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出典(authority):フリー百科事典『ウィキペディア(Wikipedia)』「2016/02/15 21:49:06」(JST)
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Binaltorphimine
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Systematic (IUPAC) name |
(1S,2S,7S,8S,12R,20R,24R,32R)-11,33-bis(cyclopropylmethyl)-22-methyl-19,25-dioxa-11,22,33-triazaundecacyclo[24.9.1.18,14.01,24.02,32.04,23.05,21.07,12.08,20.018,37.030,36]heptatriaconta-4(23),5(21),14(37),15,17,26(36),27,29-octaene-2,7,17,27-tetrol
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Identifiers |
CAS Number |
105618-27-7 |
ATC code |
None |
PubChem |
CID 5484197 |
ChemSpider |
4588407 |
Chemical data |
Formula |
C41H45N3O6 |
Molar mass |
675.813 g/mol |
SMILES
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O[C@@]57Cc1c%11c(n(c1[C@@H]6Oc2c4c(ccc2O)C[C@H]7N(CC3CC3)CC[C@@]456)C)[C@@H]%12Oc8c9c(ccc8O)C[C@H]%10N(CC[C@]9%12[C@@]%10(O)C%11)CC%13CC%13
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InChI
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InChI=1S/C41H45N3O6/c1-42-32-24(16-40(47)28-14-22-6-8-26(45)34-30(22)38(40,36(32)49-34)10-12-43(28)18-20-2-3-20)25-17-41(48)29-15-23-7-9-27(46)35-31(23)39(41,37(50-35)33(25)42)11-13-44(29)19-21-4-5-21/h6-9,20-21,28-29,36-37,45-48H,2-5,10-19H2,1H3/t28-,29+,36-,37-,38-,39-,40+,41+/m0/s1
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Key:DKIVQMBUHVYDFC-KMALJSJFSA-N
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Binaltorphimine (BNI) is a selective antagonist of the κ-opioid receptor (KOR).[1] BNI and norbinaltorphimine (nor-BNI) were the first highly selective KOR antagonists to be discovered.[1]
See also
References
- ^ a b Portoghese PS, Lipkowski AW, Takemori AE (March 1987). "Binaltorphimine and nor-binaltorphimine, potent and selective kappa-opioid receptor antagonists". Life Sci. 40 (13): 1287–92. doi:10.1016/0024-3205(87)90585-6. PMID 2882399.
Opioidergics
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Receptor
(ligands) |
MOR |
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DOR |
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KOR |
- Agonists: 6'-GNTI
- 8-CAC
- 18-MC
- 14-Methoxymetopon
- β-Chlornaltrexamine
- β-Funaltrexamine
- Adrenorphin (metorphamide)
- Akuuamicine
- Alazocine
- Allomatrine
- Asimadoline
- BAM-12P
- BAM-18P
- BAM-22P
- Big dynorphin
- Bremazocine
- BRL-52537
- Butorphanol
- BW-373U86
- Cebranopadol
- Ciprefadol
- CR665
- Cyclazocine
- Cyclorphan
- Cyprenorphine
- Diamorphine (heroin)
- Diacetylnalorphine
- Difelikefalin
- Dihydroetorphine
- Dihydromorphine
- Dynorphin A
- Dynorphin B (rimorphin)
- Eluxadoline
- Enadoline
- Eptazocine
- Erinacine E
- Ethylketazocine
- Etorphine
- Fedotozine
- Fentanyl
- Gemazocine
- GR-89696
- GR-103545
- Hemorphin-4
- Herkinorin
- HS665
- Hydromorphone
- HZ-2
- Ibogaine
- ICI-199,441
- ICI-204,448
- Ketamine
- Ketazocine
- Laudanosine
- Leumorphin (dynorphin B-29)
- Levallorphan
- Levorphanol
- Lexanopadol
- Lofentanil
- LPK-26
- Lufuradom
- Matrine
- MB-1C-OH
- Menthol
- Metazocine
- Metkefamide
- Mianserin
- Mirtazapine
- Morphine
- Moxazocine
- MR-2034
- N-MPPP
- Nalbuphine
- NalBzOH
- Nalfurafine
- Nalmefene
- Nalorphine
- Naltriben
- Norbuprenorphine
- Norbuprenorphine-3-glucuronide
- Noribogaine
- Norketamine
- O-Desmethyltramadol
- Oripavine
- Oxilorphan
- Oxycodone
- Pentazocine
- Pethidine (meperidine)
- Phenazocine
- Proxorphan
- RB-64
- Salvinorin A (salvia)
- Salvinorin B ethoxymethyl ether
- Salvinorin B methoxymethyl ether
- SKF-10047
- Spiradoline (U-62,066)
- TH-030418
- Thienorphine
- Tifluadom
- Tricyclic antidepressants (e.g., amitriptyline, desipramine, imipramine, nortriptyline)
- U-50,488
- U-54,494A
- U-69,593
- Xorphanol
- Antagonists: 4′-Hydroxyflavanone
- 4',7-Dihydroxyflavone
- 5'-GNTI
- 6'-GNTI
- 6β-Naltrexol
- 6β-Naltrexol-d4
- β-Chlornaltrexamine
- Buprenorphine/samidorphan
- Amentoflavone
- ANTI
- Apigenin
- Arodyne
- AT-076
- Axelopran
- Binaltorphimine
- BU09059
- Buprenorphine
- Catechin
- Catechin gallate
- CERC-501 (LY-2456302)
- Clocinnamox
- Cyclofoxy
- Dezocine
- DIPPA
- Diprenorphine
- EGC
- ECG
- Epicatechin
- Hyperoside
- JDTic
- LY-255582
- LY-2196044
- LY-2459989
- LY-2795050
- MeJDTic
- Methylnaltrexone
- ML190
- ML350
- MR-2266
- N-Fluoropropyl-JDTic
- Naloxone
- Naltrexone
- Naltrindole
- Naringenin
- Norbinaltorphimine
- Noribogaine
- Pawhuskin A
- PF-4455242
- RB-64
- Quadazocine
- Taxifolin
- UPHIT
- Zyklophin
- Unknown/unsorted: Akuammicine
- Akuammine
- Coronaridine
- Cyproterone acetate
- Dihydroakuuamine
- Ibogamine
- Tabernanthine
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NOP |
- Agonists: (Arg14,Lys15)Nociceptin
- ((pF)Phe4)Nociceptin(1-13)NH2
- (Phe1Ψ(CH2-NH)Gly2)Nociceptin(1-13)NH2
- Ac-RYYRWK-NH2
- Ac-RYYRIK-NH2
- BU08070
- Buprenorphine
- Cebranopadol
- Dihydroetorphine
- Etorphine
- JNJ-19385899
- Levorphanol
- Lexanopadol
- MCOPPB
- MT-7716
- NNC 63-0532
- Nociceptin (orphanin FQ)
- Nociceptin (1-11)
- Nociceptin (1-13)NH2
- Norbuprenorphine
- Ro64-6198
- Ro65-6570
- SCH-221510
- SCH-486757
- SR-8993
- SR-16435
- TH-030418
- Antagonists: (Nphe1)Nociceptin(1-13)NH2
- AT-076
- BAN-ORL-24
- J-113397
- JTC-801
- LY-2940094
- NalBzOH
- Nociceptin (1-7)
- Nocistatin
- SB-612111
- SR-16430
- Thienorphine
- Trap-101
- UFP-101
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Unsorted /
unknown |
- β-Casomorphins
- Amidorphin
- BAM-20P
- Cytochrophin-4
- Deprolorphin
- Gliadorphin (gluteomorphin)
- Gluten exorphins
- Hemorphins
- Kava constituents
- MEAGL
- MEAP
- NEM
- Neoendorphins
- Peptide B
- Peptide E
- Peptide F
- Peptide I
- Rubiscolins
- Soymorphins
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Enzyme
(inhibitors) |
Enkephalinase |
- Amastatin
- BL-2401
- Candoxatril
- D -Phenylalanine
- Dexecadotril (retorphan)
- Ecadotril (sinorphan)
- Kelatorphan
- Racecadotril (acetorphan)
- RB-101
- RB-120
- RB-3007
- Opiorphan
- Selank
- Semax
- Spinorphin
- Thiorphan
- Tynorphin
- Ubenimex (bestatin)
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Others |
- Propeptides: β-Lipotropin (proendorphin)
- Prodynorphin
- Proenkephalin
- Pronociceptin
- Proopiomelanocortin (POMC)
- Others: Kyotorphin (met-enkephalin releaser/degradation stabilizer)
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See also: Neuropeptidergics • Peptidergics
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English Journal
- Antihyperalgesic effect of [(±)-(2,4,6-cis)-4-chloro-6-(naphthalen-1-yl)-tetrahydro-2H-pyran-2-yl]methanol: participation of the NO/cGMP/KATP pathway and κ-opioid receptor.
- Gonçalves GM1, Capim SL, Vasconcellos ML, Marinho BG.
- Behavioural pharmacology.Behav Pharmacol.2016 Mar 31. [Epub ahead of print]
- The present study used behavioral analyses to investigate the involvement of the NO/cGMP/KATP pathway, serotoninergic, and opioid systems in the antinociceptive action of [(±)-(2,4,6-cis)-4-chloro-6-(naphthalen-1-yl)-tetrahydro-2H-pyran-2-yl]methanol (CTHP) in mice. Oral administration of CTHP (1,
- PMID 27035064
- Pharmacological characterization of EN-9, a novel chimeric peptide of endomorphin-2 and neuropeptide FF that produces potent antinociceptive activity and limited tolerance.
- Wang ZL1, Li N1, Wang P1, Tang HH1, Han ZL1, Song JJ1, Li XH1, Yu HP1, Zhang T1, Zhang R1, Xu B1, Zhang MN1, Fang Q2, Wang R3.
- Neuropharmacology.Neuropharmacology.2016 Mar 9. pii: S0028-3908(16)30089-2. doi: 10.1016/j.neuropharm.2016.03.017. [Epub ahead of print]
- Mounting evidences indicate the functional interactions between neuropeptide FF (NPFF) and opioids, including the endogenous opioids. In the present work, EN-9, a chimeric peptide containing the functional domains of the endogenous opioid endomorphin-2 (EM-2) and NPFF, was synthesized and pharmacolo
- PMID 26970017
- Effects of the kappa opioid receptor antagonist nor-binaltorphimine (nor-BNI) on cocaine versus food choice and extended-access cocaine intake in rhesus monkeys.
- Hutsell BA1, Cheng K2, Rice KC2, Negus SS1,3, Banks ML1,3.
- Addiction biology.Addict Biol.2016 Mar;21(2):360-73. doi: 10.1111/adb.12206. Epub 2015 Jan 8.
- The dynorphin/kappa opioid receptor (KOR) system has been implicated as one potential neurobiological modulator of the abuse-related effects of cocaine and as a potential target for medications development. This study determined effects of the KOR antagonist nor-binaltorphimine (nor-BNI) on cocaine
- PMID 25581305
Japanese Journal
- Dynorphin A (1–13) Alleviated Stress-Induced Behavioral Impairments in Mice
- Dynorphin-Kappa Opioid Receptor Signaling Partly Mediates Estrogen Negative Feedback Effect on LH Pulses in Female Rats
- The Journal of reproduction and development 59(3), 266-272, 2013-06-01
- NAID 10031184756
★リンクテーブル★
[★]
ノルビナルトルフィミン
- 関
- nor-binaltorphimine
[★]
ノルビナルトルフィミン
- 関
- norbinaltorphimine