Symptomatic and neuroprotective properties of the aliphatic propargylamines

被引：18

作者：

Boulton, AA ^{[1
]}

机构：

[1] Univ Saskatchewan, Neuropsychiat Res Unit, Saskatoon, SK S7N 5E4, Canada

来源：

MECHANISMS OF AGEING AND DEVELOPMENT | 1999年 / 111卷 / 2-3期

关键词：

aliphatic propargylamines; R-2 heptyl-N-methylpropargylamine (R-2HMP); MAO-B; neurodegenerative disorders; apoptosis; antiapoptotre drugs;

D O I：

10.1016/S0047-6374(99)00073-1

中图分类号：

Q2 [细胞生物学];

学科分类号：

071009 ; 090102 ;

摘要：

This short review describes the development of several families of aliphatic propargylamine drugs. The parent family - the aliphatic N-methylpropargylamines are potent, specific, irreversible MBO-B inhibitors, like R-deprenyl; but devoid of R-deprenyl's toxicity and amphetaminergic effects. In addition the parent drugs are potent antiapoptoic agents. Their desmethyl and further oxidized metabolites whilst devoid of MAO-B inhibitory properties of R-2HMP (our chosen drug candidate) are described along with the suggestion that this drug be developed for the treatment of several human neurodegenerative conditions. (C) 1999 Elsevier Science Ireland Ltd. All rights reserved.

引用

页码：201 / 209

页数：9

共 39 条

[1]

Berry M. D., 1999, CNS Drug Reviews, V5, P105

[2]

BERRY MD, 1998, ACNP M PUERT RIC DEC, V105, P145

[3]

Boulton A A, 1998, Adv Pharmacol, V42, P273

[4]

Boulton A A, 1998, Adv Pharmacol, V42, P308

[5]

Boulton AA, 1997, DRUG DEVELOP RES, V42, P150, DOI 10.1002/(SICI)1098-2299(199711/12)42:3/4<150::AID-DDR6>3.0.CO

[6]

2-P

[7]

BOULTON AA, 1998, CAN J CONT MED ED, V11, P195

[8] Huntington and DRPLA proteins selectively interact with the enzyme GAPDH [J].

Burke, JR ;

Enghild, JJ ;

Martin, ME ;

Jou, YS ;

Myers, RM ;

Roses, AD ;

Vance, JM ;

Strittmatter, WJ .

NATURE MEDICINE, 1996, 2 (03) :347-350

[9] ETIOLOGY OF PARKINSONS-DISEASE [J].

CALNE, DB ;

LANGSTON, JW .

LANCET, 1983, 2 (8365) :1457-1459

[10]

CARVEY PM, 1998, TREATMENT MOVEMENT D

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