522-054

522-054 Research Standard

522-054, chemically identified as 3-(2,5-difluorophenyl)-6-(1-ethyl-1H-indol-5-yl)-1,2,4-triazolo[4,3-b]pyridazine, is a triazolopyridazine-class research compound described in the scientific literature as a dual allosteric modulator of two Cys-loop ligand-gated ion channels. It was designed to enhance α7 neuronal nicotinic acetylcholine receptors (α7 nAChRs) and inhibit α5 subunit-containing GABA_A receptors (α5 GABA_ARs) within a single molecule. In controlled laboratory environments, 522-054 allows researchers to observe how simultaneous modulation of two related receptor families shapes hippocampal network activity, synaptic plasticity, and measures of cognition in cellular and animal models.

Physical & Handling Properties

Mechanism of Action & Research Context

522-054 is investigated for its capacity to act on two related ligand-gated ion channels at once, rather than as a direct agonist at either.

• Dual Allosteric Design: Published characterization describes the molecule as designed to simultaneously inhibit α5 GABA_A receptors and enhance α7 nAChRs. Both receptors belong to the Cys-loop family and both regulate hippocampal circuits that support declarative memory, which makes a single dual-acting ligand a useful tool for testing whether the two mechanisms combine.

• Hippocampal Synaptic Plasticity: In rat hippocampal slices, the compound reproduces the long-term potentiation of mossy fiber stimulation-induced excitatory postsynaptic currents in CA1 pyramidal neurons that is otherwise produced by applying two separate modulators together. Selective antagonists at either receptor block the sustained potentiation, which is the experiment that ties the effect to both targets rather than to one.

• Behavioral Correlates: Reported in vivo work describes enhanced performance in the radial arm maze and facilitation of attentional states in the five-choice serial reaction time task, with the same antagonist sensitivity observed in the slice experiments.

• Injury Models: A separate published study applied the compound during the chronic recovery period following experimental traumatic brain injury in rats, reporting reduced deficits in basal synaptic transmission and recovery of injury-impaired long-term potentiation in hippocampal slices, alongside improvements in fear memory and water maze measures without a measurable effect on cortical or hippocampal atrophy.

Research Applications

522-054 is a specialized reagent for ligand-gated ion channel and hippocampal circuit research.

Primary fields of in vitro laboratory investigation include:

• Cys-Loop Receptor Pharmacology: Characterizing positive and negative allosteric modulation at α7 nAChRs and α5 GABA_ARs in recombinant expression systems.

• Electrophysiology and Plasticity Assays: Measuring excitatory postsynaptic currents and long-term potentiation at hippocampal synapses under single-target and dual-target modulation.

• Antagonist-Block Study Design: Using selective α7 nAChR and α5 GABA_AR antagonists to separate the contribution of each target to an observed network effect.

• Structure–Activity Relationship (SAR) Studies: Comparing substituted 1,2,4-triazolo[4,3-b]pyridazine analogs to map how aryl and indolyl substitution shape activity at each receptor.

• Analytical Reference Work: Serving as a reference material for chromatographic and mass-spectrometric identification and method development.

Storage & Handling Guidelines

Store at controlled room temperature. Keep tightly closed. Liquid formats: do not refrigerate or freeze. Cold storage may cause the solution to cloud or precipitate. If this occurs, return to room temperature and mix until clear.

Storage guidance is a house recommendation. Analytical documentation is per-lot release testing.

Related Research Compounds

• TAK-653
• Nefiracetam
• DIHEXA
• NSI-189 Phosphate

Research Use Disclaimer

Research Use Only Disclaimer: This product is labeled and sold "For Research Use Only — NOT FOR HUMAN CONSUMPTION." It is not a drug, dietary supplement, food, cosmetic, or medical device, and it is not approved by the FDA or any other regulator for human or veterinary use. It is supplied to approved account holders as a research chemical for laboratory use and must be handled in accordance with applicable law.