WordNet

a narcotic antagonist (trade name Nalline) that counteracts the effects of narcotics (especially the effects of poisoning by morphine) (同)Nalline

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2013/05/12 09:40:40」(JST)

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Nalorphine (INN; Lethidrone, Nalline), also known as N-allyl-normorphine, is a mixed opioid agonist-antagonist. It acts at two opioid receptors, at the mu receptor it has antagonistic effects and at the kappa receptors it exerts agonistic characteristics. It is used to reverse opioid overdose and (starting in the 1950s) in a challenge test to determine opioid dependence.^[1]

References [edit]

^ "Medicine: Drug Detector", Time, Dec. 24, 1956

This drug article relating to the nervous system is a stub. You can help Wikipedia by expanding it.

English Journal

Predicted structures for kappa opioid G-protein coupled receptor bound to selective agonists.

Li Q1,2, Kim SK1, Goddard WA 3rd1, Chen G2, Tan H2.
Journal of chemical information and modeling.J Chem Inf Model.2015 Mar 23;55(3):614-27. doi: 10.1021/ci500523z. Epub 2015 Feb 17.
Human kappa opioid receptor (κ-OR), a G protein-coupled receptor (GPCR), has been identified as a drug target for treatment of such human disorders as pain perception, neuroendocrine physiology, affective behavior, and cognition. In order to find more selective and active agonists, one would like t
PMID 25642595
PMID 25522425

Sulfation of opioid drugs by human cytosolic sulfotransferases: metabolic labeling study and enzymatic analysis.

Kurogi K1, Chepak A1, Hanrahan MT1, Liu MY2, Sakakibara Y3, Suiko M3, Liu MC4.
European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences.Eur J Pharm Sci.2014 Oct 1;62:40-8. doi: 10.1016/j.ejps.2014.05.003. Epub 2014 May 14.
The current study was designed to examine the sulfation of eight opioid drugs, morphine, hydromorphone, oxymorphone, butorphanol, nalbuphine, levorphanol, nalorphine, and naltrexone, in HepG2 human hepatoma cells and human organ samples (lung, liver, kidney, and small intestine) and to identify the
PMID 24832963

Japanese Journal

オピエートのフロンティア電子密度の統計解析

水上善博
滋賀大学教育学部紀要. 3, 自然科学 54, 35-39, 2004
… occupied molecular orbitals of 25 opiates are calculated by semi-empirical AM1 molecular orbital calculations.Calculated opiates are morphine, oxymorphone, levorphanol, nalorphine, naloxone, levallorphan, heroin, codeine, etorphine, dihydromorphine, normorphine, pentazocine, apomorphine, buprenorphine, butorpahnol, dihydrocodeine, oxycodone, thebaine, bremazocine, cyclazocine, ketocyclazocine, naloxazone, naltrexazone, oxymorphazone.25 molecules have common molecular skeleton that includes 10 atoms(one nitrogen atom, one oxygen atom and 8 carbon …
NAID 110001183530

Synthesis and Pharmacological Activity of Sulfate Conjugates at 6-Position of N-Substituted Normorphine Derivatives

平野孝明,小栗一太,吉村英敏
Chemical & pharmaceutical bulletin 39(8), 2000-2004, 1991-08-25
… The compounds examined were nalorphine, nalorphine-6-sulfate (N-6-S), N-cyclopropylmethylnormorphine (CPN), N-cyclopropylmethylnormorphine-6-sulfate (C-6-S), N-dimethylallylnormorphine (DMN) and N-dimethylallylnormorphine-6-sulfate (D-6-S). … injection, and the activity of N-6-S was about 2 times more potent than that of nalorphine. …
NAID 110003629484

Enhanced binding of morphine and nalorphine to opioid delta receptor by glucuronate and sulfate conjugations at the 6-position

OGURI K.
Life Sci. 41, 1457-1464, 1987
NAID 80003568655

Related Pictures

★リンクテーブル★

リンク元

「オピオイド」

Nalorphine
Systematic (IUPAC) name
	(5α,6α)-17-allyl- 7,8-didehydro- 4,5-epoxymorphinan- 3,6-diol
Clinical data
AHFS/Drugs.com	International Drug Names
Pregnancy cat.	?
Legal status	?
Identifiers
CAS number	62-67-9
ATC code	V03AB02
PubChem	CID 5284595
IUPHAR ligand	1629
ChemSpider	4447643
UNII	U59WB2WRY2
ChEMBL	CHEMBL415284
Synonyms	(−)−(5R,6S)-9α-allyl- 4,5-epoxymorphin- 7-en- 3,6-diol
Chemical data
Formula	C19H21NO3
Mol. mass	311.375 g/mol
	SMILES O[C@H]2\C=C/[C@H]5[C@@H]4N(CC[C@@]51c3c(O[C@H]12)c(O)ccc3C4)C\C=C;
	InChI InChI=1S/C19H21NO3/c1-2-8-20-9-7-19-12-4-6-15(22)18(19)23-17-14(21)5-3-11(16(17)19)10-13(12)20/h2-6,12-13,15,18,21-22H,1,7-10H2/t12-,13+,15-,18-,19-/m0/s1 ; Key:UIQMVEYFGZJHCZ-SSTWWWIQSA-N ;
(what is this?) (verify);

　　[★]

英: opioid
同: 類麻薬
関: オピオイド受容体

オピオイド受容体に結合するモルフィン様物質のことを指す。

内因性のオピオイドペプチドが発見され、これらは内因性オピオイドペプチドと呼ばれるようになった。

作用

縮瞳

モルフィンと多くのμ,κアゴニストは瞳孔の縮小を引き起こす。これは瞳孔を支配する副交感神経の興奮による。μアゴニストを中毒量投与すると縮瞳し、pinpoints pupupilsはpathognomonicである。(GOO.559)

オピオイドとオピオイド類似物質の作用

GOO.552

Drugs	RECEPTOR TYPES
Drugs	μ受容体	δ受容体	κ受容体
morphine	＋＋＋		＋
methadone	＋＋＋
etorphine	＋＋＋	＋＋＋	＋＋＋
levorphanol	＋＋＋
fentanyl	＋＋＋
sufentanil	＋＋＋	＋	＋
DAMGO	＋＋＋
butorphanol	P		＋＋＋
buprenorphine	P		ーー
naloxone	ーーー	ー	ーー
naltrexone	ーーー	ー	ーーー
CTOP	ーーー
diprenorphine	ーーー	ーー	ーーー
β-funaltrexamine	ーーー	ー	＋＋
naloxonazine	ーーー	ー	ー
nalorphine	ーーー		＋
pentazocine	P		＋＋
nalbuphine	ーー		＋＋
naloxone benzoylhydrazone	ーーー	ー	ー
bremazocine	＋＋＋	＋＋	＋＋＋
ethylketocyclazocine	P	＋	＋＋＋
U50,488			＋＋＋
U69,593			＋＋＋
spiradoline	＋		＋＋＋
nor-Binaltorphimine	ー	ー	ーーー
naltrindole	ー	ーーー	ー
DPDPE		＋＋
[[［[D-Ala2,Glu4］deltorphin]]		＋＋

DSLET	＋	＋＋
endogenous Peptides
met-enkephalin	＋＋	＋＋＋
leu-enkephalin	＋＋	＋＋＋
β-endorphin	＋＋＋	＋＋＋
dynorphin A	＋＋		＋＋＋
dynorphin B	＋	＋	＋＋＋
α-neoendorphin	＋	＋	＋＋＋

＋アゴニスト　ーアンタゴニスト　P partial agonist

各鎮痛薬のオピオイド受容体への作用

　　　　　　　　　μ受容体　κ受容体

レミフェンタニル　＋＋＋　　ー

フェンタニル　　　＋＋＋　　－

モルヒネ　　　　　＋＋＋　　＋

ペチジン　　　　　＋＋　　　＋

トラマドール　　　＋　　　　－

ペンタゾシン　　　ー　　　　＋＋

ブプレノルフィン　Ｐ　　　　ー

ナロキソン　　　　ー　　　　－

[1] "Medicine: Drug Detector", Time, Dec. 24, 1956

匿名

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案内

案内

nalorphine