Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C11H12Cl2N2O.ClH |
| Molecular Weight | 295.593 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 1 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.C[C@@H](OC1=C(Cl)C=CC=C1Cl)C2=NCCN2
InChI
InChIKey=DWWHMKBNNNZGHF-OGFXRTJISA-N
InChI=1S/C11H12Cl2N2O.ClH/c1-7(11-14-5-6-15-11)16-10-8(12)3-2-4-9(10)13;/h2-4,7H,5-6H2,1H3,(H,14,15);1H/t7-;/m1./s1
DescriptionCurator's Comment: description was created based on several sources, including
https://pharm.reviews/images/statyi/british-national-formulary-2015.pdf | https://www.ncbi.nlm.nih.gov/pubmed/2879913 | https://www.drugbank.ca/drugs/DB04948
Curator's Comment: description was created based on several sources, including
https://pharm.reviews/images/statyi/british-national-formulary-2015.pdf | https://www.ncbi.nlm.nih.gov/pubmed/2879913 | https://www.drugbank.ca/drugs/DB04948
Levlofexidine is R-enantiomer of a α2A adrenergic receptor agonist Lofexidine. Levlofexidine (as a component of Lofexidine) can be used as a short-acting anti-hypertensive but is mostly used to help relieve symptoms of heroin or opiate withdrawal in opiate dependency. Lofexidine is approved in the United Kingdom but is still undergoing clinical trials in the United States. Levlofexidine showed an approximately 9-fold higher affinity than Dexlofexidine for the alpha 2-adrenoceptor-like binding sites in rat brain membranes identified by [3H]-clonidine and was 4 times more potent at displacing [3H]-prazosin from alpha 1-adrenoceptors. The possibility of using lofexidine to treat alcohol addiction withdrawal symptoms has been investigated and has not yet been shown to be an effective treatment.
Originator
Approval Year
Sample Use Guides
Initially 800 micrograms lofexidine (400 mkg Levlofexidine+400mkg Dexlofexidine) daily in divided doses, increased in steps of 400–800 micrograms daily (max. per dose 800 micrograms) as required for 7–10 days if no opioid use (but longer may be required); maximum 2.4 mg per day
Route of Administration:
Oral
Rats were decapitated, and the brains, without cerebella, were rapidly removed and stored at -20 C until use. One frozen brain (1.5 g) was homogenized in 20 vol (w/v) of 0.05 mol/L Tris.HC1 buffer (pH 7.7 at 25 "C) by using a glass homogenizer with a Teflon pestle and centrifuged twice at 48000g for 10 min at 4 C. The supernatant was discarded and the resulting pellet was resuspended in 100 mL of ice-cold buffer. In the standard binding assay 1-mL aliquots of the crude membrane homogenate were incubated together with 20 pL of [3H]clonidine (final concentration 2.5 nmol/L) and 50 WL of increasing concentrations of the Levlofexidine at 25 C for 45 min. The incubation was terminated by filtration with Whatman GF/B glass fiber filters.
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87038-06-0
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44249499
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M10T82Q9C1
Created by
admin on Sat Dec 16 11:11:38 GMT 2023 , Edited by admin on Sat Dec 16 11:11:38 GMT 2023
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PARENT (SALT/SOLVATE)
SUBSTANCE RECORD
