New serotonin 5-HT1A receptor agonists endowed with antinociceptive activity in vivo

…, B Benhamú, ML López-Rodríguez

Index: Valhondo, Margarita; Marco, Isabel; Martin-Fontecha, Mar; Vazquez-Villa, Henar; Ramos, Jose A.; Berkels, Reinhard; Lauterbach, Thomas; Benhamu, Bellinda; Lopez-Rodriguez, Maria L. Journal of Medicinal Chemistry, 2013 , vol. 56, # 20 p. 7851 - 7861

Full Text: HTML

Citation Number: 11

Abstract

We report the synthesis of new compounds 4–35 based on two different openings (A and B) of the chromane ring present in the previously identified 5-HT1A receptor (5-HT1AR) ligand 3. The synthesized compounds were assessed for binding affinity, selectivity, and functional activity at the 5-HT1AR. Selected candidates resulting from B opening were also evaluated for their potential antinociceptive effect in vivo and pharmacokinetic properties in vitro. ...