848591-90-2 Usage
Uses
Used in Pharmaceutical Research:
A 582941 is used as a research compound for studying the mechanisms underlying neurodegeneration in Alzheimer's disease. Its ability to activate glycogen synthase kinase-3β and α7 nicotinic receptors in Aβ1-42-induced tau phosphorylation in PC12 cells makes it a promising candidate for investigating potential therapeutic targets and strategies for treating Alzheimer's disease.
Used in Drug Discovery:
A 582941 is used as a lead compound in the development of new drugs targeting neurodegenerative diseases, particularly Alzheimer's disease. Its unique properties in activating key receptors and enzymes involved in the disease's progression make it a valuable starting point for designing novel therapeutic agents.
Used in Neurodegenerative Disease Research:
A 582941 is used as a research tool in the study of neurodegenerative diseases, with a specific focus on Alzheimer's disease. Its role in modulating tau phosphorylation and activating relevant receptors and enzymes provides insights into the molecular pathways that contribute to the disease's progression, aiding in the identification of potential therapeutic targets and interventions.
Biological Activity
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 [1].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 [1].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 [1].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 [1].
references
[1]. 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.
Check Digit Verification of cas no
The CAS Registry Mumber 848591-90-2 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 8,4,8,5,9 and 1 respectively; the second part has 2 digits, 9 and 0 respectively.
Calculate Digit Verification of CAS Registry Number 848591-90:
(8*8)+(7*4)+(6*8)+(5*5)+(4*9)+(3*1)+(2*9)+(1*0)=222
222 % 10 = 2
So 848591-90-2 is a valid CAS Registry Number.
848591-90-2Relevant articles and documents
Substituted diazabicycloalkane derivatives
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Page/Page column 40, (2010/02/11)
Compounds of formula (I) [in-line-formulae]Z-Ar1—Ar2??(I) [/in-line-formulae] wherein Z is a diazabicyclic amine, Ar1 is a 5- or 6-membered aromatic ring, and Ar2 is selected from the group consisting of an unsubstituted or substituted 5- or 6-membered heteroaryl ring; unsubstituted or substituted bicyclic heteroaryl ring; 3,4-(methylenedioxy)phenyl; carbazolyl; tetrahydrocarbazolyl; naphthyl; and phenyl; wherein the phenyl is substituted with 0, 1, 2, or 3 substituents in the meta- or para-positions. The compounds are useful in treating conditions or disorders prevented by or ameliorated by α7 nAChR ligands. Also disclosed are pharmaceutical compositions comprising compounds of formula (I) and methods for using such compounds and compositions.
Substituted diazabicycloakane derivatives
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Page/Page column 23, (2010/02/11)
Compounds of formula (I) Z-Ar1—Ar2??(I) wherein Z is a diazabicyclic amine, Ar1 is a 5- or 6-membered aromatic ring, and Ar2 is selected from an unsubstituted or substituted 5-membered heteroaryl ring; an unsubstituted or substituted 6-membered heteroaryl ring; 3,4-(methylenedioxy)phenyl; and phenyl substituted with 0, 1, 2, or 3 substituents in the meta- or para-positions. The compounds are useful in treating conditions or disorders prevented by or ameliorated by α7 nAChR ligands. Also disclosed are pharmaceutical compositions comprising compounds of formula (I) and methods for using such compounds and compositions.
