Norbinaltorphimine

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Norbinaltorphimine
Systematic (IUPAC) name
17,17'-(Dicyclopropylmethyl)-6,6',7,7'-6,6'-imino- 7,7'-binorphinan-3,4',14,14'-tetrol
Identifiers
CAS number	105618-26-6
ATC code	?
PubChem	3034416
Chemical data
Formula	C40H43N3O6
Mol. mass	661.784 g/mol
SMILES	eMolecules & PubChem
Synonyms	Norbinaltorphimine, nor-BNI
Pharmacokinetic data
Bioavailability	?
Metabolism	?
Half life	?
Excretion	?
Therapeutic considerations
Pregnancy cat.	?
Legal status
Routes	?

Norbinaltorphimine (nor-BNI) is an opioid antagonist used in scientific research. It is one of the few opioid antagonists available that is highly selective for the κ-opioid receptor, and blocks this receptor without affecting the μ- or δ-opioid receptors,^[1] although it has less selectivity in vivo than when used in isolated tissues.^[2] nor-BNI blocks the effects of kappa agonists in animal models,^[3][4] and produces antidepressant effects.^[5]

[edit] References

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
2. ^ 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
3. ^ 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
4. ^ 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
5. ^ 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. PMID 15312181

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