ナルフラフィン
Wikipedia preview
出典(authority):フリー百科事典『ウィキペディア(Wikipedia)』「2015/12/18 14:38:30」(JST)
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Nalfurafine
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Systematic (IUPAC) name |
(2E)-N-[(5α,6β)-17-(cyclopropylmethyl)- 3,14-dihydroxy- 4,5-epoxymorphinan- 6-yl]- 3-(3-furyl)- N-methylacrylamide
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Clinical data |
AHFS/Drugs.com |
International Drug Names |
Routes of
administration |
intravenous |
Identifiers |
CAS Number |
152658-17-8 Y |
ATC code |
V03AX02 |
PubChem |
CID: 6445230 |
IUPHAR/BPS |
1651 |
ChemSpider |
4949003 N |
UNII |
XC41AVD567 Y |
ChEMBL |
CHEMBL267495 N |
Synonyms |
TRK-820 |
Chemical data |
Formula |
C28H32N2O5 |
Molecular mass |
476.564 g/mol |
SMILES
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CN([C@@H]1CC[C@]2([C@H]3CC4=C5[C@]2([C@H]1OC5=C(C=C4)O)CCN3CC6CC6)O)C(=O)/C=C/C7=COC=C7
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InChI
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InChI=1S/C28H32N2O5/c1-29(23(32)7-4-18-9-13-34-16-18)20-8-10-28(33)22-14-19-5-6-21(31)25-24(19)27(28,26(20)35-25)11-12-30(22)15-17-2-3-17/h4-7,9,13,16-17,20,22,26,31,33H,2-3,8,10-12,14-15H2,1H3/b7-4+/t20-,22-,26+,27+,28-/m1/s1 N
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Key:XGZZHZMWIXFATA-UEZBDDGYSA-N N
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NY (what is this?) (verify) |
Nalfurafine (INN and USAN;[1] also known as AC-820, TRK-820; trade name Remitch) is a κ-opioid receptor agonist marketed as a treatment for uremic pruritus in people undergoing hemodialysis.[2]
As of January 2010[update], it is also being investigated for the treatment of pruritus in patients with chronic liver disease.[3]
References
- ^ Statement on a Nonproprietary Name adopted by the USAN Council
- ^ "AC-820". Acologix. 2009.
- ^ Clinical trial number NCT00638495 for "Phase II Study of TRK-820 Soft Capsules — Intractable Pruritus in Patients With Chronic Liver Disease" at ClinicalTrials.gov
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
- 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
- ALKS-5461
- Amentoflavone
- ANTI
- Apigenin
- Arodyne
- AT-076
- Axelopran
- Binaltorphimine
- BU09059
- Buprenorphine
- Catechin
- Catechin gallate
- CERC-501 (LY-2456302)
- Clocinnamox
- Dezocine
- DIPPA
- Diprenorphine
- EGC
- ECG
- Epicatechin
- Hyperoside
- JDTic
- LY-255582
- LY-2196044
- LY-2459989
- LY-2795050
- Methylnaltrexone
- ML190
- ML350
- MR-2266
- 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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UpToDate Contents
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English Journal
- Targeting multiple opioid receptors - improved analgesics with reduced side effects?
- Günther T1, Dasgupta P1, Mann A1, Miess E1, Kliewer A1, Fritzwanker S1, Steinborn R1, Schulz S1.
- British journal of pharmacology.Br J Pharmacol.2017 Apr 5. doi: 10.1111/bph.13809. [Epub ahead of print]
- PMID 28378462
- Nalfurafine is a G-protein biased agonist having significantly greater bias at the human than rodent form of the kappa opioid receptor.
- Schattauer SS1, Kuhar JR1, Song A1, Chavkin C2.
- Cellular signalling.Cell Signal.2017 Apr;32:59-65. doi: 10.1016/j.cellsig.2017.01.016. Epub 2017 Jan 11.
- PMID 28088389
- Predictors of pruritus in patients with chronic liver disease and usefulness of nalfurafine hydrochloride.
- Akuta N1, Kumada H1, Fujiyama S1, Kawamura Y1, Sezaki H1, Hosaka T1, Kobayashi M1, Kobayashi M2, Saitoh S1, Suzuki Y1, Suzuki F1, Arase Y1, Ikeda K1.
- Hepatology research : the official journal of the Japan Society of Hepatology.Hepatol Res.2017 Mar 21. doi: 10.1111/hepr.12894. [Epub ahead of print]
- PMID 28322485
Related Links
- Nalfurafine is a medicine available in a number of countries worldwide. A list of US medications equivalent to Nalfurafine is available on the Drugs.com website. ... Drugs.com provides accurate and independent information on more ...
- 1 注)注意-医師等の処方せんにより使用すること ナルフラフィン塩酸塩(Nalfurafine Hydrochloride)製剤 2012年2月 製造販売元 東レ株式会社 販売元 鳥居薬品株式会社 謹啓 時下、益々ご清祥のこととお慶び申し上げます。平素は ...
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