Benzodiazepine receptor ligands. Synthesis and in vitro binding activity of some 6-substituted-3-aryl-1,2,4-triazolo[3,4-a]phthalazines.
作者信息
Tarzia G, Occelli E, Barone D
出版信息
Farmaco. 1989 Jan;44(1):3-16. doi: 10.1002/chin.198938247.
PMID:2545221
Abstract
Some 3-aryl-6-hydroxymethyl-1,2,4-triazolo[3,4-a]phthalazines (VI a,b) and 3-aryl-6-(2-hydroxyethyl)-1,2,4-triazolo[3,4-a]phthalazines (XVIII) have been synthesized. From (VI b) some 3-aryl-6-(alkylamino)methyl- and 3-aryl-6-(alkoxy)methyl-1,2,4-triazolo[3,4-a]phthalazines have been prepared and evaluated in vitro for their ability to inhibit selective 3H-diazepam (3H-DZ) binding to benzodiazepine-receptors (BZRs) from homogenates of synaptosomes from rat brains. Several compounds have been shown to displace 3H-DZ from BZRs with Ki (nM) values ranging from 2.2 to 88, comparable to those of the reference drugs including Diazepam.
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