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Chen CW, Tran JA, Jiang W, Tucci FC, Arellano M, Wen J, Fleck BA, Marinkovic D, White NS, Pontillo J, Saunders J, Madan A, Foster AC, Chen C: Propionylpiperazines as human melanocortin-4 receptor ligands. . Bioorg Med Chem Lett. 2006 Sep 15;16(18):4800-3. Epub 2006 Jul 7. A series of alpha-benzylpropionylpiperazines were synthesized and tested as antagonists of the melanocortin-4 receptor. In addition to its high potency and selectivity, R-11a had desirable pharmacokinetic properties including high brain penetration in mice. |
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