関: ambenonium chloride

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2015/08/22 20:57:35」(JST)

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Ambenonium (as ambenonium dichloride, trade name Mytelase) is a cholinesterase inhibitor^[1] used in the management of myasthenia gravis.

It is classified as reversible.^[2]

Mechanism of action

Ambenonium exerts its actions against myasthenia gravis by competitive reversible inhibition of acetylcholinesterase, the enzyme responsible for the hydrolysis of acetylcholine. Myasthenia gravis occurs when the body produces antibodies against acetylcholine receptors, and thus inhibits signal transmission across the myoneural junction. Ambenonium reversibly binds acetylcholinesterase, inactivates it and therefore increases levels of acetylcholine. This, in turn, facilitates transmission of impulses across the myoneural junction and effectively treats the disease.

Indications

Ambenonium is used to treat muscle weakness due to disease or defect of the neuromuscular junction (myasthenia gravis).

References

^ Bolognesi ML, Cavalli A, Andrisano V et al. (September 2003). "Design, synthesis and biological evaluation of ambenonium derivatives as AChE inhibitors". Farmaco 58 (9): 917–28. doi:10.1016/S0014-827X(03)00150-2. PMID 13679187.
^ Hodge AS, Humphrey DR, Rosenberry TL (May 1992). "Ambenonium is a rapidly reversible noncovalent inhibitor of acetylcholinesterase, with one of the highest known affinities". Mol. Pharmacol. 41 (5): 937–42. PMID 1588924.

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English Journal

Preparation, in vitro screening and molecular modelling of symmetrical bis-quinolinium cholinesterase inhibitors--implications for early myasthenia gravis treatment.

Komloova M, Musilek K, Horova A, Holas O, Dohnal V, Gunn-Moore F, Kuca K.SourceCharles University, Faculty of Pharmacy, Department of Pharmaceutical Chemistry and Drug Control, Heyrovskeho 1203, 500 05 Hradec Kralove, Czech Republic.
Bioorganic & medicinal chemistry letters.Bioorg Med Chem Lett.2011 Apr 15;21(8):2505-9. Epub 2011 Feb 21.
This paper describes the preparation and in vitro evaluation of 18 newly prepared bis-quinolinium inhibitors on human recombinant acetylcholinesterase (AChE) and human plasmatic butyrylcholinesterase (BChE). Their inhibitory (IC(50)) and was compared to the chosen standards ambenonium dichloride, ed
PMID 21397501

Preparation and in vitro screening of symmetrical bis-isoquinolinium cholinesterase inhibitors bearing various connecting linkage--implications for early Myasthenia gravis treatment.

Musilek K, Komloova M, Holas O, Hrabinova M, Pohanka M, Dohnal V, Nachon F, Dolezal M, Kuca K.SourceUniversity of Defence, Faculty of Military Health Sciences, Department of Toxicology, Trebesska 1575, 500 01 Hradec Kralove, Czech Republic. kamil.musilek@gmail.com
European journal of medicinal chemistry.Eur J Med Chem.2011 Feb;46(2):811-8. Epub 2010 Dec 21.
Inhibitors of acetylcholinesterase are compounds widely used in the treatment of various diseases, such as Alzheimer's disease, glaucoma and Myasthenia gravis (MG). Compounds used in the therapy of MG posses a positive charge in the molecule to ensure peripheral effect of action and minimal blood-br
PMID 21236521

Japanese Journal

調節麻痺及び調節性眼精疲労におけるAmbenonium chloride(Mytelase)の使用例

田辺彌吉
臨床眼科 15(7), ????, 1961-07
NAID 40018588782

術後腸管麻痺の予防剤としてのマイテラーゼ注の効果

鈴木快輔,上坂英雄,金漢相,永野克郎,山本三雄
昭和医学会雑誌 21(7), 794-797, 1961
… Mytelase were applied on 10 cases of appendectomy, 10 cases of gastrectomy, 5 cases of intestinal resection or intestinal anastomosis and 5 cases of cholecystectomy. …
NAID 130001821488

重症筋無力症に対するMytelase(WIN8077)の臨床効果

林晴彦 [他]
臨床内科小児科 15(1), ????, 1960-01
NAID 40018614750

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リンク元	「アンベノニウム」「ambenonium chloride」

「アンベノニウム」

Ambenonium chloride
Systematic (IUPAC) name
	2,2'-[(1,2-dioxoethane-1,2-diyl)diimino]bis[N-(2-chlorobenzyl)-N,N-diethylethanaminium]
Clinical data
AHFS/Drugs.com	Consumer Drug Information
MedlinePlus	a699058
Routes of; administration	Oral
Pharmacokinetic data
Bioavailability	Low
Identifiers
CAS Registry Number	7648-98-8
ATC code	N07AA30
PubChem	CID: 8288
DrugBank	DB01122
ChemSpider	7987
UNII	L16PUN799N
KEGG	D01001
ChEBI	CHEBI:2628
ChEMBL	CHEMBL1652
Chemical data
Formula	C28H42Cl2N4O2+2
Molecular mass	537.564 g/mol
	SMILES [Cl-].[Cl-].Clc1ccccc1C[N+](CC)(CC)CCNC(=O)C(=O)NCC[N+](Cc2ccccc2Cl)(CC)CC ;
	InChI InChI=1S/C28H40Cl2N4O2.2ClH/c1-5-33(6-2,21-23-13-9-11-15-25(23)29)19-17-31-27(35)28(36)32-18-20-34(7-3,8-4)22-24-14-10-12-16-26(24)30;;/h9-16H,5-8,17-22H2,1-4H3;2*1H ; Key:DXUUXWKFVDVHIK-UHFFFAOYSA-N ;
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