Tropicamide 是一种选择性的M4毒蕈碱乙酰胆碱受体拮抗剂,作为滴眼剂使用时,会产生短效瞳孔扩张和睫状肌麻痹。
产品描述
Tropicamide is a synthetic muscarinic antagonist with actions similar to atropine and with an anticholinergic property. Upon ocular administration, tropicamide binds to and blocks the muscarinic receptors in the sphincter and ciliary muscle in the eye. This inhibits the responses from cholinergic stimulation, producing dilation of the pupil and paralysis of the ciliary muscle. Tropicamide is a diagnostic agent and is used to produce short-duration mydriasis and cycloplegia.
体外活性
0.5% Nepafenac明显抑制(46%)血-视网膜屏障破坏,导致视网膜水肿减少65%,且几乎完全抑制PGE2合成(96%).Nepafenac在眼部的生物利用度明显更大. Nepafenac对COX-1的抑制活性较弱(IC50:64.3 μM).在兔中,Nepafenac抑制视网膜/脉络膜(55%)和虹膜/睫状体(85-95%)中前列腺素的合成.和对照组小鼠相比,Nepafenac使脉络膜新生血管和缺血引起视网膜新生血管明显减少.Nepafenac也使缺血诱导的视网膜VEGF mRNA表达增加减缓.在眼和转移性动物模型中,Nepafenac延缓恶性肿瘤进程并减少葡萄膜黑色素瘤重量.在胰岛素不足型糖尿病大鼠的视网膜微血管内,Nepafenac对视网膜前列腺素E(2),超氧化物,环氧合酶2和白细胞停滞均有显著抑制作用,但对血管内皮生长因子和一氧化氮无影响.在糖尿病大鼠中,Nepafenac明显抑制转移酶介导的dUTP缺口末端标记阳性毛细管细胞、周细胞和无细胞的毛细血管的数目.
Cas No.
1508-75-4
分子式
C17H20N2O2
分子量
284.359
别名
托吡卡胺;Ro 1-7683
储存和溶解度
DMSO:53 mg/mL (186.4 mM)
Ethanol:53 mg/mL (186.4 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years