Discovery of α-Substituted Imidazole-4-acetic Acid Analogues as a Novel Class of ρ 1 γ-Aminobutyric Acid Type A Receptor Antagonists with Effect on Retinal Vascular Tone

• Published in: ChemMedChem Vol. 11; no. 20; pp. 2299 - 2310
• Main Authors: Krall, Jacob, Brygger, Benjamin M, Sigurðardóttir, Sara B, Ng, Clarissa K L, Bundgaard, Christoffer, Kehler, Jan, Nielsen, Birgitte, Bek, Toke, Jensen, Anders A, Frølund, Bente
• Format: Journal Article
• Language: English
• Published: Germany 19.10.2016
• Subjects: Animals; Arterioles - drug effects; Arterioles - metabolism; Cells, Cultured; Dose-Response Relationship, Drug; Drug Discovery; Eye - drug effects; Humans; Imidazoles - administration & dosage; Imidazoles - chemistry; Imidazoles - pharmacology; Mice; Molecular Structure; Receptors, GABA-A - metabolism; Retinal Vessels - drug effects; Retinal Vessels - metabolism; Structure-Activity Relationship; Swine; imidazole-4-acetic acid; GABAC receptors; retinal vascular tone; structure-activity relationships; ρ GABAA receptors

The ρ-containing γ-aminobutyric acid type A receptors (GABA Rs) play an important role in controlling visual signaling. Therefore, ligands that selectively target these GABA Rs are of interest. In this study, we demonstrate that the partial GABA R agonist imidazole-4-acetic acid (IAA) is able to pen...