Norbuprenorfin

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Norbuprenorfin
(IUPAC) ime
(5α,6β,14β,18R)-18-[(1S)-1-hydroxy-1,2,2-trimethylpropyl]-6-methoxy-18,19-dihydro-4,5-epoxy-6,14-ethenomorphinan-3-ol
Klinički podaci
Identifikatori
CAS broj 78715-23-8
ATC kod nije dodeljen
PubChem[1][2] 6426801
ChemSpider[3] 4932224
Hemijski podaci
Formula C25H35NO4 
Mol. masa 413.55 g/mol
SMILES eMolekuli & PubHem
Farmakoinformacioni podaci
Trudnoća ?
Pravni status

Norbuprenorfin je primarni aktivni metabolit buprenorfina. Norbuprenorfin deluje kao pun agonist μ-opioidnog, δ-opioidnog, i nociceptinskog receptora,[4][5] kao i parcijalni agonist κ-opioidnog receptora.[5] Norbuprenorfin prolazi kroz krvno-moždanu barijeru slično buprenorfinu i verovatno doprinosi njegovom dejstvu.[6]

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Literatura[uredi | uredi kod]

  1. Li Q, Cheng T, Wang Y, Bryant SH (2010). „PubChem as a public resource for drug discovery.”. Drug Discov Today 15 (23-24): 1052-7. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519.  edit
  2. Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). „Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities”. Annual Reports in Computational Chemistry 4: 217-241. DOI:10.1016/S1574-1400(08)00012-1. 
  3. Hettne KM, Williams AJ, van Mulligen EM, Kleinjans J, Tkachenko V, Kors JA. (2010). „Automatic vs. manual curation of a multi-source chemical dictionary: the impact on text mining”. J Cheminform 2 (1): 3. DOI:10.1186/1758-2946-2-3. PMID 20331846.  edit
  4. Yassen A, Kan J, Olofsen E, Suidgeest E, Dahan A, Danhof M (May 2007). „Pharmacokinetic-pharmacodynamic modeling of the respiratory depressant effect of norbuprenorphine in rats”. The Journal of Pharmacology and Experimental Therapeutics 321 (2): 598–607. DOI:10.1124/jpet.106.115972. PMID 17283225. 
  5. 5,0 5,1 Huang P, Kehner GB, Cowan A, Liu-Chen LY (May 2001). „Comparison of pharmacological activities of buprenorphine and norbuprenorphine: norbuprenorphine is a potent opioid agonist”. The Journal of Pharmacology and Experimental Therapeutics 297 (2): 688–95. PMID 11303059. 
  6. Jensen ML, Foster D, Upton R, Grant C, Martinez A, Somogyi A (April 2007). „Comparison of cerebral pharmacokinetics of buprenorphine and norbuprenorphine in an in vivo sheep model”. Xenobiotica; the Fate of Foreign Compounds in Biological Systems 37 (4): 441–57. DOI:10.1080/00498250701251126. PMID 17455115. 

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