Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C16H19N |
Molecular Weight | 225.3288 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 1 / 1 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CN(C)[C@H](CC1=CC=CC=C1)C2=CC=CC=C2
InChI
InChIKey=YEJZJVJJPVZXGX-MRXNPFEDSA-N
InChI=1S/C16H19N/c1-17(2)16(15-11-7-4-8-12-15)13-14-9-5-3-6-10-14/h3-12,16H,13H2,1-2H3/t16-/m1/s1
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/2571492Curator's Comment: description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/16991666 | https://www.ncbi.nlm.nih.gov/pubmed/26276083 | https://www.ncbi.nlm.nih.gov/pubmed/1417455
Sources: https://www.ncbi.nlm.nih.gov/pubmed/2571492
Curator's Comment: description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/16991666 | https://www.ncbi.nlm.nih.gov/pubmed/26276083 | https://www.ncbi.nlm.nih.gov/pubmed/1417455
Lefetamine (L-SPA; L-1,2-diphenyl-l-dimethylaminoethane hydrochloride) is a synthetic compound with analgesic and anti-inflammatory action, introduced in clinical practice in Italy and Japan as ‘Santenol’. Santenol is available for oral (50 mg tablets1 and intramuscular (60 mg vials containing also lidocainel use. Animal studies have shown an analgesic effect and changes in EEG activity and O2 consumption of the nervous tissue. Lefetamine may be an opioid partial agonist. Lefetamine was first marketed in the 1940s as an opioid analgesic. Since withdrawal symptoms were observed during treatment, it became a controlled substance.
CNS Activity
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
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Target ID: CHEMBL233 Sources: https://www.ncbi.nlm.nih.gov/pubmed/2571492 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
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Primary | Unknown Approved UseUnknown |
PubMed
Title | Date | PubMed |
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Treatment of polydrug-using opiate dependents during withdrawal: towards a standardisation of treatment. | 2006 Nov 15 |
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Toxicokinetics of lefetamine and derived diphenylethylamine designer drugs-Contribution of human cytochrome P450 isozymes to their main phase I metabolic steps. | 2015 Nov 4 |
Patents
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/2571492
In clinical trial patients were assigned to lefetamine treatment programme.
After stabilization on admission with a sufficient lefetamine dosage (mean 450 mg/day) five of them underwent a progressive lefetamine withdrawal with increasing sedative-antimanic therapy (neuroleptics such as levopromazine, chlorpromazine or sodium valproatel.
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/26276083
Incubation mixtures (final volume: 50 mkL) consisted of 90 mM phosphate buffer (pH 7.4), 5 mM Mg2+, 5 mM isocitrate, 1.2 mM NADP+, 0.5 U/mL isocitrate dehydrogenase, 200 U/mL superoxide dismutase, liver enzymes and the LEFETAMINE (up to 1000mkM), diluted in the phosphate buffer. Reactions were started by addition of the ice-cold microsomes and
stopped with 50 mkL of an ice-cold mixture of acetonitrile, containing the IS (diphenhydramine, 10 mkM). The solutions were centrifuged for 2 min at 14,000 x g, 50 mkL of the supernatant was transferred to an autosampler vial and injected onto the LC–MSn system.
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Classification Tree | Code System | Code | ||
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NCI_THESAURUS |
C241
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DEA NO. |
1635
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3457
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DTXSID7046833
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m1201
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LEFETAMINE
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100000082585
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C81381
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7262-75-1
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3316
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CHEMBL2106355
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4J9726V5Y9
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SUB08423MIG
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443970
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C011896
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ACTIVE MOIETY
SALT/SOLVATE (PARENT)