848591-89-9
Chemical Structure
A-582941
- CAS No.: 848591-89-9
- Formula:C17H20N4
- Molecular Weight:280.38
IUPAC Name: 2-methyl-5-(6-phenylpyridazin-3-yl)octahydropyrrolo[3,4-c]pyrrole
InChIKey: GTMRUYCIJSNXGB-UHFFFAOYSA-N
SMILES: N=1N=C(C=CC1C=2C=CC=CC2)N3CC4CN(C)CC4C3
Biological Activity: A-582941 is a selective, orally active, blood-brain barrier-permeable α7 nAChR agonist, with Ki values of 10.8 nM and 17 nM in rat brain and human frontal cortex, respectively. A-582941 exhibits agonistic activity at 5-HT3 receptors, with a Ki of 150 nM. A-582941 triggers phosphorylation of ERK1/2 and CREB, inhibits GSK-3β via Ser-9 phosphorylation, increases acetylcholine release, induces the expression of Arc and c-Fos, activates brain regions associated with working memory and attention, and reduces cell death caused by nerve growth factor (NGF) deprivation. A-582941 is applicable for the research of Alzheimer's disease and schizophrenia[1][2][3].
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A-582941 | A-582941 is a selective, orally active, blood-brain barrier-permeable α7 nAChR agonist, with Ki values of 10.8 nM and 17 nM in rat brain and human frontal cortex, respectively. A-582941 exhibits agonistic activity at 5-HT3 receptors, with a Ki of 150 nM. A-582941 triggers phosphorylation of ERK1/2 and CREB, inhibits GSK-3β via Ser-9 phosphorylation, increases acetylcholine release, induces the expression of Arc and c-Fos, activates brain regions associated with working memory and attention, and reduces cell death caused by nerve growth factor (NGF) deprivation. A-582941 is applicable for the research of Alzheimer's disease and schizophrenia. | |||||||||||||||||||||
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References
- [1]. Tietje KR, et al. Preclinical characterization of A-582941: a novel alpha7 neuronal nicotinic receptor agonist with broad spectrum cognition-enhancing properties. CNS Neurosci Ther. 2008;14(1):65-82. [Content Brief]
- [2]. Thomsen MS, et al. The selective alpha7 nicotinic acetylcholine receptor agonist A-582941 activates immediate early genes in limbic regions of the forebrain: Differential effects in the juvenile and adult rat. Neuroscience. 2008;154(2):741-753. [Content Brief]
- [3]. Buccafusco JJ, et al. Profile of nicotinic acetylcholine receptor agonists ABT-594 and A-582941, with differential subtype selectivity, on delayed matching accuracy by young monkeys. Biochem Pharmacol. 2007;74(8):1202-1211. [Content Brief]
