
Bioorganic and Medicinal Chemistry Letters p. 487 - 492 (1998)
Update date:2022-08-03
Topics:
Carlier, Paul R.
Lo, Michael M.-C.
Lo, Priscilla C.-K.
Richelson, Elliott
Tatsumi, Masahiko
Reynolds, Ian J.
Sharma, Terre A.
A series of gamma-amino alcohols were synthesized and screened for reuptake inhibition and noncompetitive NMDA antagonism. Compound (±)-3f simultaneously and potently inhibits reuptake of 5-HT, NE, and DA, representing a potential wide-spectrum reuptake inhibitor antidepressant. In addition, comparative rat and human studies uncovered a species-selective DA reuptake inhibitor (±)-2e, K(D)(hDAT)/K(D)(rDAT) = 97.
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