848591-90-2
Chemical Structure
A-582941 dihydrochloride
- CAS No.: 848591-90-2
- Formula:C17H22Cl2N4
- Molecular Weight:353.29
IUPAC Name: 2-methyl-5-(6-phenylpyridazin-3-yl)octahydropyrrolo[3,4-c]pyrrole dihydrochloride
InChIKey: PGTCSMQEIJMZTJ-UHFFFAOYSA-N
SMILES: CN1CC(CN(C2=NN=C(C3=CC=CC=C3)C=C2)C4)C4C1.[H]Cl.[H]Cl
Biological Activity: A-582941 dihydrochloride 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 dihydrochloride exhibits agonistic activity at 5-HT3 receptors, with a Ki of 150 nM. A-582941 dihydrochloride 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 dihydrochloride is applicable for the research of Alzheimer's disease and schizophrenia[1][2][3].
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A-582941 dihydrochloride | 99.78% | A-582941 dihydrochloride 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 dihydrochloride exhibits agonistic activity at 5-HT3 receptors, with a Ki of 150 nM. A-582941 dihydrochloride 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 dihydrochloride is applicable for the research of Alzheimer's disease and schizophrenia. | ||||||||||||||||||||
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- [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]
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