3-[[(4-Aryl-1-piperazinyl) alkyl] cyclohexyl]-1 H-indoles as Dopamine D2 Partial Agonists and Autoreceptor Agonists

…, LM Georgic, TA Pugsley, SZ Whetzel…

Index: Wustrow, David J.; Smith III, William J.; Corbin, Ann E.; Davis, M. Duff; Georgic, Lynn M.; Pugsley, Thomas A.; Whetzel, Steven Z.; Heffner, Thomas G.; Wise, Lawrence D. Journal of Medicinal Chemistry, 1997 , vol. 40, # 2 p. 250 - 259

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Citation Number: 10

Abstract

A series of arylpiperazines and tetrahydropyridines joined to indoles by semirigid cycloalkyl spacers were prepared. Target compounds were studied for their ability to bind to the DA D2 receptor in vitro and to inhibit dopamine synthesis and spontaneous locomotor activity in rats. Effects of tether length and relative stereochemistry were assessed for a series of 2- pyridylpiperazines. The cyclohexylethyl spacer was found to be the most active in the ...