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Chemical Compound Review

Orlaam     [(3S,6S)-6-dimethylamino-4,4- diphenyl...

Synonyms: LAAM, Levomethadyl, CHEMBL1514, SureCN93805, CHEBI:6441, ...
 
 
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Disease relevance of levo-alpha-Acetylmethadol

 

Psychiatry related information on levo-alpha-Acetylmethadol

 

High impact information on levo-alpha-Acetylmethadol

 

Chemical compound and disease context of levo-alpha-Acetylmethadol

 

Biological context of levo-alpha-Acetylmethadol

 

Anatomical context of levo-alpha-Acetylmethadol

 

Associations of levo-alpha-Acetylmethadol with other chemical compounds

 

Gene context of levo-alpha-Acetylmethadol

  • The ratio [dinor-LAAM/(nor-LAAM plus dinor-LAAM)] with microsomes and CYP3A4 decreased with increasing LAAM concentration, suggesting most dinor-LAAM is formed from released nor-LAAM that subsequently reassociates with CYP3A4 [23].
  • Of the cDNA-expressed isoforms examined, CYP2B6 and 3A4 had the highest activity toward LAAM and nor-LAAM at both low (2 microM) and high (250 microM) substrate concentrations [23].
  • 3. Using patch clamp electrophysiology, we found that l-alpha-acetylmethadol inhibited HERG channel currents in a voltage-dependent manner displaying an IC(50) value of 3 microM [31].
  • The major active metabolite of l-alpha-acetylmethadol, noracetylmethadol, inhibited HERG with an estimated IC(50) values of 12 microM. l-alpha-acetylmethadol had little or no effect on Kv4.3 or KvLQT1/minK K(+) channel currents at concentration up to 10 microM [31].
  • Hepatic and intestinal microsomal N-demethylation in vitro is catalysed mainly by cytochrome P450 (CYP) 3A4; however, the role of CYP3A in LAAM disposition in humans in vivo is unknown [2].
 

Analytical, diagnostic and therapeutic context of levo-alpha-Acetylmethadol

References

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  21. Transfer of L-alpha-acetylmethadol (LAAM) and L-alpha-acetyl-N-normethadol (norLAAM) by the perfused human placental lobule. Nanovskaya, T.N., Deshmukh, S.V., Miles, R., Burmaster, S., Ahmed, M.S. J. Pharmacol. Exp. Ther. (2003) [Pubmed]
  22. Physiological disposition and biotransformation of l-alpha-[2-3H]acetylmethadol (LAAM) in acutely and chronically treated monkeys. Misra, A.L., Mulé, S.J., Bloch, R., Bates, T.R. J. Pharmacol. Exp. Ther. (1978) [Pubmed]
  23. Metabolism of levo-alpha-Acetylmethadol (LAAM) by human liver cytochrome P450: involvement of CYP3A4 characterized by atypical kinetics with two binding sites. Oda, Y., Kharasch, E.D. J. Pharmacol. Exp. Ther. (2001) [Pubmed]
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  29. Efficacy of dose and contingency management procedures in LAAM-maintained cocaine-dependent patients. Oliveto, A., Poling, J., Sevarino, K.A., Gonsai, K.R., McCance-Katz, E.F., Stine, S.M., Kosten, T.R. Drug and alcohol dependence. (2005) [Pubmed]
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