Norbuprenorfin je primarni aktivni metabolit buprenorfina. Norbuprenorfin deluje kao pun agonist μ-opioidnog, δ-opioidnog, i nociceptinskog receptora,[1][2] kao i parcijalni agonist κ-opioidnog receptora.[2] Norbuprenorfin prolazi kroz krvno-moždanu barijeru slično buprenorfinu i verovatno doprinosi njegovom dejstvu.[3]

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
Identifikatori
CAS broj78715-23-8 ДаY
ATC kodnone
PubChemCID 6426801
ChemSpider4932224
Hemijski podaci
FormulaC25H35NO4
Molarna masa413.55 g/mol
  • CC(C)(C)C(C)(C1CC23CCC1 (C4C25CCNC3CC6=C5C(=C(C=C6)O)O4)OC)O

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Literatura

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  1. ^ Yassen A, Kan J, Olofsen E, Suidgeest E, Dahan A, Danhof M (2007). „Pharmacokinetic-pharmacodynamic modeling of the respiratory depressant effect of norbuprenorphine in rats”. The Journal of Pharmacology and Experimental Therapeutics. 321 (2): 598—607. PMID 17283225. doi:10.1124/jpet.106.115972. 
  2. ^ а б Huang P, Kehner GB, Cowan A, Liu-Chen LY (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. 
  3. ^ Jensen ML, Foster D, Upton R, Grant C, Martinez A, Somogyi A (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. PMID 17455115. doi:10.1080/00498250701251126. 

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