Molecular Formula | C20H31NO |
Molar Mass | 301.47 |
Density | 1.01±0.1 g/cm3(Predicted) |
Boling Point | 375.2±25.0 °C(Predicted) |
pKa | pKa 9.61±0.03(H2O t=25±0.1 I=0.1(NaCl)) (Uncertain) |
Storage Condition | Room Temprature |
In vitro study | 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 IC 50 value of 168 nM. Deramciclane also decreases basal phosphoinositide hydrolysis by up to 33% (EC 50 = 93 nM) in a physiological system in the choroid plexus, suggesting that Deramciclane possesses inverse agonist properties at this receptor. |
In vivo study | 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. |
biological activity | Deramciclane has high affinity for 5-HT2A and 5-HT2C receptors. Deramciclane, as an antagonist of two receptor subtypes, has inverse agonist properties at the 5-HT2C receptor and no direct stimulating agonist. |