Manku M S, Horrobin D F
Prostaglandins. 1976 Nov;12(5):789-801. doi: 10.1016/0090-6980(76)90053-8.
Chloroquine, quinine, procaine, quinidine and clomipramine behave as prostaglandin (PG) antagonists in a rat mesenteric vascular bed preparation. The ID50 concentrations were within the range of therapeutically effective human plasma levels in each case. Antagonism to PGE2 was studied in detail and seemed to be at least in part competitive. The drugs also antagonized the effects of PGs A1, A2, F2alpha and E1. Each drug also had weak prostaglandin agonist activity but only over a very narrow range of concentrations. It is possible that some of the clinical actions of these drugs may depend on blockade or imitation of natural PG effects. The findings suggest new approaches to the search for PG antagonists, a new screening technique for anti-inflammatory drugs and possible new uses for these established drugs. A preliminary study suggests that chloroquine may be successful in closing a patent ductus arteriosus in infants.
氯喹、奎宁、普鲁卡因、奎尼丁和氯米帕明在大鼠肠系膜血管床制备中表现为前列腺素（PG）拮抗剂。每种药物的半数抑制浓度（ID50）均在人类治疗有效血浆水平范围内。对前列腺素E2（PGE2）的拮抗作用进行了详细研究，似乎至少部分是竞争性的。这些药物还拮抗前列腺素A1、A2、F2α和E1的作用。每种药物也具有微弱的前列腺素激动剂活性，但仅在非常窄的浓度范围内。这些药物的某些临床作用可能取决于对天然前列腺素效应的阻断或模拟。这些发现为寻找前列腺素拮抗剂提供了新方法，为抗炎药物提供了新的筛选技术，并为这些已确立的药物带来了可能的新用途。一项初步研究表明，氯喹可能成功闭合婴儿的动脉导管未闭。
