1451411-31-6Relevant articles and documents
Toward the development of bivalent ligand probes of cannabinoid CB1 and Orexin OX1 receptor heterodimers
Perrey, David A.,Gilmour, Brian P.,Thomas, Brian F.,Zhang, Yanan
, p. 634 - 638 (2014/07/07)
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 interaction with CB1-OX1 dimers. Bivalent ligands targeting CB1-OX1 receptor dimers could be potentially useful as a tool for further exploring the roles of such heterodimers in vitro and in vivo.