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化驗
≥98% (HPLC)
形狀
solid
儲存條件
desiccated
溶解度
DMSO: >10 mg/mL
儲存溫度
2-8°C
SMILES 字串
Cl[H].[H]O[H].Clc1ccc(cc1)C(=O)N[C@H]2CN3CCC2CC3
InChI
1S/C14H17ClN2O.ClH.H2O/c15-12-3-1-11(2-4-12)14(18)16-13-9-17-7-5-10(13)6-8-17;;/h1-4,10,13H,5-9H2,(H,16,18);1H;1H2/t13-;;/m0../s1
InChI 密鑰
OCWLMMBVXIESNP-GXKRWWSZSA-N
應用
PNU-282987 水合物用于检查其在伤口修复中的活性,即通过在链脲佐菌素(STZ)诱导的糖尿病小鼠模型中抑制 AGE(高级糖化终产物)介导的肿瘤坏死因子-α (TNF-α)产生。 还用于评价烟碱 α-7乙酰胆碱受体(nAChRα7)激活对非糖尿病伤口愈合的影响。
生化/生理作用
PNU-282987是烟碱 α-7乙酰胆碱受体(nAChRα7)激动剂。 它有助于减少脂多糖(LPS)刺激引起的急性肺损伤(ALI)。PNU-282987 可增加脑切片中 GABA 能的突触活性,有助于恢复麻醉大鼠的听觉门控缺陷。
同聚 α7 烟碱乙酰胆碱受体 (nAChR) 表达减少与精神分裂症感觉信息处理能力丧失有关。PNU-282987 是一种新型的 α7nachr 选择性激动剂,可诱发培养的大鼠海马神经元全细胞电流,该神经元对选择性 α7nachr 拮抗剂 methyllycaconitine (MLA) 敏感,并增强 gaba 能突触活性。α7nachr 激动剂 PNU-282987 改善听觉门控和增强海马振荡活动。这些结果进一步支持了选择性激活 α7 受体的药物可能为精神分裂症的治疗提供一种新的、潜在的药物治疗。
特點和優勢
该化合物在受体分类和信号转导手册的乙酰胆碱受体(烟碱型)页面上有详细描述。想要浏览手册的其他页面, 请单击此处。
注意
空气敏感
儲存類別代碼
11 - Combustible Solids
水污染物質分類(WGK)
WGK 3
閃點(°F)
Not applicable
閃點(°C)
Not applicable
Activation of alpha7nAChR promotes diabetic wound healing by suppressing AGE-induced TNF-alpha production
Inflammation, 39(2), 687-699 (2016)
The selective alpha7 nicotinic acetylcholine receptor agonist PNU-282987 [N-[(3R)-1-azabicyclo [2.2. 2] oct-3-yl]-4-chlorobenzamide hydrochloride] enhances GABAergic synaptic activity in brain slices and restores auditory gating deficits in anesthetized rats
Journal of Pharmacology and Experimental Therapeutics, 312(3), 1213-1222 (2005)
alpha7-nAChR Activation Has an Opposite Effect on Healing of Covered and Uncovered Wounds
Inflammation, 41(2), 474-484 (2018)
Acute lung injury is reduced by the alpha7nAChR agonist PNU-282987 through changes in the macrophage profile
Faseb Journal, 31(1), 320-332 (2016)
Molecular medicine reports, 19(5), 3791-3798 (2019-03-14)
The cholinergic anti‑inflammatory pathway is considered an attractive approach for the alleviation of inflammatory diseases. Sepsis is characterized by systemic inflammation and widespread organ injury, especially that in the lung. In the present study, we explored the effects of an
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Sigma-Aldrich offers many products related to nicotinic acetylcholine receptors for your research needs.
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