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| Cas No.: | 123464-89-1 |
| Chemical Name: | PNU282987 HCl |
| Synonyms: | Benzamide,N-(3R)-1-azabicyclo[2.2.2]oct-3-yl-4-chloro-, hydrochloride (1:1);N-(3R)-1-Azabicyclo[2.2.2]oct-3-yl-4-chlorobenzamide hydrochloride;PNU 282987;PNU 282987,N-(3R)-1-Azabicyclo[2.2.2]oct-3-yl-4-chlorobenzamide;PNU-282,987;Kisspeptin 234;PNU282987 HCl;PNU 282987(PNU 282987 hydrochloride);N-(3R)-1-AZABICYCLO[2.2.2]OCT-3-YL-4-CHLOROBENZAMIDE;N-(3R)-1-Azabicyclo[2.2.2]oct-3-yl-4-chlorobenzamide hydrochloride PNU 282987;PNU-282987 |
| SMILES: | ClC1=CC=C(C=C1)C(=O)N[C@@H]2C3CCN(CC3)C2 |
| Formula: | C14H18Cl2N2O |
| M.Wt: | 301.211 |
| Purity: | >98% |
| Sotrage: | 2 years -20°C Powder, 2 weeks4°C in DMSO,6 months-80°C in DMSO |
| 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). |
| Target: | IC50 value: 26 nM(Ki) [1] Target: α7 nAChR agonist |
| 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]. |
| In 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]. |
| 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. |