8
更新日期:1985-04-01 00:00:00
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pub_type: 杂志文章
doi:10.1016/j.bcp.2015.11.026
更新日期:2016-02-01 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:1995-09-07 00:00:00
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journal_title:Biochemical pharmacology
pub_type: 杂志文章,评审
doi:10.1016/j.bcp.2005.09.019
更新日期:2005-12-19 00:00:00
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journal_title:Biochemical pharmacology
pub_type: 杂志文章
doi:10.1016/0006-2952(91)90557-l
更新日期:1991-05-15 00:00:00
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journal_title:Biochemical pharmacology
pub_type: 杂志文章
doi:10.1016/j.bcp.2006.07.007
更新日期:2006-10-16 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
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更新日期:2012-01-15 00:00:00
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journal_title:Biochemical pharmacology
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更新日期:2000-02-15 00:00:00
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journal_title:Biochemical pharmacology
pub_type: 杂志文章
doi:10.1016/0006-2952(94)90164-3
更新日期:1994-09-15 00:00:00
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journal_title:Biochemical pharmacology
pub_type: 杂志文章
doi:10.1016/0006-2952(87)90040-2
更新日期:1987-05-15 00:00:00
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journal_title:Biochemical pharmacology
pub_type: 杂志文章
doi:10.1016/0006-2952(94)90044-2
更新日期:1994-08-17 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:2003-06-15 00:00:00
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journal_title:Biochemical pharmacology
pub_type: 杂志文章
doi:10.1016/j.bcp.2008.09.008
更新日期:2008-12-15 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:1990-08-15 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:1986-05-01 00:00:00
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journal_title:Biochemical pharmacology
pub_type: 杂志文章
doi:10.1016/0006-2952(94)90329-8
更新日期:1994-04-20 00:00:00