CSP-2503 explained

CSP-2503 is a potent and selective 5-HT_1A receptor agonist, 5-HT_2A receptor antagonist, and 5-HT₃ receptor antagonist of the naphthylpiperazine class.^[1] First synthesized in 2003, it was designed based on computational models and QSAR studies.^{[2] [3]} In rat studies, CSP-2503 has demonstrated anxiolytic effects, and thus has been suggested as a treatment for anxiety in humans with a multimodal mechanism of action.^[1]

See also

• Naphthylpiperazine
• S-14,671
• S-14,506

Notes and References

1. Delgado M, Caicoya AG, Greciano V . Anxiolytic-like effect of a serotonergic ligand with high affinity for 5-HT1A, 5-HT2A and 5-HT3 receptors . European Journal of Pharmacology . 511 . 1 . 9–19 . March 2005 . 15777774 . 10.1016/j.ejphar.2005.01.032 . etal.
2. López-Rodríguez ML, Morcillo MJ, Fernández E . Design and synthesis of S-(−)-2-4-(napht-1-yl)piperazin-1-ylmethyl]-1,4-dioxoperhydropyrrolo[1,2-a]pyrazine (CSP-2503) using computational simulation. A 5-HT1A receptor agonist . Bioorganic & Medicinal Chemistry Letters . 13 . 8 . 1429–32 . April 2003 . 12668005 . 10.1016/S0960-894X(03)00160-4. etal.
3. López-Rodríguez ML, Morcillo MJ, Fernández E . Synthesis and structure-activity relationships of a new model of arylpiperazines. 8. Computational simulation of ligand-receptor interaction of 5-HT(1A)R agonists with selectivity over alpha1-adrenoceptors . Journal of Medicinal Chemistry . 48 . 7 . 2548–58 . April 2005 . 15801844 . 10.1021/jm048999e . etal.