Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C20H31NO.C4H4O4 |
| Molecular Weight | 417.5384 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 3 / 3 |
| E/Z Centers | 1 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
OC(=O)\C=C\C(O)=O.[H][C@]12CC[C@](C)(C1(C)C)[C@@](C2)(OCCN(C)C)C3=CC=CC=C3
InChI
InChIKey=RFQWRWCCNQNACG-HJYQBBATSA-N
InChI=1S/C20H31NO.C4H4O4/c1-18(2)17-11-12-19(18,3)20(15-17,22-14-13-21(4)5)16-9-7-6-8-10-16;5-3(6)1-2-4(7)8/h6-10,17H,11-15H2,1-5H3;1-2H,(H,5,6)(H,7,8)/b;2-1+/t17-,19-,20+;/m1./s1
| Molecular Formula | C4H4O4 |
| Molecular Weight | 116.0722 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 1 |
| Optical Activity | NONE |
| Molecular Formula | C20H31NO |
| Molecular Weight | 301.4662 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 3 / 3 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
Deramciclane is camphor derivative. It is an anxiolytic agent that binds with high affinity to 5-HT2A/2C receptor. Deramciclane showed significant evidence of efficacy for the treatment of generalized anxiety disorder in adult patients. A single dose of deramciclane was rapidly absorbed with peak plasma concentrations being reached after about 3 h. Deramciclane has a half-life of around 27 h. The most commonly reported adverse event was headache. In the in vitro studies deramciclane concentration-dependently inhibited NMDA evoked spreading depression.
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| Deramciclane (Egis). | 2002 Feb |
|
| Studies of the side chain cleavage of deramciclane in rats with radiolabelled compounds. | 2002 Mar |
|
| In vitro simulation of food effect on dissolution of deramciclane film-coated tablets and correlation with in vivo data in healthy volunteers. | 2002 Mar |
|
| Pharmacokinetics of deramciclane, a novel anxiolytic agent, after intravenous and oral administration. | 2003 |
|
| Effect of the novel anxiolytic drug deramciclane on the pharmacokinetics and pharmacodynamics of the CYP3A4 probe drug buspirone. | 2003 Dec |
|
| The effect of oil as a dietary component on in vitro dissolution of an acid-labile drug. | 2003 Jul |
|
| Comparison of deramciclane to benzodiazepine agonists in behavioural activity of mice and in alcohol drinking of alcohol-preferring rats. | 2004 Apr |
|
| Pharmacokinetics of deramciclane and N-desmethylderamciclane after single and repeated oral doses in healthy volunteers. | 2004 Aug |
|
| Effect of the novel anxiolytic drug deramciclane on cytochrome P(450) 2D6 activity as measured by desipramine pharmacokinetics. | 2004 Feb |
|
| Influence of food on the oral bioavailability of deramciclane from film-coated tablet in healthy male volunteers. | 2004 Nov |
|
| Deramciclane in the treatment of generalized anxiety disorder: a placebo-controlled, double-blind, dose-finding study. | 2005 Dec |
|
| Biotransformation of deramciclane in primary hepatocytes of rat, mouse, rabbit, dog, and human. | 2005 Nov |
|
| Role of CYP2E1 in deramciclane metabolism. | 2005 Nov |
|
| Comparison of the effects of deramciclane, ritanserin and buspirone on extracellular dopamine and its metabolites in striatum and nucleus accumbens of freely moving rats. | 2008 Jan |
|
| Deramciclane improves object recognition in rats: potential role of NMDA receptors. | 2010 Feb |
|
| Selective binding interactions of deramciclane to the genetic variants of human alpha(1)-acid glycoprotein. | 2010 Mar |
Patents
| Substance Class |
Chemical
Created
by
admin
on
Edited
Fri Dec 15 15:25:41 GMT 2023
by
admin
on
Fri Dec 15 15:25:41 GMT 2023
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| Record UNII |
W1183TY0EE
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| Record Status |
Validated (UNII)
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| Record Version |
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m4186
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ACTIVE MOIETY |
