| 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
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
PubMed
Patents
Sample Use Guides
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
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.
ACTIVE MOIETY
SALT/SOLVATE (PARENT)
