In vivo Characterization of a Selective, Orally Available, and Brain Penetrant Small Molecule GPR139 Agonist

• Main Authors: James R. Shoblock (Author), Natalie Welty (Author), Ian Fraser (Author), Ryan Wyatt (Author), Brian Lord (Author), Timothy Lovenberg (Author), Changlu Liu (Author), Pascal Bonaventure (Author)
• Format: Book
• Published: Frontiers Media S.A., 2019-03-01T00:00:00Z.
• Subjects: article
• Online Access: Connect to this object online.

Recently, our group along with another demonstrated that GPR139 can be activated by L-phenylalanine (L-Phe) and L-tryptophan (L-Trp) at physiologically relevant concentrations. GPR139 is discretely expressed in brain, with highest expression in medial habenula. Not only are the endogenous ligands ca...