Norbinaltorfimin

Из Википедије, слободне енциклопедије
Norbinaltorfimin
(IUPAC) ime
17,17'-(dicyclopropylmethyl)-6,6',7,7'-6,6'-imino- 7,7'-binorphinan-3,4',14,14'-tetrol
Klinički podaci
Identifikatori
CAS broj 105618-26-6
ATC kod nije dodeljen
PubChem[1][2] 3034416
Hemijski podaci
Formula C40H43N3O6 
Mol. masa 661.784 g/mol
SMILES eMolekuli & PubHem
Farmakoinformacioni podaci
Trudnoća  ?
Pravni status

Norbinaltorphimin (nor-BNI) je opioidni antagonist koji se koristi u naučnim istraživanjima. On je jedan od malobrojnih dostupnih opioidnih antagonista koji su visoko selektivni za κ-opioidni receptor, i blokiraju taj receptor bez uticaja na μ- ili δ-opioidni receptor.[3] although On je manje selektivan in vivo nego kad se koristi u izolovanim tkivima.[4] nor-BNI blokira efekte kapa agonista u životinjskim modelima,[5][6] i proizvodi antidepresantske efekte.[7]

Vidi još[уреди]

Literatura[уреди]

  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. ^ Portoghese PS, Lipkowski AW, Takemori AE. Binaltorphimine and nor-binaltorphimine, potent and selective kappa-opioid receptor antagonists. Life Sciences. 1987 Mar 30;40(13):1287-92. PMID 2882399
  4. ^ Birch PJ, Hayes AG, Sheehan MJ, Tyers MB. Norbinaltorphimine: antagonist profile at kappa opioid receptors. European Journal of Pharmacology. 1987 Dec 15;144(3):405-8. PMID 2831070
  5. ^ Takemori AE, Ho BY, Naeseth JS, Portoghese PS. Nor-binaltorphimine, a highly selective kappa-opioid antagonist in analgesic and receptor binding assays. Journal of Pharmacology and Experimental Therapeutics. 1988 Jul;246(1):255-8. PMID 2839664
  6. ^ Takemori AE, Schwartz MM, Portoghese PS. Suppression by nor-binaltorphimine of kappa opioid-mediated diuresis in rats. Journal of Pharmacology and Experimental Therapeutics. 1988 Dec;247(3):971-4. PMID 2849679
  7. ^ Shirayama Y, Ishida H, Iwata M, Hazama GI, Kawahara R, Duman RS. Stress increases dynorphin immunoreactivity in limbic brain regions and dynorphin antagonism produces antidepressant-like effects. Journal of Neurochemistry. 2004 Sep;90(5):1258-68. DOI 10.1111/j.1471-4159.2004.02589.x} PMID 15312181

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