202929-85-9

Upstream product

• 202931-56-4 6-chloro-3-phenyl-7,8,9,10-tetrahydro-(7,10-ethano)-1,2,4-triazolo[3,4-a]phthalazine 
• 202931-77-9 [3-(cyclopropylmethoxy)pyridin-2-yl]methanol 
• 202823-65-2 2,3,5,6,7,8-hexahydro-5,8-ethanophthalazine-1,4-dione 
• 202823-67-4 3,6-dichloro-4,5-diazatricyclo[6.2.2.2,7]dodeca-2⁽⁷⁾,3,5-triene 
• 613-94-5 benzoic acid hydrazide 
• 14173-30-9 3-hydroxy-2-hydroxymethylpyridine hydrochloride 

Relevant academic research and scientific papers

Discovery of functionally selective 7,8,9,10-tetrahydro-7,10-ethano-1,2,4- triazolo[3,4-a]phthalazines as GABAA receptor agonists at the α3 subunit

We have previously identified the 7,8,9,10-tetrahydro-7,10-ethano-1,2,4- triazolo[3,4-a]phthalazine (1) as a potent partial agonist for the 0.3 receptor subtype with 5-fold selectivity in binding affinity over α1. This paper describes a detailed investigation of the substituents on this core structure at both the 3- and 6-positions. Despite evaluating a wide range of groups, the maximum selectivity that could be achieved in terms of affinity for the α3 subtype over the α1 subtype was 12-fold (for 57). Although most analogues showed no selectivity in terms of efficacy, some did show partial agonism at α1 and antagonism at α3 (e.g., 25 and 75). However, two analogues tested (93 and 96), both with triazole substituents in the 6-position, showed significantly higher efficacy for the α3 subtype over the α1 subtype. This was the first indication that selectivity in efficacy in the required direction could be achieved in this series.

Substituted triazolo-pyridazine derivatives as ligands for GABA receptors

Substituted triazolo-pyridazine derivative compounds represented by wherein the variables are disclosed herein are selective ligands for GABA-A receptors, particularly for the α2 and/or α3 subunits.

Antispastic use of triazolo-pyridazine derivatives

A class of substituted 7,8-ring fused 1,2,4-triazolo[4,3-b]pyridazine derivatives, as shown in Formula I possessing an optionally substituted cycloalkyl, phenyl or heteroaryl substituent at the 3-position and a substituted alkoxy moiety at the 6-position, are selective ligands for GABAA receptors, in particular having high affinity for the α2 and/or α3 subunit thereof, and are accordingly of benefit in the treatment and/or prevention of muscle spasm or spasticity, e.g. in paraplegic patients. STR1