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Development of novel 4-aminopyridine derivatives as potential treatments for neurological injury and disease.

Abstract：

:The amine position of the K+ channel blocker 4-aminopyridine was functionalized to form amide, carbamate and urea derivatives in an attempt to identify novel compounds which restore conduction in injured spinal cord. Eight derivatives were tested in vitro, using a double sucrose gap chamber, for the ability to restore conduction in isolated, injured guinea pig spinal cord. The methyl, ethyl and t-butyl carbamates of 4-aminopyridine induced an increase in the post injury compound action potential. The methyl and ethyl carbamates were further tested in an in vivo model of spinal cord injury. These results represent the first time that 4-aminopyridine has been derivatized without losing its ability to restore function in injured spinal cord tissue.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Smith DT,Shi R,Borgens RB,McBride JM,Jackson K,Byrn SR

doi

10.1016/j.ejmech.2005.04.017

subject

Has Abstract

pub_date

2005-09-01 00:00:00

pages

908-17

issue

9

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(05)00113-3

journal_volume

40

pub_type

杂志文章

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