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Influence of Angiotensin II on α1-Adrenergic Receptors Function in Rat Aorta and Expression in Vascular Smooth Muscle Cells
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作者 Itzell Alejandrina Gallardo-Ortíz Juan Pablo de Jesús Benítez-Garrido +3 位作者 Santiago C. Sigrist-Flores Juan Javier López-Guerrero Enrique Hong Rafael Villalobos-Molina 《Journal of Biosciences and Medicines》 2024年第4期123-134,共12页
Angiotensin II (Ang II) is the main mediator of the Renin-Angiotensin-System acting on AT<sub>1</sub> and other AT receptors. It is regarded as a pleiotropic agent that induces many actions, including func... Angiotensin II (Ang II) is the main mediator of the Renin-Angiotensin-System acting on AT<sub>1</sub> and other AT receptors. It is regarded as a pleiotropic agent that induces many actions, including functioning as a growth factor, and as a contractile hormone, among others. The aim of this work was to examine the impact of Ang II on the expression and function of α<sub>1</sub>-adrenergic receptors (α<sub>1</sub>-ARs) in cultured rat aorta, and aorta-derived smooth muscle cells. Isolated Wistar rat aorta was incubated for 24 h in DMEM at 37˚C, then subjected to isometric tension and to the action of added norepinephrine, in concentration-response curves. Ang II was added (1 × 10<sup>−5</sup> M), and in some experiments, 5-Methylurapidil (α<sub>1A</sub>-AR antagonist), AH11110A (α<sub>1B</sub>-AR antagonist), or BMY-7378 (α<sub>1D</sub>-AR antagonist), were used to identify the α<sub>1</sub>-AR involved in the response. Desensitization of the contractile response to norepinephrine was observed due to incubation time, and by the Ang II action. α<sub>1D</sub>-AR was protected from desensitization by BMY-7378;while RS-100329 and prazosin partially mitigated desensitization. In another set of experiments, isolated aorta-derived smooth muscle cells were exposed to Ang II and α<sub>1</sub>-ARs proteins were evaluated. α<sub>1D</sub>-AR increased at 30 and 60 min post Ang II exposure, the α<sub>1A</sub>-AR diminished from 1 to 4 h, while α<sub>1B</sub>-AR remained unchanged over 24 h of Ang II exposure. Ang II induced an increase of α<sub>1D</sub>-AR at short times, and BMY-7378 protected α<sub>1D</sub>-AR from desensitization. 展开更多
关键词 Angiotensin II α1D-ar α1-ar Expression Rat aorta Smooth Muscle Cells
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卤代芳氧烷胺类α_1-肾上腺素受体拮抗剂的合成、生物活性及构效关系研究 被引量:3
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作者 习保民 李华 +3 位作者 张斌 倪沛洲 夏霖 江振洲 《中国药物化学杂志》 CAS CSCD 2005年第1期5-11,共7页
目的设计合成卤代苯氧烷胺类α1 肾上腺素受体 (α1 AR)拮抗剂并研究它们的降压活性及构效关系。方法根据苯氧烷胺类化合物DDPH的代谢物设计合成 12个卤代芳氧烷胺类化合物 ,以 2 ,6 二甲基苯酚为原料经多步反应得中间体卤代苯氧丙酮 ... 目的设计合成卤代苯氧烷胺类α1 肾上腺素受体 (α1 AR)拮抗剂并研究它们的降压活性及构效关系。方法根据苯氧烷胺类化合物DDPH的代谢物设计合成 12个卤代芳氧烷胺类化合物 ,以 2 ,6 二甲基苯酚为原料经多步反应得中间体卤代苯氧丙酮 ,再还原胺化得目标物 ,测试了目标化合物的降压活性 ,并用WHIM描述子进行构效关系研究。结果共合成 12个目标物 ,其结构经红外、质谱、核磁共振谱确证。药理实验显示 :12个目标物均具有一定的降压活性 ,化合物 3、10有较强的降压作用 ,但降压持续时间均比DDPH短。结论提高整个分子的对称性 ,或降低分子的取代基的复杂程度 ,对延长该类药物的降压时间是有利的。 展开更多
关键词 药物化学 制备 化学合成 α1-肾上腺索受体拮抗剂 QSAR 降压活性
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消癃通闭对犬大脑皮层α_1-肾上腺素受体的拮抗作用 被引量:1
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作者 贾金铭 严建霞 +4 位作者 孙利民 马春涛 吕志珍 李寅增 韩启德 《中药药理与临床》 CAS CSCD 2000年第3期31-32,共2页
消癃通闭浸出液与犬大脑皮层粗制膜及IBE12 5作用测定其对IBE12 5与犬大脑皮层α1 AR结合的抑制作用 ,结果消癃通闭对IBE12 5犬大脑皮层的结合呈竞争性拮抗作用 ,IC50 为 3 4 0± 6 0 g/L ,Hill系数为 0 70± 0 0 6,佐证本... 消癃通闭浸出液与犬大脑皮层粗制膜及IBE12 5作用测定其对IBE12 5与犬大脑皮层α1 AR结合的抑制作用 ,结果消癃通闭对IBE12 5犬大脑皮层的结合呈竞争性拮抗作用 ,IC50 为 3 4 0± 6 0 g/L ,Hill系数为 0 70± 0 0 6,佐证本方具有α1 AR拮抗作用。 展开更多
关键词 前列腺增生 消癃通闭 Α1-肾上腺素受体 拮抗作用 放射配基结合试验 药理学
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