| 词条 | Norbuprenorphine |
| 释义 |
| IUPAC_name = (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 | image = Norbuprenorphine.png | tradename = | pregnancy_category = | legal_status = | routes_of_administration = | bioavailability = | protein_bound = | metabolism = | elimination_half-life = | excretion = | CAS_number = 78715-23-8 | ATC_prefix = None | ATC_suffix = | PubChem = 114976 | ChemSpiderID = 102911 | C=25 | H=35 | N=1 | O=4 | molecular_weight = 413.55 g/mol | smiles = C[C@]([C@H]1C[C@@]23CC[C@@]1([C@H]4[C@@]25CCN[C@@H]3Cc6c5c(c(cc6)O)O4)OC)(C(C)(C)C)O | StdInChI = 1S/C25H35NO4/c1-21(2,3)22(4,28)16-13-23-8-9-25(16,29-5)20-24(23)10-11-26-17(23)12-14-6-7-15(27)19(30-20)18(14)24/h6-7,16-17,20,26-28H,8-13H2,1-5H3/t16-,17-,20-,22+,23-,24+,25-/m1/s1 | StdInChIKey = YOYLLRBMGQRFTN-IOMBULRVSA-N }}Norbuprenorphine is a major active metabolite of the opioid modulator buprenorphine. It is a μ-opioid, δ-opioid, and nociceptin receptor full agonist,[1][2] and a κ-opioid receptor partial agonist.[2] In rats, unlike buprenorphine, norbuprenorphine produces marked respiratory depression but with very little antinociceptive effect.[3] In explanation of these properties, norbuprenorphine has been found to be a high affinity P-glycoprotein substrate, and in accordance, shows very limited blood-brain-barrier penetration.[3] See also
References1. ^{{cite journal |vauthors=Yassen A, Kan J, Olofsen E, Suidgeest E, Dahan A, Danhof M | title = Pharmacokinetic-pharmacodynamic modeling of the respiratory depressant effect of norbuprenorphine in rats | journal = The Journal of Pharmacology and Experimental Therapeutics | volume = 321 | issue = 2 | pages = 598–607 |date=May 2007 | pmid = 17283225| doi = 10.1124/jpet.106.115972 | url = http://jpet.aspetjournals.org/cgi/pmidlookup?view=long&pmid=17283225}} {{Opioid receptor modulators}}{{nervous-system-drug-stub}}2. ^1 {{cite journal |vauthors=Huang P, Kehner GB, Cowan A, Liu-Chen LY | title = Comparison of pharmacological activities of buprenorphine and norbuprenorphine: norbuprenorphine is a potent opioid agonist | journal = The Journal of Pharmacology and Experimental Therapeutics | volume = 297 | issue = 2 | pages = 688–95 |date=May 2001 | pmid = 11303059 | doi = | url = http://jpet.aspetjournals.org/cgi/pmidlookup?view=long&pmid=11303059}} 3. ^1 {{cite journal |vauthors=Brown SM, Campbell SD, Crafford A, Regina KJ, Holtzman MJ, Kharasch ED | title = P-glycoprotein is a major determinant of norbuprenorphine brain exposure and antinociception | journal = J. Pharmacol. Exp. Ther. | volume = 343 | issue = 1 | pages = 53–61 |date=October 2012 | pmid = 22739506 | pmc = 3464040 | doi = 10.1124/jpet.112.193433 | url = http://jpet.aspetjournals.org/cgi/pmidlookup?view=long&pmid=22739506}} 10 : Morphinans|Phenols|Alcohols|Ethers|Kappa agonists|Mu-opioid agonists|Delta-opioid agonists|Nociceptin receptor agonists|Opioid metabolites|Peripherally selective drugs |
| 随便看 |
|
开放百科全书收录14589846条英语、德语、日语等多语种百科知识，基本涵盖了大多数领域的百科知识，是一部内容自由、开放的电子版国际百科全书。