Toward the Development of Bivalent Ligand Probes of Cannabinoid CB1 and Orexin OX1 Receptor Heterodimers.
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ABSTRACT:
SUBMITTER: Perrey DA
PROVIDER: S-EPMC4060943 | biostudies-literature | 2014 Jun
REPOSITORIES: biostudies-literature
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Toward the Development of Bivalent Ligand Probes of Cannabinoid CB1 and Orexin OX1 Receptor Heterodimers.
Perrey David A DA Gilmour Brian P BP Thomas Brian F BF Zhang Yanan Y
ACS medicinal chemistry letters 20140325 6
Cannabinoid CB1 and orexin OX1 receptors have been suggested to form heterodimers and oligomers. Aimed at studying these complexes, a series of bivalent CB1 and OX1 ligands combining SR141716 and ACT-078573 pharmacophores were designed, synthesized, and tested for activity against CB1 and OX1 individually and in cell lines that coexpress both receptors. Compound 20 showed a robust enhancement in potency at both receptors when coexpressed as compared to individually expressed, suggesting possible ...[more]
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