基於點擊化學的基托桑衍生品N-(levodopa) 在腦細胞中顯示了生物功能
Olimpia Ortega-Fimbres1, Marcelino Montiel-Herrera1, Denisse García-Villa1
1Department of Medicine and Health Sciences, University of Sonora, Hermosillo, Sonora, Mexico.
Drug development and industrial pharmacy
|June 13, 2023
概括
合成了新型的N- ((levodopa) 基托衍生物,并表明它们进入大脑细胞. 这些衍生物可以转化为多巴胺,为治疗神经退行性疾病提供了潜在的潜力.
科学领域:
- 生物材料科学 生物材料科学
- 神经科学是一个神经科学.
- 药物运输 药物运输 药物运输
背景情况:
- 开发用于神经退行性疾病的有效药物输送系统是具有挑战性的,因为血脑屏障.
- 奇托是一种生物相容的聚合物,有可能用于药物输送应用.
研究的目的:
- 使用点击化学合成N- ((levodopa) 奇托衍生物.
- 研究这些衍生物穿越脑细胞膜并产生生物医学效应的能力.
- 探索它们作为治疗神经系统疾病的药物储备的潜力.
主要方法:
- 通过点击化学合成N-(levodopa) 基托衍生物.
- 描述包括FT-IR,1H-NMR,TGA和动态光散射.
- 通过Ca2+成像和UPLC评估细胞反应,使用了初级大鼠大脑细胞培养物.
主要成果:
- 基托桑衍生物N-(levodopa) 在脑细胞中成功诱导了细胞内Ca2+反应.
- UPLC分析证实了脑细胞内多巴转化为多巴胺的情况.
- 这项研究证明了宏分子大脑细胞膜穿越的概念证明.
结论:
- N-利沃多巴) 基托衍生物可以穿透大脑细胞膜并表现出生物活性.
- 这些衍生物充当分子储库,在脑细胞内转化为多巴胺.
- 这种方法对开发神经退行性疾病的新型治疗策略具有前景.
相关概念视频
Direct-Acting Cholinergic Agonists: Pharmacokinetics
1.3K
Direct-acting cholinergic agonists, such as synthetic choline esters and naturally occurring alkaloids, exert their effects by enhancing the actions of acetylcholine and stimulating the parasympathetic nervous system. Synthetic choline esters share structural similarities with acetylcholine. For example, they have a positively charged quaternary ammonium or onium group, contributing to their hydrophilic characteristics. As a result, they are poorly absorbed in the body through oral...
1.3K
Direct-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship
1.1K
Cholinergic agonists or cholinomimetics mimic the action of acetylcholine to stimulate the parasympathetic nervous system. They are categorized into direct-acting and indirect-acting agents. The direct-acting cholinergic drugs induce the parasympathetic response by directly binding to the muscarinic or nicotine receptors. In comparison, the indirect-acting cholinergic drugs prevent acetylcholine hydrolysis, indirectly contributing to the extended parasympathetic response.
The direct-acting...
The direct-acting...
1.1K
Cholinergic Antagonists: Chemistry and Structure-Activity Relationship
2.3K
Cholinergic antagonists bind to cholinergic receptors and limit the effects of acetylcholine and other cholinergic agonists. Based on the specific cholinergic receptor affinity, these antagonists are classified as muscarinic or nicotinic. Anticholinergics interrupt parasympathetic innervations while sympathetic innervations remain uninterrupted. Muscarinic antagonists are also called 'muscarinic antagonists', 'antimuscarinics', or 'parasympatholytics'. Nicotinic...
2.3K


