Arrestin-3/β-Arrestin 2 Agonist

IHCH-7086 is a blood-brain barrier-permeable, partial β-arrestin-biased agonist of 5-HT_2AR with a K_i of 12.59 nM. IHCH-7086 blocks D-lysergic acid diethylamide-induced head-twitch response in mice and alleviates depression-like behaviors in mice subjected to acute restraint stress or injected with Corticosterone (HY-B1618). IHCH-7086 is applicable to research related to depression.

GEP44 is a peptide biased triple agonist targeting Glucagon-like peptide 1 receptor (GLP-1R), neuropeptide Y1 Receptor (Y1-R), and neuropeptide Y2 Receptor (Y2-R). GEP44 induces Y1-R antagonist-controlled, GLP-1R-dependent stimulation of insulin secretion in both rat and human pancreatic islets by counteracting effects of Y1-R and GLP-1R agonism. GEP44 promotes insulin-independent Y1-R-mediated glucose uptake in muscle tissue and significantly reduces food intake and body weight in diet-induced obese rat models. GEP44 can be used for obesity and type 2 diabetes mellitus research.

ID110460002 possesses both full agonist activity at the μ-opioid receptor (OPRM) and agonist activity at the δ-opioid receptor (OPRD). ID110460002 acts as a potent agonist for the G protein pathways of both receptors, but exhibits only very weak partial agonist activity towards the β-arrestin-2 pathway. The agonistic potency of ID110460002 at OPRM has extremely high intrinsic activity and is unaffected by reduced receptor expression levels, while its potency at OPRD depends on receptor expression levels. ID110460002 displays tissue- or organ-dependent properties, and serves as a critical compound for investigating pain mechanisms and analgesia.