Benzoylalanine analogues as inhibitors of rat brain kynureninase and kynurenine 3-hydroxylase.
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Alanine↗
Biomedical subjects
M Varasi
Publications and source records attributed to M Varasi.
Enantiospecific synthesis and in vitro activity of selective inhibitors of rat brain kynureninase and kynurenine-3-hydroxylase.
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Alanine↗
28833, a selective kynurenine 3-hydroxylase inhibitor. Effects on the kynurenine pathway metabolites in the gerbil.
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Animals↗
New 2-substituted 2,3,3a,4-tetrahydro-1H-imidazo[5,1-c] [1,4]benzoxazin-1-ones as alpha 2-adrenoceptor antagonists.
The synthesis of new 2-imidazol(in)yl-alkyl derivatives of 2,3,3a,4-tetrahydro-1H-imidazo[5,1-c][1,4]benzoxazin-1-one is reported. Some compounds of the series have shown high affinity for alpha 2 receptors, high alpha 2/alpha 1 selectivity and alpha 2 antagonism in vitro (vas deferens). Owing to their selective alpha 2-antagonism associated to a novel structure, compounds 8 and 20 have been selected for further biological investigation as potential antidepressants.
Adrenergic alpha-Antagonists↗
Synthesis and anticonvulsant activity of some benzopyranone imino derivatives of GABA and related compounds.
The synthesis of some 5-hydroxy-4-imino-2,3-dihydrobenzopyran derivatives of GABA and alkylamines is described. The products were tested for their GABA-receptor binding and anticonvulsant activity in mice. Some compounds showed anticonvulsant activity. No binding to GABA receptors was observed.
3-Mercaptopropionic Acid↗
Heterocyclic GABA analogues. Displacement of radiolabelled 3H-GABA from rat brain membrane preparations.
2,5-Dimethyl-1H-pyrrol-1-yl-butanoic acid (I) and 2,5-diethyl-1H-pyrrol-1-yl-butanoic acid (V) were synthesised as non basic analogues of 4-aminobutanoic acid (GABA) to investigate the influence of the pKa of the 4-nitrogen on the in vitro binding to GABA receptors. (I) displaced 3H-GABA from specific binding sites of synaptosomal membrane preparations from rat cerebellum with an IC50 of 0.5 microM and (V) with an IC50 of 0.4 microM. (I) was inactive in vivo in the bicuculline anticonvulsant test (mice i.p.). The authors conclude that a basic nitrogen is not necessary for the binding to the GABAergic receptors although the ensuing complex is likely to be pharmacologically ineffective.
Animals↗