Norbinaltorfimin
Izgled
(IUPAC) ime | |||
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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 | ||
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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]
- ↑ 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.
- ↑ 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.
- ↑ 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
- ↑ 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
- ↑ 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
- ↑ 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
- ↑ 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