Doering, Skye R. published the artcileDiscovery of Nanomolar Melanocortin-3 Receptor (MC3R)-Selective Small Molecule Pyrrolidine Bis-Cyclic Guanidine Agonist Compounds Via a High-Throughput “”Unbiased”” Screening Campaign, Computed Properties of 104-01-8, the main research area is energy balance MC3R MC4R melanocortin agonist guanidines body weight.
The central melanocortin-3 and melanocortin-4 receptors (MC3R, MC4R) are key regulators of body weight and energy homeostasis. Herein, the discovery and characterization of first-in-class small mol. melanocortin agonists with selectivity for the melanocortin-3 receptor over the melanocortin-4 receptor are reported. Identified via “”unbiased”” mixture-based high-throughput screening approaches, pharmacol. evaluation of these pyrrolidine bis-cyclic guanidines resulted in nanomolar agonist activity at the melanocortin-3 receptor. The pharmacol. profiles at the remaining melanocortin receptor subtypes tested indicated similar agonist potencies at both the melanocortin-1 and melanocortin-5 receptors and antagonist or micromolar agonist activities at the melanocortin-4 receptor. This group of small mols. represents a new area of chem. space for the melanocortin receptors with mixed receptor pharmacol. profiles that may serve as novel lead compounds to modulate states of dysregulated energy balance.
Journal of Medicinal Chemistry published new progress about Body weight. 104-01-8 belongs to class isoquinoline, name is 4-Methoxyphenylacetic acid, and the molecular formula is C9H10O3, Computed Properties of 104-01-8.
Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem