SYNTHESIS OF A POTENT WIDE-SPECTRUM SEROTONIN-REUPTAKE, NOREPINEPHRINE-REUPTAKE, DOPAMINE-REUPTAKE INHIBITOR (SNDRI) AND A SPECIES-SELECTIVE DOPAMINE-REUPTAKE INHIBITOR BASED ON THE GAMMA-AMINO ALCOHOL FUNCTIONAL-GROUP
Pr. Carlier et al., SYNTHESIS OF A POTENT WIDE-SPECTRUM SEROTONIN-REUPTAKE, NOREPINEPHRINE-REUPTAKE, DOPAMINE-REUPTAKE INHIBITOR (SNDRI) AND A SPECIES-SELECTIVE DOPAMINE-REUPTAKE INHIBITOR BASED ON THE GAMMA-AMINO ALCOHOL FUNCTIONAL-GROUP, Bioorganic & medicinal chemistry letters, 8(5), 1998, pp. 487-492
A series of gamma-amino alcohols were synthesized and screened for reu
ptake inhibition and noncompetitive NMDA antagonism. Compound (+/-)-3f
simultaneously and potently inhibits reuptake of 5-HT, NE, and DA, re
presenting a potential wide-spectrum reuptake inhibitor antidepressant
. In addition, comparative rat and human studies uncovered a species-s
elective DA reuptake inhibitor (+/-)-2e, K-D(kDAT)/K-D(rDAT) = 97. (C)
1998 Elsevier Science Ltd. All rights reserved.