Norbinaltorfimin
Из Википедије, слободне енциклопедије
| (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 |
| PubHem | 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.[1] although On je manje selektivan in vivo nego kad se koristi u izolovanim tkivima.[2] nor-BNI blokira efekte kapa agonista u životinjskim modelima,[3][4] i proizvodi antidepresantske efekte.[5]
Vidi još [уреди]
Literatura [уреди]
- ^ 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
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