receptor inverse agonist selective for the α
= 3 nM). Exhibits affinity at benzodiazepine binding site of recombinant human GABAA
values are 0.77 nM, 0.83 nM, 0.85 nM and 1.4 nM for α
2-, and α
5-containing respectively). Increases long-term potentiation (LTP) in mouse hippocampal slices. Exhibits no anxiogenic or proconvulsant activity.
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Manufactured and sold under license from Merck & Co., Inc. for use solely for preclinical research purposes (ie: not for administration to or other use in humans)
An orally bioavailable, functionally selective inverse agonist at the benzodiazepine site of GABAA α5 receptors with cognition enhancing properties.
Chambers et al.
In vitro and in vivo properties of 3-tert-butyl-7-(5-methylisoxazol-3-yl)-2-(1-methyl-1H-1,2,4-triazol-5-ylmethoxy)-pyrazolo[1,5-d]-[1,2,4]triazine (MRK-016), a GABAA receptor α5 subtype-selective inverse agonist.
Atack et al.