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Deramciclane

Catalog No. T10996   CAS 120444-71-5
Synonyms: EGIS-3886

Deramciclane has high affinity for 5-HT2A and 5-HT2C receptors. It acts as an antagonist in both receptor subtypes and has inverse agonist properties for 5-HT2C receptors, but no direct stimulant agonists.

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Deramciclane Chemical Structure
Deramciclane, CAS 120444-71-5
Pack Size Availability Price/USD Quantity
25 mg 6-8 weeks $ 1,080.00
50 mg 6-8 weeks $ 1,410.00
100 mg 6-8 weeks $ 1,990.00
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Biological Description
Chemical Properties
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Description Deramciclane has high affinity for 5-HT2A and 5-HT2C receptors. It acts as an antagonist in both receptor subtypes and has inverse agonist properties for 5-HT2C receptors, but no direct stimulant agonists.
In vitro Deramciclane is a new anti-anxiety drug that can bind to 5-HT2A/2C receptor with high affinity. The interaction between deracixan and serotonin 5-HT2C receptor was further characterized using receptor phosphoinositide hydrolysis assay and receptor autoradiography. Deramciclane antagonizes 5-HT2C receptor-mediated 5-HT stimulated phosphoinositide hydrolysis with IC50 value of 168 nM. In the physiological system of the choroid plexus nervous system, diracic clane can also reduce the hydrolysis of basic inositol phosphate by as much as 33% (EC50 = 93 nM), which indicates that deracic clane has inverse agonism at this receptor Agent properties.
In vivo Compared with basal levels, at any time point, doramamine 3 and 10 mg/kg did not significantly change dopamine levels, while at 40-100 minutes and 160-240 minutes, delamethasone 30 mg/kg was significant Increased dopamine levels (P <0.05). Deramciclane is a putative anti-serotoninergic compound that reduces 5-HT-induced phosphoinositide hydrolysis and multiple effects caused by serotoninergic agonists. The receptor binding curve of Deramciclane is comparable to that of ritanserin. Deramciclane has high affinity for 5-HT2A and 5-HT2C receptors. It acts as an antagonist in both receptor subtypes and has inverse agonist properties for 5-HT2C receptors without direct stimulatory agonist effects. In some animal experiments, deraciciran has been shown to have anxiolytic effects.
Synonyms EGIS-3886
Molecular Weight 301.47
Formula C20H31NO
CAS No. 120444-71-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

TargetMolReferences and Literature

1. P?lvim?ki EP, et al. Deramciclane, a putative anxiolytic drug, is a serotonin 5-HT2C receptor inverse agonist but fails to induce 5-HT2C receptor down-regulation. Psychopharmacology (Berl). 1998 Mar;136(2):99-104. 2. K??ri?inen TM, et al. Comparison of the effects of deramciclane, ritanserin and buspirone on extracellular dopamine and its metabolites in striatum and nucleus accumbens of freely moving rats. Basic Clin Pharmacol Toxicol. 2008 Jan;102(1):50-8.

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Keywords

Deramciclane 120444-71-5 GPCR/G Protein Neuroscience 5-HT Receptor EGIS3886 EGIS-3886 EGIS 3886 inhibitor inhibit

 

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