Cannon J G, Koble-Suarez C, Long J P, Ilhan M, Bhatnagar R K
J Pharm Sci. 1985 Jun;74(6):672-5. doi: 10.1002/jps.2600740619.
Cis- and trans-4-n-Propyloctahydrobenzo(f)quinolines 4a,b were prepared for further assessment of dopaminergic effects of non-oxygenated dopamine congeners. The trans isomer 4b exhibited marked dopamine-like effects in the cat cardioaccelerator nerve assay and in a rat rotation model. Compound 4b produced dose-related lowering of blood pressure in the cat. The cis isomer 4a was inactive in these assays. Both compounds were inactive in a dopamine binding assay, but both appeared active in a spiroperidol binding assay. Both compounds are active alpha 1- and alpha 2-adrenoceptor antagonists. Compound 4b provides evidence that alpha 2-adrenoceptors and dopamine receptors are different entities, since this compound is an alpha 2 antagonist and a dopamine receptor agonist at presynaptic sites.
制备顺式和反式-4-正丙基八氢苯并(f)喹啉4a、4b，用于进一步评估非氧化多巴胺类似物的多巴胺能效应。反式异构体4b在猫心脏加速神经试验和大鼠旋转模型中表现出明显的多巴胺样效应。化合物4b在猫中产生与剂量相关的血压降低。顺式异构体4a在这些试验中无活性。两种化合物在多巴胺结合试验中均无活性，但在螺哌啶醇结合试验中均表现出活性。两种化合物都是活性α1和α2肾上腺素能受体拮抗剂。化合物4b提供了α2肾上腺素能受体和多巴胺受体是不同实体的证据，因为该化合物在突触前部位是α2拮抗剂和多巴胺受体激动剂。
