Electric Literature of 19064-67-6, Chemistry is the experimental science by definition. We want to make observations to prove hypothesis. For this purpose, we perform experiments in the lab. 19064-67-6, Name is 6-Chloro-3-hydroxypyridazine,introducing its new discovery.
Synthesis and Structure-Activity Relationships of Series of Aminopyridazine Derivatives of gamma-Aminobutyric Acid Acting as Selective GABA-A Antagonists
We have recently shown that an aryloaminopyridazine derivarive of GABA, SR 95103 <2-(3-carboxypropyl)-3-amino-4-methyl-6-phenylpyridazinium chloride>, is a selective and competitive GABA-A receptor antagonist.In order to further explore the structural requirements for GABA receptor affinity, we synthesized a series of 38 compounds by attaching various pyridazinic structures to GABA or GABA-like side chains.Most of the compounds displaced <3H>GABA from rat brain membranes.All the active compounds antagonized the GABA-elicited enhancement of <3H>diazepam binding, strongly suggesting that all these compounds are GABA-A receptor antagonists.None of the compounds that displaced <3H>GABA from rat brain membranes interacted with other GABA recognition sites (GABA-B receptor, GABA uptake binding site, glutamate decarboxylase, GABA-transaminase).They did not interact with the Cl- ionophore associated with the GABA-A receptor and did not interact with the benzodiazepine, strychnine, and glutamate binding sites.Thus these compounds appear to be specific GABA-A receptor antagonists.In terms of structure-activity, it can be concluded that a GABA moiety bearing a positive charge is necessary for optimal GABA-A receptor recognition.Additional binding sites are tolerated only if they are part of a charge-delocalized amidinic or guanidinic system.If this delocalization is achieved by linking a butyric acid moiety to the N(2) nitrogen of a 3-aminopyridazine, GABA-antagonistic character is produced.The highest potency (ca.250 times bicuculline) was observed when an aromatic ? system, bearing electron-donating substituents, was present on the 6-position of the pyridazine ring.
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Reference：
Pyridazine – Wikipedia,
Pyridazine | C4H4N771 – PubChem