A 85380 dihydrochloride
High affinity and selective α4β2 nACh receptor agonist (Ki values are 0.05, 148 and 314 nM for α4β2, α7 and α1β1δγ receptors respectively). Stimulates cation efflux in K177 cells expressing α4β2.
|Storage||Desiccate at RT|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 237.13. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||4.22 mL||21.09 mL||42.17 mL|
|5 mM||0.84 mL||4.22 mL||8.43 mL|
|10 mM||0.42 mL||2.11 mL||4.22 mL|
|50 mM||0.08 mL||0.42 mL||0.84 mL|
References are publications that support the biological activity of the product.
Abreo et al (1996) Novel 3-Pyridyl ethers with subnanomolar affinity for central neuronal nicotinic acetylcholine receptors. J.Med.Chem. 39 817 PMID: 8632405
Sullivan et al (1996) A-85380 [3-(2(S)-azetidinylmethoxy) pyridine]: in vitro pharmacological properties of a novel, high affinity α4β2 nicotinic acetylcholine receptor ligand. Neuropharmacology 35 725 PMID: 8887981
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Literature in this Area
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Alzheimer's disease (AD) is a degenerative brain disease and the most common cause of dementia, affecting approximately 47 million people worldwide. Updated in 2015, this poster summarizes the structural and functional changes observed in the progression of this neurodegenerative disease, as well as classic AD drug targets.
Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described.