LY-2795050
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LY-2795050 is a chemical compound that acts as a selective antagonist of the kappa-opioid receptor (KOR). It was developed by Eli Lilly and Company as a potential therapeutic agent for the treatment of various neuropsychiatric disorders, including depression, anxiety, and addiction.
Pharmacology[edit | edit source]
LY-2795050 is notable for its high selectivity for the kappa-opioid receptor over other opioid receptors, such as the mu-opioid receptor (MOR) and the delta-opioid receptor (DOR). This selectivity is important because it allows researchers to study the specific effects of kappa-opioid receptor antagonism without the confounding effects of activity at other opioid receptors.
Mechanism of Action[edit | edit source]
The kappa-opioid receptor is a G-protein coupled receptor that is involved in modulating mood, perception of pain, and stress responses. Antagonism of the kappa-opioid receptor by LY-2795050 is thought to produce antidepressant and anxiolytic effects by blocking the dysphoric and stress-inducing effects of endogenous kappa-opioid receptor agonists, such as dynorphin.
Clinical Research[edit | edit source]
LY-2795050 has been investigated in clinical trials for its potential use in treating mood disorders and substance use disorders. Early studies have shown that it is well-tolerated in humans and may have beneficial effects on mood and anxiety.
Chemical Properties[edit | edit source]
LY-2795050 is a small molecule with the chemical formula C25H25N3O2. It is a chiral compound, meaning it has a specific three-dimensional arrangement that is important for its activity at the kappa-opioid receptor.
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