Positive allosteric modulator for the α7 nicotinic acetylcholine receptor
Biological descriptionCompetitive, type II positive allosteric modulator for α7nAChR (EC50 = 216 nM). Increases potency of nicotinic agonists. No effect on α4β2, α3β4 and α9α10 nAChRs. Active in vivo.
Storage instructionsStore at +4°C. Store under desiccating conditions. The product can be stored for up to 12 months.
Solubility overviewSoluble in DMSO to 100 mM
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.
Collins T et al. Competitive binding at a nicotinic receptor transmembrane site of two a7-selective positive allosteric modulators with differing effects on agonist-evoked desensitization. Neuropharmacology61:1306-13 (2011).
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Livingstone PD et al. alpha7 and non-alpha7 nicotinic acetylcholine receptors modulate dopamine release in vitro and in vivo in the rat prefrontal cortex. Eur J Neurosci29:539-50 (2009).
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Hurst RS et al. A novel positive allosteric modulator of the alpha7 neuronal nicotinic acetylcholine receptor: in vitro and in vivo characterization. J Neurosci25:4396-405 (2005).
Read more (PubMed: 15858066) »