|
|Section2= |Section3= }} Benzilylcholine mustard (''N''-2-chloroethyl-''N''-methyl 2-aminoethyl benzilate) is a modified version of acetylcholine, so named because after cyclization in solution it forms an iminium derivative that is structurally similar to benzilylcholine. It is well known for being an irreversible antagonist of the muscarinic acetylcholine receptor.〔Gill, E.W.; Rang, H.P. (July 1966) ("An Alkylating Derivative of Benzilylcholine with Specific and Long-Lasting Parasympatholytic Activity" ), ''Molecular Pharmacology'', vol.2 no.4 284-297〕 It has been used in pharmacological experiments investigating the relationship between receptor occupancy and response. It was also one of the tools in characterization of the muscarinic acetylcholine receptor.〔Gupta, Surendra K.; Moran, John F.; Triggle, David F. (November 1976) ("Mechanism of Action of Benzilylcholine Mustard at the Muscarinic Receptor" ), ''Molecular Pharmacology'', vol.12 no.6 1019-1026〕 ==Mechanism== On the muscarinic acetylcholine receptor, benzilylcholine mustard acts as an alkylating agent at two sites, one site being the acetylcholine recognition site itself, and the other a site that stabilises the receptor in its inactive state.〔Gupta, Moran, Triggle (1974)〕 Groups that can be alkylated in this way include thiols, alcohols, imines and carboxylic acids.〔John C. Foreman, Torben Johansen, Alasdair J. Gibb (2009) ''Textbook of Receptor Pharmacology, Third Edition'', CRC Press, (page 51 )〕 抄文引用元・出典: フリー百科事典『 ウィキペディア（Wikipedia）』 ■ウィキペディアで「Benzilylcholine mustard」の詳細全文を読む スポンサード リンク
|