Synthesis and structure-activity relationships of 1-aminophthalazinium bromides as GABAA receptor ligands

The synthesis and the GABA A binding activity of a series of 1-amino-2-alkylphthalazinium bromides (series A) and 1-amino-3-alkylphthalazinium bromides (series B) bearing different substituents at position-4 are reported. Some compounds of series A, bearing a lipophilic substituent at position-4, showed a good binding activity as well as in vivo convulsant activity