関: nor-binaltorphimine

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2016/02/26 21:15:47」(JST)

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Norbinaltorphimine (nor-BNI or nBNI) 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 κ-opioid agonists in animal models,^[3]^[4] and produces antidepressant effects.^[5]

References

^ 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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English Journal

Opioid systems in the lateral hypothalamus regulate feeding behavior through orexin and GABA neurons.

Ardianto C1, Yonemochi N1, Yamamoto S1, Yang L1, Takenoya F2, Shioda S3, Nagase H4, Ikeda H5, Kamei J1.
Neuroscience.Neuroscience.2016 Apr 21;320:183-93. doi: 10.1016/j.neuroscience.2016.02.002. Epub 2016 Feb 6.
The hypothalamus controls feeding behavior. Since central opioid systems may regulate feeding behavior, we examined the role of μ-, δ- and κ-opioid receptors in the lateral hypothalamus (LH), the hunger center, in feeding behavior of mice. Non-selective (naloxone; 3mg/kg, s.c.) and selective μ-
PMID 26855191

Two short-acting kappa opioid receptor antagonists (zyklophin and LY2444296) exhibited different behavioral effects from the long-acting antagonist norbinaltorphimine in mouse anxiety tests.

Huang P1, Yakovleva T2, Aldrich JV2, Tunis J1, Parry C1, Liu-Chen LY3.
Neuroscience letters.Neurosci Lett.2016 Feb 26;615:15-20. doi: 10.1016/j.neulet.2016.01.017. Epub 2016 Jan 15.
Prototypical long-acting kappa opioid receptor (KOPR) antagonists [e.g., norbinaltorphimine (norBNI)] have been reported to exert anxiolytic-like effects in several commonly used anxiety tests in rodents including the novelty-induced hypophagia (NIH) and elevated plus maze (EPM) tests. It remains un
PMID 26780565

Determination of sites of U50,488H-promoted phosphorylation of the mouse κ opioid receptor (KOPR): disconnect between KOPR phosphorylation and internalization.

Chen C1, Chiu YT1, Wu W1, Huang P1, Mann A2, Schulz S2, Liu-Chen LY3.
The Biochemical journal.Biochem J.2016 Feb 15;473(4):497-508. doi: 10.1042/BJ20141471. Epub 2015 Dec 3.
Phosphorylation sites of KOPR (κ opioid receptor) following treatment with the selective agonist U50,488H {(-)(trans)-3,4-dichloro-N-methyl-N-[2-(1-pyrrolidiny)cyclo-hexyl]benzeneacetamide} were identified after affinity purification, SDS/PAGE, in-gel digestion with Glu-C and HPLC-MS/MS. Single- an
PMID 26635353

Japanese Journal

コンビナトリアルケミストリーを活用した天然物とその類縁体の高速合成法の開発

有機合成化学協会誌 : JOURNAL OF Synthetic Organic Chemistry JAPAN 65(8), 795-804, 2007-08-01
NAID 10019753608

Gastric Acid Secretion by Central Injection of Dynorphin A-(1-17), an Endogenous Ligand of κ-Opioid Receptor, in Urethane-Anesthetized Rats

The Japanese journal of pharmacology 87(1), 14-20, 2001-09-01
NAID 130000078334

Sensitization of the Adenylyl Cyclase System in Cloned κ-Opioid Receptor-Transfected Cells Following Sustained Agonist Treatment : A Chimeric Study Using G Protein α_<i2>/α_q Subunits

The Japanese journal of pharmacology 81(4), 353-361, 1999-12-01
NAID 10008197587

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「nor-binaltorphimine」

Norbinaltorphimine
Systematic (IUPAC) name
	17,17'-(dicyclopropylmethyl)-6,6',7,7'-6,6'-imino- 7,7'-bimorphinan-3,4',14,14'-tetrol
Identifiers
CAS Number	105618-26-6
ATC code	None
PubChem	CID 3034416
IUPHAR/BPS	1642
ChemSpider	21248347
Chemical data
Formula	C40H43N3O6
Molar mass	661.784 g/mol
	SMILES C1CC1CN2CC[C@]34[C@@H]5C6=C(C[C@]3([C@H]2CC7=C4C(=C(C=C7)O)O5)O)C8=C(N6)[C@H]9[C@@]12CCN([C@@H]([C@@]1(C8)O)CC1=C2C(=C(C=C1)O)O9)CC1CC1 ;
	InChI InChI=1S/C40H43N3O6/c44-25-7-5-21-13-27-39(46)15-23-24-16-40(47)28-14-22-6-8-26(45)34-30(22)38(40,10-12-43(28)18-20-3-4-20)36(49-34)32(24)41-31(23)35-37(39,29(21)33(25)48-35)9-11-42(27)17-19-1-2-19/h5-8,19-20,27-28,35-36,41,44-47H,1-4,9-18H2/t27-,28-,35+,36+,37+,38+,39-,40-/m1/s1 ; Key:APSUXPSYBJVPPS-YAUKWVCOSA-N ;
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