CAS 123464-89-1|PNU 282987

Introduction：Basic information about CAS 123464-89-1|PNU 282987, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.

Table of Contents

1. Names
2. PNU 282987 BiologicalActivity
3. Chemical & Physical Properties
4. Synonyms

Common Name	PNU 282987
CAS Number	123464-89-1	Molecular Weight	301.21
Density	1.3±0.1 g/cm3	Boiling Point	431.5±30.0 °C at 760 mmHg
Molecular Formula	C₁₄H₁₈Cl₂N₂O	Melting Point	/
MSDS	USA	Flash Point	214.8±24.6 °C

Names

Name	N-(3R)-1-Azabicyclo[2.2.2]oct-3-yl-4-chlorobenzamide
Synonym	More Synonyms

PNU 282987 BiologicalActivity

Description	PNU-282987 is a selective α7 nicotinic acetylcholine receptor(α7 nAChR) agonist with Ki of 26 nM; no affinity for α1β1γδ and α3β4 nAChRs (IC50 ≥ 60 μM).IC50 value: 26 nM(Ki) [1]Target: α7 nAChR agonistin vitro: Treatment with PNU-282987 resulted in an attenuation of neuroinflammation in the MPTP-lesioned SN. Furthermore, PNU-282987 attenuated MPTP-induced dopaminergic cell loss in the SN and reduced striatal dopamine depletion [3].in vivo: Mice were subjected to 70% partial hepatic I/R for 60 min and pretreated with either vehicle or with PNU-282987, and blood and hepatic tissue samples were collected at 3, 6, and 12 h following reperfusion. pretreatment with PNU-282987 decreased serum transaminase levels and ameliorated liver injury after hepatic I/R. Moreover, pretreatment with PNU-282987 suppressed NF-κB activation, cytokine production (tumor necrosis factor α, interleukin 1β), and HMGB1 expression in liver after hepatic I/R [2]. Mice treated with 2.5 and 10 mg/kg of PNU devoted less time to rearing into open arms. In the HB task, MC mice displayed higher exploratory activity reflected in more head-dips (HD) during the first minute than EE and SE, whereas EE displayed low exploration levels reflected in total HD (5 min) [4].
Related Catalog	Signaling Pathways >>Membrane Transporter/Ion Channel >>nAChRSignaling Pathways >>Neuronal Signaling >>nAChRResearch Areas >>Neurological Disease
References	[1]. Bodnar AL, et al. Discovery and structure-activity relationship of quinuclidine benzamides as agonists of alpha7 nicotinic acetylcholine receptors. J Med Chem. 2005 Feb 24;48(4):905-8. [2]. Li F, et al. The protective effect of PNU-282987, a selective α7 nicotinic acetylcholine receptor agonist, on the hepatic ischemia-reperfusion injury is associated with the inhibition of high-mobility group box 1 protein expression and nuclear factor κB activation in mice. Shock. 2013 Feb;39(2):197-203. [3]. Stuckenholz V, et al. The α7 nAChR agonist PNU-282987 reduces inflammation and MPTP-induced nigral dopaminergic cell loss in mice. J Parkinsons Dis. 2013;3(2):161-72. [4]. Mesa-Gresa P, et al. Behavioral effects of different enriched environments in mice treated with the cholinergic agonist PNU-282987. Behav Processes. 2014 Mar;103:117-24. [5]. Dong Jun Yu, et al. Effect of ischemic preconditioning combined with α7 nAchR agonists on limb ischemia-reperfusion lung injury in rat. Biomed Res. 2017; Special Issue: ISSN 0970.

Description

PNU-282987 is a selective α7 nicotinic acetylcholine receptor(α7 nAChR) agonist with Ki of 26 nM; no affinity for α1β1γδ and α3β4 nAChRs (IC50 ≥ 60 μM).IC50 value: 26 nM(Ki) [1]Target: α7 nAChR agonistin vitro: Treatment with PNU-282987 resulted in an attenuation of neuroinflammation in the MPTP-lesioned SN. Furthermore, PNU-282987 attenuated MPTP-induced dopaminergic cell loss in the SN and reduced striatal dopamine depletion [3].in vivo: Mice were subjected to 70% partial hepatic I/R for 60 min and pretreated with either vehicle or with PNU-282987, and blood and hepatic tissue samples were collected at 3, 6, and 12 h following reperfusion. pretreatment with PNU-282987 decreased serum transaminase levels and ameliorated liver injury after hepatic I/R. Moreover, pretreatment with PNU-282987 suppressed NF-κB activation, cytokine production (tumor necrosis factor α, interleukin 1β), and HMGB1 expression in liver after hepatic I/R [2]. Mice treated with 2.5 and 10 mg/kg of PNU devoted less time to rearing into open arms. In the HB task, MC mice displayed higher exploratory activity reflected in more head-dips (HD) during the first minute than EE and SE, whereas EE displayed low exploration levels reflected in total HD (5 min) [4].

Related Catalog

Signaling Pathways >>Membrane Transporter/Ion Channel >>nAChRSignaling Pathways >>Neuronal Signaling >>nAChRResearch Areas >>Neurological Disease

References

[1]. Bodnar AL, et al. Discovery and structure-activity relationship of quinuclidine benzamides as agonists of alpha7 nicotinic acetylcholine receptors. J Med Chem. 2005 Feb 24;48(4):905-8.

[2]. Li F, et al. The protective effect of PNU-282987, a selective α7 nicotinic acetylcholine receptor agonist, on the hepatic ischemia-reperfusion injury is associated with the inhibition of high-mobility group box 1 protein expression and nuclear factor κB activation in mice. Shock. 2013 Feb;39(2):197-203.

[3]. Stuckenholz V, et al. The α7 nAChR agonist PNU-282987 reduces inflammation and MPTP-induced nigral dopaminergic cell loss in mice. J Parkinsons Dis. 2013;3(2):161-72.

[4]. Mesa-Gresa P, et al. Behavioral effects of different enriched environments in mice treated with the cholinergic agonist PNU-282987. Behav Processes. 2014 Mar;103:117-24.

[5]. Dong Jun Yu, et al. Effect of ischemic preconditioning combined with α7 nAchR agonists on limb ischemia-reperfusion lung injury in rat. Biomed Res. 2017; Special Issue: ISSN 0970.

Chemical & Physical Properties

Density	1.3±0.1 g/cm3
Boiling Point	431.5±30.0 °C at 760 mmHg
Molecular Formula	C₁₄H₁₈Cl₂N₂O
Molecular Weight	301.21
Flash Point	214.8±24.6 °C
PSA	32.34000
LogP	2.49
Vapour Pressure	0.0±1.0 mmHg at 25°C
Index of Refraction	1.612
InChIKey	HSEQUIRZHDYOIX-ZOWNYOTGSA-N
SMILES	Cl.O=C(NC1CN2CCC1CC2)c1ccc(Cl)cc1
Storage condition	2-8℃

Synonyms

PNU-282987

N-[(3R)-1-Azabicyclo[2.2.2]oct-3-yl]-4-chlorobenzamide

Kisspeptin 234

Benzamide, N-[(3R)-1-azabicyclo[2.2.2]oct-3-yl]-4-chloro-

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