Lefetamine Information
Lefetamine (Santenol) is a drug which is a stimulant and also an analgesic with effects comparable to codeine.
Lefetamine was invented in the 1930s[1] and showed weak analgetic activity.[2]
It was investigated in Japan in 1960. The l-isomere showed weak analgetic action comparable to codeine and antitussive action far weaker than codeine. The d-isomer showed no such activity but caused seizures in rats.[3]
It was abused in Japan during the 1950s. In a small study in 1989 it showed some effect against opioid withdrawal symptoms without causing withdrawal symptoms itself. It was concluded that it may be an opioid partial agonist.[4]
It has been abused in Europe, in 1989 a small study of 15 abusers and some volunteers found, that it had some partial similarity to opioids, that it produced withdrawal symptoms and had dependence and abuse potential to a certain degree.[5]
In a small study in 1994 it was compared to clonidine and buprenorphine for the detoxification of methadone patients and found to be inferior to both for this purpose.[6]
Research
Some related pyrrylphenylethanones had analgetic activity comparable to morphine[7] Some pyrrole analogues were reported to have analgetic effects comparable to lefetamine and being devoid of neurotoxic properties.[8]
See also
References
JP Patent 61 23087
- ^ Thomson; Stevens Journal of the Chemical Society, 1932, p. 1932,1935
- ^ Dodds, E. C.; Lawson, W.; Simpson, S. A.; Williams, P. C. (1945). "Testing diphenylethylamine compounds for analgesic action". The Journal of physiology 104 (1): 47–51. . PMID 16991666. http://www.pubmedcentral.nih.gov/articlerender.fcgi?tool=pmcentrez&artid=1393527.
- ^ Fujimura, H.; Kawai, K. (1960). "Pharmacological Studies on Diphenylalkylamine Derivatives" (pdf). Bulletin of the Institute for Chemical Research, KyotoUniversity 39 (1): 67–77. http://repository.kulib.kyoto-u.ac.jp/dspace/bitstream/2433/75783/1/chd039_1_067.pdf.
- ^ Mannelli, P.; Janiri, L.; De Marinis, M.; Tempesta, E. (1989). "Lefetamine: New abuse of an old drug--clinical evaluation of opioid activity". Drug and alcohol dependence 24 (2): 95–101. doi:10.1016/0376-8716(89)90071-9. PMID 2571492.
- ^ Janiri, L.; Mannelli, P.; Pirrongelli, C.; Lo Monaco, M.; Tempesta, E. (1989). "Lephetamine abuse and dependence: Clinical effects and withdrawal syndrome". British Journal of Addiction 84 (1): 89–95. doi:10.1111/j.1360-0443.1989.tb00555.x. PMID 2917208.
- ^ Janiri, L.; Mannelli, P.; Persico, A. M.; Serretti, A.; Tempesta, E. (1994). "Opiate detoxification of methadone maintenance patients using lefetamine, clonidine and buprenorphine". Drug and alcohol dependence 36 (2): 139–145. doi:10.1016/0376-8716(94)90096-5. PMID 7851281.
- ^ Massa, S.; Di Santo, R.; Mai, A.; Artico, M.; Pantaleoni, G. C.; Giorgi, R.; Coppolino, M. F. (1992). "Pyrrylphenylethanones related to cathinone and lefetamine: Synthesis and pharmacological activities". Archiv der Pharmazie 325 (7): 403–409. PMID 1417455.
- ^ Massa, S.; Stefancich, G.; Artico, M.; Corelli, F.; Silvestri, R.; Pantaleoni, G. C.; Fanini, D.; Palumbo, G. et al (1989). "Synthesis, neuropsychopharmacological effects and analgesic-antiinflammatory activities of pyrrole analogues of lefetamine". Farmaco (Societa chimica italiana : 1989) 44 (9): 763–777. PMID 2604832.
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See also
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Analgesics (N02A, N02B)
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| Opioids
See also: |
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Opium & alkaloids thereof
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Semi-synthetic opium
derivatives
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Synthetic opioids
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| Pyrazolones |
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| Cannabinoids |
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| Anilides |
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| Non-steroidal
anti-inflammatories
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Propionic acid class
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Oxicam class
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Acetic acid class
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COX-2 inhibitors
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Anthranilic acid
(fenamate) class
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Salicylates
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| Atypical, adjuvant and potentiators,
Metabolic agents and miscellaneous |
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Adrenergics
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Receptor ligands
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α1
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- Agonists: 5-FNE
- 6-FNE
- Amidephrine
- Anisodamine
- Anisodine
- Cirazoline
- Dipivefrine
- Dopamine
- Ephedrine
- Epinephrine (Adrenaline)
- Etilefrine
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- Indanidine
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- Methyldopa
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- Naphazoline
- Norepinephrine (Noradrenaline)
- Octopamine
- Oxymetazoline
- Phenylephrine
- Phenylpropanolamine
- Pseudoephedrine
- Synephrine
- Tetrahydrozoline
Antagonists: Abanoquil
- Adimolol
- Ajmalicine
- Alfuzosin
- Amosulalol
- Arotinolol
- Atiprosin
- Benoxathian
- Buflomedil
- Bunazosin
- Carvedilol
- CI-926
- Corynanthine
- Dapiprazole
- DL-017
- Domesticine
- Doxazosin
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- GYKI-12,743
- GYKI-16,084
- Indoramin
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- L-765,314
- Labetalol
- Mephendioxan
- Metazosin
- Monatepil
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- Naftopidil
- Nantenine
- Neldazosin
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- RS-97,078
- SGB-1,534
- Silodosin
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- Spiperone
- Talipexole
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- Tibalosin
- Tiodazosin
- Tipentosin
- Tolazoline
- Trimazosin
- Upidosin
- Urapidil
- Zolertine
* Note that many TCAs, TeCAs, antipsychotics, ergolines, and some piperazines like buspirone, trazodone, nefazodone, etoperidone, and mepiprazole all antagonize α1-adrenergic receptors as well, which contributes to their side effects such as orthostatic hypotension.
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α2
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β
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List of adrenergic drugs
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Dopaminergics
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Receptor ligands
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Agonists
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- Adamantanes: Amantadine
- Memantine
- Rimantadine; Aminotetralins: 7-OH-DPAT
- 8-OH-PBZI
- Rotigotine
- UH-232; Benzazepines: 6-Br-APB
- Fenoldopam
- SKF-38,393
- SKF-77,434
- SKF-81,297
- SKF-82,958
- SKF-83,959; Ergolines: Bromocriptine
- Cabergoline
- Dihydroergocryptine
- Epicriptine
- Lisuride
- LSD
- Pergolide; Dihydrexidine derivatives: 2-OH-NPA
- A-86,929
- Ciladopa
- Dihydrexidine
- Dinapsoline
- Dinoxyline
- Doxanthrine; Others: A-68,930
- A-77636
- A-412,997
- ABT-670
- ABT-724
- Aplindore
- Apomorphine
- Aripiprazole
- Bifeprunox
- BP-897
- CY-208,243
- Dizocilpine
- Etilevodopa
- Flibanserin
- Ketamine
- Melevodopa
- Modafinil
- Pardoprunox
- Phencyclidine
- PD-128,907
- PD-168,077
- PF-219,061
- Piribedil
- Pramipexole
- Propylnorapomorphine
- Pukateine
- Quinagolide
- Quinelorane
- Quinpirole
- RDS-127
- Ro10-5824
- Ropinirole
- Rotigotine
- Roxindole
- Salvinorin A
- SKF-89,145
- Sumanirole
- Terguride
- Umespirone
- WAY-100,635
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Antagonists
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Releasing agents
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- Morpholines: Fenbutrazate
- Morazone
- Phendimetrazine
- Phenmetrazine; Oxazolines: 4-Methylaminorex (4-MAR, 4-MAX)
- Aminorex
- Clominorex
- Cyclazodone
- Fenozolone
- Fluminorex
- Pemoline
- Thozalinone; Phenethylamines (also amphetamines, cathinones, phentermines, etc): 2-Hydroxyphenethylamine (2-OH-PEA)
- 4-CAB
- 4-Methylamphetamine (4-MA)
- 4-Methylmethamphetamine (4-MMA)
- Alfetamine
- Amfecloral
- Amfepentorex
- Amfepramone
- Amphetamine (Dextroamphetamine
- Levoamphetamine)
- Amphetaminil
- β-Methylphenethylamine (β-Me-PEA)
- Benzodioxolylbutanamine (BDB)
- Benzodioxolylhydroxybutanamine (BOH)
- Benzphetamine
- Buphedrone
- Butylone
- Cathine
- Cathinone
- Clobenzorex
- Clortermine
- D-Deprenyl
- Dimethoxyamphetamine (DMA)
- Dimethoxymethamphetamine (DMMA)
- Dimethylamphetamine
- Dimethylcathinone (Dimethylpropion, metamfepramone)
- Ethcathinone (Ethylpropion)
- Ethylamphetamine
- Ethylbenzodioxolylbutanamine (EBDB)
- Ethylone
- Famprofazone
- Fenethylline
- Fenproporex
- Flephedrone
- Fludorex
- Furfenorex
- Hordenine
- Iofetamine
- Lophophine (Homomyristicylamine)
- Mefenorex
- Mephedrone
- Methamphetamine (Desoxyephedrine, Methedrine; Dextromethamphetamine
- Levomethamphetamine)
- Methcathinone (Methylpropion)
- Methedrone
- Methoxymethylenedioxyamphetamine (MMDA)
- Methoxymethylenedioxymethamphetamine (MMDMA)
- Methylbenzodioxolylbutanamine (MBDB)
- Methylenedioxyamphetamine (MDA, tenamfetamine)
- Methylenedioxyethylamphetamine (MDEA)
- Methylenedioxyhydroxyamphetamine (MDOH)
- Methylenedioxymethamphetamine (MDMA)
- Methylenedioxymethylphenethylamine (MDMPEA, homarylamine)
- Methylenedioxyphenethylamine (MDPEA, homopiperonylamine)
- Methylone
- Ortetamine
- Parabromoamphetamine (PBA)
- Parachloroamphetamine (PCA)
- Parafluoroamphetamine (PFA)
- Parafluoromethamphetamine (PFMA)
- Parahydroxyamphetamine (PHA)
- Paraiodoamphetamine (PIA)
- Paredrine (Norpholedrine, Oxamphetamine)
- Phenethylamine (PEA)
- Pholedrine
- Phenpromethamine
- Prenylamine
- Propylamphetamine
- Tiflorex (Flutiorex)
- Tyramine (TRA)
- Xylopropamine
- Zylofuramine; Piperazines: 2,5-Dimethoxy-4-bromobenzylpiperazine (2C-B-BZP)
- Benzylpiperazine (BZP)
- Methoxyphenylpiperazine (MeOPP, paraperazine)
- Methylbenzylpiperazine (MBZP)
- Methylenedioxybenzylpiperazine (MDBZP, piperonylpiperazine); Others: 2-Amino-1,2-dihydronaphthalene (2-ADN)
- 2-Aminoindane (2-AI)
- 2-Aminotetralin (2-AT)
- 4-Benzylpiperidine (4-BP)
- 5-IAI
- Clofenciclan
- Cyclopentamine
- Cypenamine
- Cyprodenate
- Feprosidnine
- Gilutensin
- Heptaminol
- Hexacyclonate
- Indanylaminopropane (IAP)
- Indanorex
- Isometheptene
- Methylhexanamine
- Naphthylaminopropane (NAP)
- Octodrine
- Phthalimidopropiophenone
- Propylhexedrine (Levopropylhexedrine)
- Tuaminoheptane (Tuamine)
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List of dopaminergic drugs
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