partial agonist of α7 nicotinic acetylcholine receptors
Sample solution is provided at 25 µL, 10mM.
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|Cas No.||848591-90-2||SDF||Download SDF|
|Canonical SMILES||CN1C[[email protected]]2[[email protected]@H](CN(C3=NN=C(C4=CC=CC=C4)C=C3)C2)C1|
|Solubility||Soluble in DMSO > 10 mM||Storage||Desiccate at RT|
|Physical Appearance||White solid||Shipping Condition||Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request|
|General tips||For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.|
A 582941 is a highly selective partial agonist of α7 nicotinic acetylcholine receptors (nAChRs), with an EC50 value of 4260 nM to human α7 nAChRs .
nAChRs are a family of pentameric ligand-gated ion channels. They are derived from multiple α (α2-α10) and β (β2-β4) subunit genes. α7 nAChR receptor exhibits higher Ca2+ permeability than other nAChR combinations. These receptors modulate the release of multiple neurotransmitters, including acetylcholine (ACh), glutamate, and GABA .
In FLIPR, A 582941 did not activate recombinant heteromeric nAChRs (α4β2, α3β2, α3β4, or α4β4) according to Ca2+ dynamics results. In IMR-32 cells expressing native human α3β4 nAChRs, A 582941 did not produce an agonist effect (with an efficacy less than 20% at concentrations up to 100,000 nM). In Xenopus oocytes expressing an α9α10 nAChR construct, A 582941 at concentrations up to 100,000 nM did not evoke currents. With respect to nAChRs, A 582941 activated only the homomeric α7 subtype .
In a rat model of short-term memory based on olfactory cues, saline-treated adults used investigation times during the second session nearly equal to the first session, exhibiting little recognition of the juvenile. Treatment with A 582941 in adult rats resulted in a dose-related reduction in the exploration time during the second session compared with the first session, exhibiting improved recognition of the juvenile .
. Tietje KR, Anderson DJ, Bitner RS, et al. Preclinical Characterization of A-582941: A Novel α7 Neuronal Nicotinic Receptor Agonist with Broad Spectrum Cognition-Enhancing Properties. CNS neuroscience & therapeutics, 2008, 14(1): 65-82.