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HomeProduct name listDERAMCICLANE

DERAMCICLANE

DERAMCICLANE Structural

What is DERAMCICLANE?

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 further characterized 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

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 < /sub> receptors without direct stimulatory agonist effects. Deramciclane has been shown to have anxiolytic-like activity in several animal tests.

Properties of DERAMCICLANE

Boiling point: 375.2±25.0 °C(Predicted)
Density  1.01±0.1 g/cm3(Predicted)
storage temp.  Store at -20°C
solubility  Soluble in DMSO
form  Oil
pka pKa 9.61±0.03(H2O t=25±0.1 I=0.1(NaCl)) (Uncertain)
color  Light yellow to yellow

Safety information for DERAMCICLANE

Computed Descriptors for DERAMCICLANE

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