Boido V, Boido A, Boido-Canu C, Sparatore F
Farmaco Sci. 1979 Aug;34(8):673-87.
Since lupinylamine [(I); R = H] exhibits hypotensive activity, mainly due to ganglionic blocking properties, and it is known that a high degree of steric hindrance around the basic function of other ganglioplegic amines is of paramount importance for optimal activity, several guinolizidine derivatives were prepared. They differ in the length of the alkyl chain connected to the ring and in the position of the amino group along the chain. Some N-substituted derivatives of 2-quinolizidin-1'alpha-yl-ethylamine (II) together with O-lupinylhydroxylamine and 2-quinolizidin-1'beta-yl-ethylamine, respectively isosteric and epimeric to it, were also prepared. When administered orally to spontaneously hypertensive rats, the amines (II), (III) and (XI) produced high and long-lasting antihypertensive activity, while the remaining compounds so far tested were inactive or had only modest effect on blood pressure. Compared with alpha-methyl-DOPA, amine (II) appears to be approximately two to three times as potent. The antihypertensive activity of (II) appears to be linked to glanglionic blocking properties, since this amine proved 1,2 times as potent as mecamylamine in the inhibition of cat nictitating membrane response to stimulation of the preganglionic sympathetic nerve.
由于羽扇豆胺[（I）；R = H]具有降压活性，主要归因于神经节阻断特性，并且已知其他神经节阻断胺的碱性官能团周围的高度空间位阻对于最佳活性至关重要，因此制备了几种喹诺里西啶衍生物。它们在连接到环的烷基链的长度以及氨基沿链的位置上有所不同。还分别制备了2-喹诺里西啶-1'α-基-乙胺（II）的一些N-取代衍生物以及与其等排和差向异构的O-羽扇豆基羟胺和2-喹诺里西啶-1'β-基-乙胺。当口服给予自发性高血压大鼠时，胺（II）、（III）和（XI）产生了高且持久的降压活性，而迄今为止测试的其余化合物无活性或对血压仅有适度影响。与α-甲基多巴相比，胺（II）的效力似乎约为其两到三倍。（II）的降压活性似乎与神经节阻断特性有关，因为在抑制猫瞬膜对节前交感神经刺激的反应中，这种胺的效力被证明是美加明的1.2倍。
