Birnbaum J E, Chan P S, Cervoni P, Dessy F, Van Humbeeck L
Prostaglandins. 1982 Feb;23(2):185-99. doi: 10.1016/0090-6980(82)90045-4.
Topically applied 16-vinylprostaglandins demonstrate the property of rapid transit through the skin and a profound effect on the cutaneous vasculature. At low concentrations in the guinea pig and rabbit. 15-deoxy-16-hydroxy-16-vinyl-PGE2 (DHV-PGE2) and its methyl ester (DHV-PGE2Me) elicit a distinct and persistent erythema which is restricted to the area of application and is not associated with a wheal. Skin temperatures are elevated for several hours following application. Accordingly, these compounds may have therapeutic utility in conditions where local blood flow is compromised or where an enhanced blood flow is desired . In the spontaneously hypertensive rat, topically applied DHV-PGE2 and DHV-PGE2Me produce a dramatic and persistent lowering of blood pressure. The maximal effects are comparable to those obtained wit equal oral or intravenous doses and are maintained for a longer period of time. Moreover, with the topical route, there is no prolongation in the time required for onset of action (3-5 minutes). It appears that while the skin presents only a minimal diffusion barrier to these compounds, a sufficient depot is maintained to give sustained release and prolonged duration. Transdermal delivery of 16-vinyl prostaglandins may offer a convenient means of achieving a clinical antihypertensive effect without the characteristic side effects generally associated with oral or intravascular prostaglandins.
局部应用的16-乙烯基前列腺素显示出能快速透过皮肤，并对皮肤血管系统有深远影响的特性。在豚鼠和兔子身上，低浓度的15-脱氧-16-羟基-16-乙烯基-PGE2（DHV-PGE2）及其甲酯（DHV-PGE2Me）会引发一种明显且持续的红斑，该红斑仅限于用药部位，且不伴有风团。用药后皮肤温度会升高数小时。因此，这些化合物在局部血流受损或需要增加血流的情况下可能具有治疗作用。在自发性高血压大鼠中，局部应用DHV-PGE2和DHV-PGE2Me会使血压显著且持续降低。最大效应与同等口服或静脉注射剂量所获得的效应相当，且维持时间更长。此外，通过局部给药途径，起效时间（3 - 5分钟）没有延长。看来，虽然皮肤对这些化合物仅呈现出最小的扩散屏障，但仍能维持足够的贮库以实现持续释放和延长作用时间。经皮递送16-乙烯基前列腺素可能提供一种方便的方法来实现临床抗高血压效果，而不会产生通常与口服或血管内前列腺素相关的典型副作用。
