Synthesis and structure-activity relationships of 1-aminophthalazinium bromides as GABAA receptor ligands. 1993

D Catarzi, and L Cecchi, and G Filacchioni, and A Bartolini, and R Carpenedo, and A Galli, and F Mori
Dipartimento di Scienze Farmaceutiche, Università di Firenze, Italy.

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.

UI MeSH Term Description Entries
D008024 Ligands A molecule that binds to another molecule, used especially to refer to a small molecule that binds specifically to a larger molecule, e.g., an antigen binding to an antibody, a hormone or neurotransmitter binding to a receptor, or a substrate or allosteric effector binding to an enzyme. Ligands are also molecules that donate or accept a pair of electrons to form a coordinate covalent bond with the central metal atom of a coordination complex. (From Dorland, 27th ed) Ligand
D010793 Phthalazines Bicyclic heterocyclic compounds containing a BENZENE ring fused to PYRIDAZINE.
D011724 Pyridazines Six-membered rings with two adjacent nitrogen atoms also called 1,2-diazine.
D001965 Bromides Salts of hydrobromic acid, HBr, with the bromine atom in the 1- oxidation state. (From McGraw-Hill Dictionary of Scientific and Technical Terms, 4th ed) Bromide
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D013329 Structure-Activity Relationship The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups. Relationship, Structure-Activity,Relationships, Structure-Activity,Structure Activity Relationship,Structure-Activity Relationships
D051379 Mice The common name for the genus Mus. Mice, House,Mus,Mus musculus,Mice, Laboratory,Mouse,Mouse, House,Mouse, Laboratory,Mouse, Swiss,Mus domesticus,Mus musculus domesticus,Swiss Mice,House Mice,House Mouse,Laboratory Mice,Laboratory Mouse,Mice, Swiss,Swiss Mouse,domesticus, Mus musculus
D018079 Receptors, GABA Cell-surface proteins that bind GAMMA-AMINOBUTYRIC ACID with high affinity and trigger changes that influence the behavior of cells. GABA-A receptors control chloride channels formed by the receptor complex itself. They are blocked by bicuculline and usually have modulatory sites sensitive to benzodiazepines and barbiturates. GABA-B receptors act through G-proteins on several effector systems, are insensitive to bicuculline, and have a high affinity for L-baclofen. GABA Receptors,Receptors, gamma-Aminobutyric Acid,gamma-Aminobutyric Acid Receptors,GABA Receptor,gamma-Aminobutyric Acid Receptor,Receptor, GABA,Receptor, gamma-Aminobutyric Acid,Receptors, gamma Aminobutyric Acid,gamma Aminobutyric Acid Receptor,gamma Aminobutyric Acid Receptors

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