Vassilev P, Radomirov R
Department of Experimental Pharmacology, Bulgarian Academy of Sciences, Sofia.
Prostaglandins. 1992 Nov;44(5):471-83. doi: 10.1016/0090-6980(92)90141-f.
Prostaglandin E2 (PGE2) applied cumulatively (1 nM-1 microM) induced concentration-dependent tonic contractions in the longitudinal muscle of isolated rat rectum. The PGE2 effects were not altered by guanethidine (50 microM), whereas atropine (3 microM), guanethidine plus atropine or tetrodotoxin (0.1 microM) reduced them to an almost equal extent and increased the EC50 values for PGE2. The after-contractions following electrical stimulation were enhanced by PGE2 (10 nM) and inhibited by atropine. Diphloretin phosphate (DPP, 100 microM) shifted the regression lines for PGE2 to the right in both untreated and tetrodotoxin-treated preparations, and thereby increased the EC50 values. Slopes of the concentration-effect lines for PGE2 before and after DPP differed in the presence of tetrodotoxin. The regression line for PGE2 with SC 19220 (100 microM) in tetrodotoxin-treated preparations was shifted to the right in a parallel fashion. It is concluded that PGE2 exerted both a neural (cholinergic) and a smooth muscle effect. There may be a competitive antagonism between SC 19220 and PGE2 but the block by DPP may be nonselective.
累积应用前列腺素E2(PGE2,1 nM - 1 microM)可诱导离体大鼠直肠纵肌产生浓度依赖性的强直性收缩。胍乙啶(50 microM)不改变PGE2的作用,而阿托品(3 microM)、胍乙啶加阿托品或河豚毒素(0.1 microM)可将其作用降低至几乎相同程度,并增加PGE2的半数有效浓度(EC50)值。电刺激后的后收缩可被PGE2(10 nM)增强,并被阿托品抑制。磷酸二氯雷他定(DPP,100 microM)可使未处理和河豚毒素处理的标本中PGE2的回归线右移,从而增加EC50值。在存在河豚毒素的情况下,DPP处理前后PGE2浓度 - 效应线的斜率不同。在河豚毒素处理的标本中,PGE2与SC 19220(100 microM)的回归线以平行方式右移。结论是,PGE2发挥了神经(胆碱能)和平滑肌作用。SC 19220与PGE2之间可能存在竞争性拮抗作用,但DPP的阻断作用可能是非选择性的。