L-803,087

{{Drugbox | verifiedrevid = 477318123 | IUPAC_name = (1R,2R)-3-[[2-(2,3-dihydro-1-benzofuran-5-yl)ethyl]amino]-1-[[3-(trifluoromethyl)phenyl]methyl]cyclopentane-1,2-diol | image = L-803,087_structure.png | width = 200 | CAS_number = 161314-49-2 | PubChem = 9938895 | ChemSpiderID = 8114955 | UNII = 3X0FQ0KJ7Z | KEGG = D06092 | C=21 | H=24 | F=3 | N=1 | O=3 | smiles = C1CC(C(C1O)O)C(C2=CC(=CC=C2)C(F)(F)F)NCC3=CC4=C(O3)CCC4 }}

L-803,087 is a synthetic compound that acts as a potent and selective agonist for the melanocortin receptors, particularly the melanocortin 4 receptor (MC4R). It has been primarily used in scientific research to study the role of MC4R in various physiological processes, including energy homeostasis, sexual function, and cardiovascular regulation.

Pharmacology

L-803,087 is known for its high affinity and selectivity towards the MC4R, which is a G protein-coupled receptor involved in the regulation of appetite and energy balance. Activation of MC4R by L-803,087 has been shown to influence feeding behavior, making it a compound of interest in obesity research.

Mechanism of Action

L-803,087 binds to the MC4R, leading to the activation of adenylate cyclase and an increase in intracellular cyclic AMP (cAMP) levels. This signaling cascade ultimately results in the modulation of neuronal activity that controls appetite and energy expenditure.

Research Applications

L-803,087 has been utilized in various preclinical studies to explore its effects on:

• Appetite Regulation: Studies have demonstrated that L-803,087 can reduce food intake in animal models, suggesting its potential as a therapeutic agent for obesity.
• Sexual Function: Research indicates that MC4R agonists like L-803,087 may enhance sexual arousal and performance, providing insights into treatments for sexual dysfunction.
• Cardiovascular Effects: The compound has been investigated for its role in modulating blood pressure and heart rate, highlighting its potential impact on cardiovascular health.

Safety and Toxicology

While L-803,087 is primarily used in research settings, its safety profile in humans is not well-established. Animal studies have not reported significant adverse effects at research doses, but comprehensive toxicological evaluations are necessary before considering clinical applications.

Also see

• Melanocortin receptor
• Melanocortin 4 receptor
• Obesity
• G protein-coupled receptor