Deramciclane

Deramciclane has a high affinity for 5-HT_2A and 5-HT_2C receptors; it acts as an antagonist at both receptor subtypes and has inverse agonist properties at the 5-HT_2C receptors without direct stimulatory agonist. IC50 & Target: 5-HT_2A receptor, 5-HT_2C receptor^[1] In Vitro: Deramciclane is a novel anxiolytic agent that binds with high affinity to 5-HT_2A/_2C receptors. The interactions of Deramciclane with the serotonin 5-HT_2C receptor are characterized further using receptor phosphoinositide hydrolysis assays and receptor autoradiography. Deramciclane antagonizes 5-HT_2C receptor mediated 5-HT-stimulated phosphoinositide hydrolysis with an IC₅₀ value of 168 nM. Deramciclane also decreases basal phosphoinositide hydrolysis by up to 33% (EC₅₀= 93 nM) in a physiological system in the choroid plexus, suggesting that Deramciclane possesses inverse agonist properties at this receptor^[1]. In Vivo: Deramciclane 3 and 10 mg/kg does not change the dopamine levels significantly at any time point versus the basal level whereas 30 mg/kg of Deramciclane significantly increases the levels at 40-100 min and at 160-240 min (P<0.05). Deramciclane is a putative antiserotonergic compound that reduces 5-HT-induced phosphoinositol hydrolysis and a variety of actions caused by serotonergic agonists. The receptor binding profile of Deramciclane is rather similar to that of ritanserin. Deramciclane has a high affinity for 5-HT_2A and 5-HT_2C receptors; it acts as an antagonist at both receptor subtypes and has inverse agonist properties at the 5-HT_2C receptors without direct stimulatory agonist effects. Deramciclane has been shown to have anxiolytic-like activity in several animal tests^[2].