Highly potent alpha2/alph3 GABA-A receptor partial agonist for benzodiazepine binding site with anxiolytic activity but lacking sedative activity
TPA023 is a highly potent, functionally selective agonist for α2-, α3-, and α5GABAA receptors that shows zero efficacy at a1GABAA subtypes. TPA023 exhibits anxiolytic and anticonvulsant effects in both animals and humans but lacks sedative effects and abuse potential.
Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology, 38(6), 1006-1014 (2013-01-11)
Benzodiazepines are prescribed widely but their utility is limited by unwanted side effects, including abuse potential. The mechanisms underlying the abuse-related effects of benzodiazepines are not well understood, although α1 subunit-containing GABAA receptors have been proposed to have a critical
The Journal of pharmacology and experimental therapeutics, 332(1), 17-25 (2009-09-26)
The GABA(A) receptor alpha2/alpha3 subtype-selective compound 7-(1,1-dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3-ylmethoxy)-3-(2-fluorophenyl)-1,2,4-triazolo[4,3-b]pyridazine (TPA023; also known as MK-0777) is a triazolopyridazine that has similar, subnanomolar affinity for the benzodiazepine binding site of alpha1-, alpha2-, alpha3-, and alpha5-containing GABA(A) receptors and has partial agonist efficacy at the
The Journal of pharmacology and experimental therapeutics, 366(1), 145-157 (2018-05-04)
In nonhuman primates we tested a new set of behavioral categories for observable sedative effects using pediatric anesthesiology classifications as a basis. Using quantitative behavioral observation techniques in rhesus monkeys, we examined the effects of alprazolam and diazepam (nonselective benzodiazepines)
Questions
Reviews
★★★★★ No rating value
Active Filters
Our team of scientists has experience in all areas of research including Life Science, Material Science, Chemical Synthesis, Chromatography, Analytical and many others.
