Lellouche J P, Aubert F, Beaucourt J P, Rechencq E, Niel G, Girard J P, Rossi J C, Boucard M
Service des Molecules Marquées, Centre d'Etudes Nucleaires de Saclay, C.E.A., Gif sur Yvette, France.
Prostaglandins. 1989 Jan;37(1):93-103. doi: 10.1016/0090-6980(89)90034-8.
The (5S,6R) isomers of new acetylenic and allenic analogues of leukotrienes C4 and D4 were synthesized for comparative pharmacological studies on intestinal smooth muscle preparations. These new analogues are poor spasmogenic agonists, the replacement of the 11,12-ene with a relatively more stable triple bond causing an important reduction in intrinsic activity. They did not show any significant antagonist activity. Unexpectedly, these results prove that the 11,12 portion in the triene structure of the lipophilic chain is critical for an agonist activity.
合成了白三烯C4和D4新型炔类及联烯类类似物的(5S,6R)异构体，用于对肠平滑肌制剂进行比较药理学研究。这些新型类似物是较弱的致痉挛激动剂，用相对更稳定的三键取代11,12-烯导致内在活性显著降低。它们未表现出任何显著的拮抗活性。出乎意料的是，这些结果证明亲脂性链三烯结构中的11,12部分对激动剂活性至关重要。
