Synthesis and structure-activity relationships of 1-aminophthalazinium bromides as GABAA receptor ligands.
The synthesis and the GABAA 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.
Catarzi
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Dipartimento di Scienze Farmaceutiche, Università di Firenze, Italy.
Cecchi
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L
Filacchioni
G
G
Bartolini
A
A
Carpenedo
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R
Galli
A
A
Mori
F
F
D000818:Animals; D001965:Bromides / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism; D008024:Ligands; D051379:Mice; D010793:Phthalazines / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism; D011724:Pyridazines; D018079:Receptors, GABA / Q000378:metabolism*; D013329:Structure-Activity Relationship
D001965:Bromides; D008024:Ligands; D010793:Phthalazines; D011724:Pyridazines; D018079:Receptors, GABA; C044796:2-(carboxy-3'-propyl)-3-amino-4-methyl-6-phenylpyridazinium chloride