Partial agonist efficacy of EMD386088, a 5-HT6 receptor ligand, in functional in vitro assays.
Journal Title: Pharmacological Reports - Year 2013, Vol 65, Issue 4
Abstract
Over recent years, the 5-hydroxytryptamine6 (5-HT6) receptor has emerged as a promising molecular target which interacts with several central nervous system acting drugs. In animal models, both agonists and antagonists of this receptor exhibit equivalent potency and efficacy as potential antidepressants, anxiolytics and anti-obesity or anti-dementia drugs. EMD386088 (5-chloro-2-methyl-3-(1,2,3,6-tetrahydro-4-pyridinyl)-1H-indole hydrochloride) has been described as a high affinity 5-HT6 receptor ligand with a full agonist activity and with moderate affinity for 5-HT3 sites.
Authors and Affiliations
Magdalena Jastrzębska-Więsek, Agata Siwek, Grzegorz Kazek, Barbara Nawieśniak, Anna Partyka, Monika Marcinkowska, Marcin Kołaczkowski
Keywords
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