Ontology highlight
ABSTRACT:
SUBMITTER: Perrey DA
PROVIDER: S-EPMC3849818 | biostudies-literature | 2013 Sep
REPOSITORIES: biostudies-literature
Perrey David A DA German Nadezhda A NA Gilmour Brian P BP Li Jun-Xu JX Harris Danni L DL Thomas Brian F BF Zhang Yanan Y
Journal of medicinal chemistry 20130826 17
Increasing evidence implicates the orexin 1 (OX1) receptor in reward processes, suggesting OX1 antagonism could be therapeutic in drug addiction. In a program to develop an OX1 selective antagonist, we designed and synthesized a series of substituted tetrahydroisoquinolines and determined their potency in OX1 and OX2 calcium mobilization assays. Structure-activity relationship (SAR) studies revealed limited steric tolerance and a preference for electron deficiency at the 7-position. Pyridylmethy ...[more]