α-肾上腺素能受体试剂。3. 一些2-取代的1,4-苯并二噁烷作为选择性突触前α2-肾上腺素能受体拮抗剂的合成。
Alpha-adrenoreceptor reagents. 3. Synthesis of some 2-substituted 1,4-benzodioxans as selective presynaptic alpha 2-adrenoreceptor antagonists.
作者信息
Stillings M R, Chapleo C B, Butler R C, Davis J A, England C D, Myers M, Myers P L, Tweddle N, Welbourn A P, Doxey J C
出版信息
J Med Chem. 1985 Aug;28(8):1054-62. doi: 10.1021/jm00146a013.
PMID:2862284
Abstract
The synthesis and pharmacological activity of a series of 2-substituted derivatives of the selective alpha 2-adrenoreceptor antagonist idazoxan (RX 781094) is described. Substitution in this position by alkyl, alkenyl, cycloalkenyl, and alkoxy groups in many cases gives compounds whose potencies and selectivities are significantly greater than those of the parent compound.
摘要
本文描述了一系列选择性α2-肾上腺素能受体拮抗剂伊达唑烷（RX 781094）的2-取代衍生物的合成及药理活性。在该位置用烷基、烯基、环烯基和烷氧基取代，在许多情况下得到的化合物其效力和选择性明显高于母体化合物。
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