Abstract：
:Milacemide (CP 1552 S, 2-n-pentylaminoacetamide), a drug with anti-epileptic potency, increases the gamma-aminobutyric acid (GABA) content specifically in the substantia nigra of rat brain. The effect is dose-related from 25 to 100 mg/kg p.o. The time course shows that at 100 mg/kg p.o. after 2, 3 and 4 hr the substantia nigra GABA content is significantly increased by 28, 33 and 38%, respectively. After 6 hr the GABA contents return to the control value. After repeated oral administration of milacemide a comparable effect to acute administration is obtained. After degeneration of the striato-nigral GABA-ergic pathway, milacemide no longer enhances the content of GABA in the substantia nigra. GABA-transaminase activity measured ex vivo in rat brain homogenate is not influenced by milacemide. On the other hand, the glutamate decarboxylase activity measured ex vivo 3 hr after 100 mg/kg of milacemide is significantly increased by 11% in homogenates of the whole rat brain. The results show that milacemide increases the GABA content in the GABA pool which is associated with the striato-nigral neurons. This increase is not due to GABA-transaminase inhibition but might be the result of an enhanced synthesis, possibly through glutamate decarboxylase activation.
journal_name
Biochem Pharmacoljournal_title
Biochemical pharmacologyauthors
de Varebeke PJ,Niebes P,Pauwels G,Roba J,Korf Jdoi
10.1016/0006-2952(83)90087-4subject
Has Abstractpub_date
1983-09-15 00:00:00pages
2751-5issue
18eissn
0006-2952issn
1873-2968pii
0006-2952(83)90087-4journal_volume
32pub_type
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pub_type： 杂志文章
doi：10.1016/0006-2952(85)90561-1
更新日期：1985-08-01 00:00:00
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更新日期：2010-01-15 00:00:00
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pub_type： 杂志文章,评审
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更新日期：2002-10-01 00:00:00
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pub_type： 杂志文章
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更新日期：2010-10-15 00:00:00
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pub_type： 杂志文章
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更新日期：1982-04-01 00:00:00
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pub_type： 传,历史文章,杂志文章,评审
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更新日期：2015-11-15 00:00:00
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更新日期：1995-06-16 00:00:00
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pub_type： 杂志文章
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更新日期：1982-02-15 00:00:00
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pub_type： 杂志文章
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更新日期：2012-05-01 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：2008-02-01 00:00:00
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pub_type： 杂志文章
doi：10.1016/j.bcp.2007.12.017
更新日期：2008-04-01 00:00:00
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journal_title：Biochemical pharmacology
pub_type： 杂志文章
doi：10.1016/0006-2952(87)90022-0
更新日期：1987-11-01 00:00:00
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journal_title：Biochemical pharmacology
pub_type： 杂志文章
doi：10.1016/0006-2952(89)90380-8
更新日期：1989-02-01 00:00:00
