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Synthesis and pharmacological investigation of aralkyl diamine derivatives as potential triple reuptake inhibitors.
- Source :
-
European Journal of Medicinal Chemistry . Oct2014, Vol. 86, p219-234. 16p. - Publication Year :
- 2014
-
Abstract
- A series of aralkyl diamine derivatives were designed, synthesized, and evaluated for their triple reuptake inhibitory abilities. Compounds 18c (5-HT, NE, DA, IC 50 = 389, 69, 238 nM), 36a (5-HT, NE, DA, IC 50 = 378, 477, 247 nM), and 36d (5-HT, NE, DA, IC 50 = 501, 206, 357 nM) showed in vivo activities in the rat forced swim test at 5, 10, and 20 mg/kg PO. 36a was identified as the most promising candidate in this study. Specifically, 36a exhibited high selectivity for monoamine transporters over a number of CNS-related targets. Furthermore, 36a showed a good pharmacokinetic properties and acceptable safety profile in preclinical studies. [ABSTRACT FROM AUTHOR]
- Subjects :
- *DIAMINES
*LABORATORY rats
*PHARMACOKINETICS
*PHARMACOLOGY
*CHEMICAL synthesis
Subjects
Details
- Language :
- English
- ISSN :
- 02235234
- Volume :
- 86
- Database :
- Academic Search Index
- Journal :
- European Journal of Medicinal Chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 98809612
- Full Text :
- https://doi.org/10.1016/j.ejmech.2014.08.045