| 词条 | Lefetamine |
| 释义 |
| Verifiedfields = changed | Watchedfields = changed | verifiedrevid = 464370579 | IUPAC_name = (1R)-N,N-dimethyl-1,2-diphenylethanamine | image = Lefetamine.svg | image2 = Lefetamine3d.png | width2 = 160 | tradename = | pregnancy_category = | legal_AU = S4 | legal_CA = Schedule III | legal_US = Schedule IV | legal_UK = Class B | legal_DE = Anlage I | routes_of_administration = Oral | bioavailability = | metabolism = | elimination_half-life = | excretion = | CAS_number_Ref = {{cascite|changed|??}} | CAS_number = 7262-75-1 | ATC_prefix = none | ATC_suffix = | PubChem = 443970 | ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}} | ChemSpiderID = 392017 | UNII_Ref = {{fdacite|correct|FDA}} | UNII = 4J9726V5Y9 | C=16 | H=19 | N=1 | molecular_weight = 225.329 g/mol | smiles = CN([C@@H](C1=CC=CC=C1)CC2=CC=CC=C2)C | StdInChI_Ref = {{stdinchicite|correct|chemspider}} | StdInChI = 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 | StdInChIKey_Ref = {{stdinchicite|correct|chemspider}} | StdInChIKey = YEJZJVJJPVZXGX-MRXNPFEDSA-N }} Lefetamine (Santenol) is a drug which is a stimulant and also an analgesic with effects comparable to codeine. Lefetamine-related 1,2-diphenylethylamines were invented in the 1940s and showed weak analgesic activity.[1] It was investigated in Japan in 1950s.[2] The l-isomer showed weak analgesic action comparable to codeine and antitussive action far weaker than codeine. The d-isomer showed no such activity but caused seizures in rats.[3][4] 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.[5] 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.[6] In a small study in 1994, it was compared to clonidine and buprenorphine in the detoxification of methadone patients and found to be inferior to both of them.[7] Regulation may vary; it does not appear as either a Narcotic or Non-Narcotic under the US Controlled Substances Act 1970 [8] The Canadian Controlled Drugs and Substances Act was amended in 2016 to include the substance as a Schedule III substance. Possession without legal authority can result in maximum 3 years imprisonment. Further, Health Canada amended the Food and Drug Regulations in May, 2016 to classify Lefetamine as a controlled drug.[9] ResearchSome related pyrrylphenylethanones had analgetic activity comparable to morphine.[10] Some pyrrole analogues were reported to have analgesic effects comparable to lefetamine and being devoid of neurotoxic properties.[11] See also
References1. ^{{Cite journal | last1 = Dodds | first1 = E. C. | last2 = Lawson | first2 = W. | last3 = Simpson | first3 = S. A. | last4 = Williams | first4 = P. C. | title = Testing Diphenylethylamine Compounds for Analgesic Action | journal = The Journal of Physiology | volume = 104 | issue = 1 | pages = 47–51 | year = 1945 | pmid = 16991666 | pmc = 1393527| url = https://www.ncbi.nlm.nih.gov/pmc/articles/PMC1393527/pdf/jphysiol01495-0059.pdf| format = pdf | doi=10.1113/jphysiol.1945.sp004105}} {{Stimulants}}{{Analgesics}}{{Monoamine reuptake inhibitors}}{{Opioid receptor modulators}}{{Phenethylamines}}2. ^{{ cite patent | country = DE | status = patent | number = 1159958 | title = Verfahren zur Herstellung von antitussiv wirksamem l-1,2-Diphenyl-1-dimethylaminoaethan und dessen Salzen | gdate = 1963-12-27 | inventor = Ogyu, K.; Fujimura H.; Yamakawa Y.; Mita I. | assign1 = Institut Seikatsu Kagaku Kenkyusho (Scientific Research Institute for Practical Life, Kyoto) }} 3. ^{{ cite journal | last1 = Fujimura | first1 = H. | last2 = Kawai | first2 = K. | title = Pharmacological Studies on Diphenylalkylamine Derivatives. (I) | journal = Bulletin of the Institute for Chemical Research, Kyoto University | year = 1961 | volume = 39 | issue = 1 | pages = 67–77 | url = http://repository.kulib.kyoto-u.ac.jp/dspace/bitstream/2433/75783/1/chd039_1_067.pdf | format = pdf }} 4. ^{{ cite journal | last1 = Fujimura | first1 = H. | last2 = Kawai | first2 = K. | last3 = Ohata | first3 = K. | last4 = Shibata | first4 = S. | title = Pharmacological Studies on Diphenylalkylamine Derivatives. (II): On the Actions of l-1,2-Diphenyl-1-dimethylaminoethane Hydrochloride (SPA) | journal = Bulletin of the Institute for Chemical Research, Kyoto University | year = 1961 | volume = 39 | issue = 1 | pages = 78–94 | url = http://repository.kulib.kyoto-u.ac.jp/dspace/bitstream/2433/75782/1/chd039_1_078.pdf | format = pdf }} 5. ^{{Cite journal | last1 = Mannelli | first1 = P. | last2 = Janiri | first2 = L. | last3 = de Marinis | first3 = M. | last4 = Tempesta | first4 = E. | title = Lefetamine: New Abuse of an Old Drug -- Clinical Evaluation of Opioid Activity | journal = Drug and Alcohol Dependence | volume = 24 | issue = 2 | pages = 95–101 | year = 1989 | pmid = 2571492 | doi=10.1016/0376-8716(89)90071-9}} 6. ^{{Cite journal | doi = 10.1111/j.1360-0443.1989.tb00555.x | last1 = Janiri | first1 = L. | last2 = Mannelli | first2 = P. | last3 = Pirrongelli | first3 = C. | last4 = lo Monaco | first4 = M. | last5 = Tempesta | first5 = E. | title = Lephetamine Abuse and Dependence: Clinical Effects and Withdrawal Syndrome | journal = British Journal of Addiction | volume = 84 | issue = 1 | pages = 89–95 | year = 1989 | pmid = 2917208}} 7. ^{{Cite journal | doi = 10.1016/0376-8716(94)90096-5 | last1 = Janiri | first1 = L. | last2 = Mannelli | first2 = P. | last3 = Persico | first3 = A. M. | last4 = Serretti | first4 = A. | last5 = Tempesta | first5 = E. | title = Opiate Detoxification of Methadone Maintenance Patients Using Lefetamine, Clonidine and Buprenorphine | journal = Drug and Alcohol Dependence | volume = 36 | issue = 2 | pages = 139–145 | year = 1994 | pmid = 7851281}} 8. ^http://www.deadiversion.usdoj.gov/quotas/conv_factor/index.html 9. ^Regulations Amending the Food and Drug Regulations (Parts G and J — Lefetamine, AH-7921, MT-45 and W-18) 10. ^{{Cite journal | last1 = Massa | first1 = S. | last2 = di Santo | first2 = R. | last3 = Mai | first3 = A. | last4 = Artico | first4 = M. | last5 = Pantaleoni | first5 = G. C. | last6 = Giorgi | first6 = R. | last7 = Coppolino | first7 = M. F. | title = Pyrrylphenylethanones Related to Cathinone and Lefetamine: Synthesis and Pharmacological Activities | journal = Archiv der Pharmazie | volume = 325 | issue = 7 | pages = 403–409 | year = 1992 | pmid = 1417455 | doi = 10.1002/ardp.19923250707}} 11. ^{{Cite journal | last1 = Massa | first1 = S. | last2 = Stefancich | first2 = G. | last3 = Artico | first3 = M. | last4 = Corelli | first4 = F. | last5 = Silvestri | first5 = R. | last6 = Pantaleoni | first6 = G. C. | last7 = Fanini | first7 = D. | last8 = Palumbo | first8 = G. | last9 = Giorgi | first9 = R. | title = Synthesis, Neuropsychopharmacological Effects and Analgesic-Antiinflammatory Activities of Pyrrole Analogues of Lefetamine | journal = Farmaco | publisher = Societa Chimica Italiana | volume = 44 | issue = 9 | pages = 763–777 | year = 1989 | pmid = 2604832}} 5 : Norepinephrine-dopamine reuptake inhibitors|Stimulants|Phenethylamines|Mu-opioid agonists|Diarylethylamines |
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