N-(3R)-1-AZABICYCLO[2.2.2]OCT-3-YL-4-CHLOROBENZAMIDE Struktur

N-(3R)-1-AZABICYCLO[2.2.2]OCT-3-YL-4-CHLOROBENZAMIDE

Bezeichnung:N-(3R)-1-AZABICYCLO[2.2.2]OCT-3-YL-4-CHLOROBENZAMIDE

CAS-Nr123464-89-1

Englisch Name:N-(3R)-1-AZABICYCLO[2.2.2]OCT-3-YL-4-CHLOROBENZAMIDE

CBNumberCB6847535

SummenformelC14H17ClN2O

Molgewicht264.75058

MOL-Datei123464-89-1.mol

N-(3R)-1-AZABICYCLO[2.2.2]OCT-3-YL-4-CHLOROBENZAMIDE physikalisch-chemischer Eigenschaften

Schmelzpunkt	240-242℃
storage temp.	Inert atmosphere,2-8°C
Löslichkeit	Soluble in DMSO (up to 25 mg/ml)
Aggregatzustand	Off-white solid
Farbe	White
Stabilität	Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months.

Gefahreninformationscode (GHS)

N-(3R)-1-AZABICYCLO[2.2.2]OCT-3-YL-4-CHLOROBENZAMIDE Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
PNU 282987 (CAS 123464-89-1) is a selective α7 nicotinic acetylcholine receptor (nAChR) agonist (Ki?= 26 nM).1? The?a7 nAChR is a potential therapeutic target of cognitive deficits in diseases such as Alzheimer’s, Parkinson’s, schizophrenia, and attention deficit disorders – agonism of this receptor with PNU 282987 has shown potential to ameliorate these deficits.2-5
Verwenden
PNU 282987 is used as an activator of α-7 nicotinic acetylcholine receptor.
Allgemeine Beschreibung
A potent agonist highly selective for α7 nAChRs (K_i = 26 nM). Used in investigating the roles of α7 nAChRs in sensory gating, learning and memory, cognitive functions, and treatment of Schizophrenia.
Biologische Aktivität
Highly selective α 7 nAChR agonist (K i = 26 nM) displaying negligible blockade of α 1 β 1 γ δ and α 3 β 4 nAChRs (IC 50 ≥ 60 μ M). Found to be inactive against a panel of 32 receptors at 1 μ M, except 5-HT 3 receptors (K i = 930 nM).
Biochem/physiol Actions
Primary Targetα7 nAChRs
Einzelnachweise
1) Bodnar?et al.?(2005),?Discovery and structure-activity relationship of quinuclidine benzamides as agonists of α7 nicotinic acetylcholine receptors; J. Med. Chem.?48?905 2) Stuckenholz?et al.?(2013),?The α7 nAChR agonist PNU-282987 reduces inflammation and MPTP-induced nigral dopaminergic cell loss in mice; J. Parkinsons Dis.?3?161 3) Vicens?et al. (2013),?Motor and anxiety effects of PNU-282987, an alpha7 nicotinic receptor agonist, and stress in an animal model of Alzheimer’s disease; Curr. Alzheimer Res.?10?516 4) Navarro?et al.?(2015),?Alpha7 nicotinic receptor activation protects against oxidative stress via heme-oxygenase I induction; Biochem. Pharmacol.?97?473 5) McLean?et al.?(2016),?Nicotinic α7 and α4β2 agonists enhance the formation and retrieval of recognition memory: Potential mechanisms for cognitive performance enhancement in neurological and psychiatric disorders; Behav. Brain Res.?302?73

N-(3R)-1-AZABICYCLO[2.2.2]OCT-3-YL-4-CHLOROBENZAMIDE Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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