Derivatives of cis-2-Amino-8-hydroxy-1-methyltetralin: Mixed 5-HT1A-Receptor Agonists and Dopamine D2-Receptor Antagonists
作者:Ye Liu、Hong Yu、Nina Mohell、Gunnar Nordvall、Tommy Lewander、Uli Hacksell
DOI:10.1021/jm00001a020
日期:1995.1
(1S,2R)-8-Hydroxy-1-methyl-2-(dipropylamino)tetralin [(1S,2R)-3] has been previously characterized as a selective and potent but partial 5-HT1A-receptor agonist. In the present study, we have prepared derivatives of (1S,2R)- and (1R,2S)-3 in which various C8-substituents have been introduced. In addition, the enantiomers of the N-isopropyl-N-n-propylamino derivative of 3 were prepared. The new derivatives
(1S,2R)-8-羟基-1-甲基-2-(二丙基氨基)四氢化萘[(1S,2R)-3]先前已被表征为选择性和有效但部分的5-HT1A-受体激动剂。在本研究中,我们制备了(1S,2R)-和(1R,2S)-3的衍生物,其中引入了各种C8取代基。另外,制备了3的N-异丙基-Nn-丙基氨基衍生物的对映异构体。通过在大鼠中进行行为和生化测试,对新衍生物进行了体内测试。另外,通过与[3 H] -8-OH-DPAT在大鼠脑组织中的竞争实验研究了化合物的亲和力。表现得像选择性5-HT1A受体激动剂的唯一新衍生物是C8-羧酰胺衍生物(1S,2R)-13。其他活性衍生物,包括(1S,2R)-3