SYNTHESIS AND BINDING-PROPERTIES TO GABA RECEPTORS OF 3-HYDROXYPYRIDINYL-ANALOGS AND 3-HYDROXYPIPERIDINYL-ANALOGS OF BACLOFEN

被引：9

作者：

DESIDERI, N ^{[1
]}

GALLI, A ^{[1
]}

SESTILI, I ^{[1
]}

STEIN, ML ^{[1
]}

机构：

[1] UNIV FLORENCE,DIPARTIMENTO FARMACOL PRECLIN & CLIN MARIO AIAZZI MANCINI,I-50134 FLORENCE,ITALY

来源：

ARCHIV DER PHARMAZIE | 1992年 / 325卷 / 01期

关键词：

D O I：

10.1002/ardp.19923250108

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The synthesis of 3-(3-hydroxy-2-pyridinyl)propanoic acid, 3-(3-hydroxy-2-pyridinyl)-4-aminobutanoic acid, their corresponding piperidine compounds, and of some cyclized derivatives is described. In in vitro assays none of the new compounds shows any noteworthy affinity for GABA(A) or GABA(B) receptors; only (R,S)-3-(3-hydroxy-2-pyndinyl)-4-aminobutanoic acid and its lactam inhibited in some degree [H-3]GABA binding, at 10(-4) M concentration, with low specificity as regards the two receptors.

引用

页码：29 / 33

页数：5

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