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  • Title: Synthesis and SAR of highly potent dual 5-HT1A and 5-HT1B antagonists as potential antidepressant drugs.
    Author: Kling A, Lange UE, Mack H, Bakker MH, Drescher KU, Hornberger W, Hutchins CW, Möller A, Müller R, Schmidt M, Unger L, Wicke K, Schellhaas K, Steiner G.
    Journal: Bioorg Med Chem Lett; 2005 Dec 15; 15(24):5567-73. PubMed ID: 16219465.
    Abstract:
    Novel 5-HT(1) autoreceptor ligands based on the N-4-aryl-piperazinyl-N'-ethyl-5,6,7,8-tetrahydropyrido[4', 3':4,5]thieno[2,3-d]pyrimidin-4(3H)-one core are described. Aiming at antidepressants with a novel mode of action our objective was to identify potent antagonists showing balanced affinities and high selectivity for the 5-HT(1A) and 5-HT(1B) receptors. Strategies for the development of dual 5-HT(1A) and 5-HT(1B) antagonists based on 1 and 2 as leads and the corresponding results are discussed. Isoquinoline analogue 33 displayed high affinity and an antagonistic mode of action for the 5-HT(1A) and the 5-HT(1B) receptors and was characterized further with respect to selectivity, electrically stimulated [(3)H]5-HT release and in vivo efficacy.
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