WordNet

a complex consisting of an organic base in association with hydrogen chloride

Wikipedia preview

出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2015/11/06 01:35:35」(JST)

wiki en

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

This dermatologic drug article is a stub. You can help Wikipedia by expanding it.

UpToDate Contents

全文を閲覧するには購読必要です。 To read the full text you will need to subscribe.

1. 過敏性腸症候群に対するアロセトロン塩酸塩（Lotronex） alosetron hydrochloride lotronex for irritable bowel syndrome
2. 変形性関節症の初回薬物療法 initial pharmacologic therapy of osteoarthritis
3. そう痒症：マネージメントの概要 pruritus overview of management
4. クリンダマイシン：概要 clindamycin an overview
5. 成人における急性咽頭炎の対症療法 symptomatic treatment of acute pharyngitis in adults

English Journal

The effect of 17-N substituents on the activity of the opioid κ receptor in nalfurafine derivatives.

Nemoto T, Yamamoto N, Wada N, Harada Y, Tomatsu M, Ishihara M, Hirayama S, Iwai T, Fujii H, Nagase H.SourceSchool of Pharmacy, Kitasato University, 5-9-1 Shirokane, Minato-ku, Tokyo 108-8641, Japan.
Bioorganic & medicinal chemistry letters.Bioorg Med Chem Lett.2013 Jan 1;23(1):268-72. doi: 10.1016/j.bmcl.2012.10.100. Epub 2012 Oct 30.
We have previously reported the essential structure of the opioid κ receptor agonist nalfurafine hydrochloride (TRK-820) for binding to the κ receptor. In the course of this study, we focused on the effect of the substituent at 17-N in nalfurafine on the binding affinity for the κ receptor. The e
PMID 23200250

In vitro and in vivo pharmacological characterization of the main metabolites of nalfurafine hydrochloride.

Nakao K, Togashi Y, Honda T, Momen S, Umeuchi H, Sakakibara S, Tanaka T, Okano K, Mochizuki H.SourcePharmaceutical Research Laboratories, Toray Industries, Inc., 10-1 Tebiro 6-chome, Kamakura, Kanagawa, Japan. Kaoru_Nakao@nts.toray.co.jp
European journal of pharmacology.Eur J Pharmacol.2012 Nov 15;695(1-3):57-61. doi: 10.1016/j.ejphar.2012.08.017. Epub 2012 Sep 4.
Pharmacological characterization of the main metabolites of nalfurafine hydrochloride ((E)-N-[17-(cyclopropylmethyl)-4,5α-epoxy-3,14-dihydroxymorphinan-6β-yl]-3-(furan-3-yl)-N-methylprop-2-enamide monohydrochloride; a selective κ-opioid receptor agonist and an antipruritic for uremic pruritus in
PMID 22981641

Effect of nalfurafine hydrochloride on pruritus and anxiety level in hemodialysis patients.

Inui S, Shirakawa Y, Itami S.
The Journal of dermatology.J Dermatol.2012 Oct;39(10):886-7. doi: 10.1111/j.1346-8138.2011.01442.x. Epub 2011 Dec 5.
PMID 22142516

Japanese Journal

血液透析患者におけるそう痒症の実態とナルフラフィン塩酸塩の臨床効果 : 東海地区17施設における1,936例のアンケート調査

山田成樹,櫻井寛,春日弘毅 [他]
日本透析医学会雑誌 45(12), 1133-1140, 2012-12-00
NAID 40019541780

血液透析患者のかゆみの指標としての thymus and activation-regulated chemokine (TARC) の意義

山田吉広,須澤大知,熊藤公博 [他],袖山孝徳,島村栄,棚岡綾乃,浦野浩明,百瀬光生,床尾万寿雄
日本透析医学会雑誌 = Journal of Japanese Society for Dialysis Therapy 44(6), 577-580, 2011-06-28
慢性血液透析患者ではヒスタミンH<SUB>1</SUB>受容体拮抗薬の内服にてもそう痒症を訴える既存治療抵抗性皮膚そう痒症透析患者（以下そう痒症透析患者）が認められる．そこで現在の痒みの状態を定量化するため，また，痒みの主観的感覚を客観的な数値に置き換えるために聴覚アナログ尺度（hearing analogus scale：HAS）を考案使用してHASと，ケモカインの一種で …
NAID 10029407186

新規メカニズムに基づく難治性そう痒症治療薬ナルフラフィン塩酸塩の創出

長瀬博,川村邦昭,河合孝治 [他],早川潤
有機合成化学協会誌 68(12), 1261-1271, 2010-12-01
… Nalfurafine hydrochloride (1) was launched on March of 2009 in Japan as the first in class non-narcotic opioid drug for intractable itch caused by haemodialysis. … Nalfurafine hydrochloride (1) showed significant opioid κ-agonist activity and induced neither aversion nor preference in rats on the CPP (Conditioned Place Preference) test. …
NAID 10027409446

「ナルフラフィン」

Nalfurafine
Systematic (IUPAC) name
	(2E)-N-[(5α,6β)-17-(cyclopropylmethyl)- 3,14-dihydroxy- 4,5-epoxymorphinan- 6-yl]- 3-(3-furyl)- N-methylacrylamide
Clinical data
AHFS/Drugs.com	International Drug Names
Routes of; administration	intravenous
Identifiers
CAS Registry Number	152658-17-8
ATC code	V03AX02
PubChem	CID: 6445230
IUPHAR/BPS	1651
ChemSpider	4949003
UNII	XC41AVD567
ChEMBL	CHEMBL267495
Synonyms	TRK-820
Chemical data
Formula	C28H32N2O5
Molecular mass	476.564 g/mol
	SMILES 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 ;
	InChI 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 ; Key:XGZZHZMWIXFATA-UEZBDDGYSA-N ;
(what is this?) (verify)