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About This Item
実験式（ヒル表記法）:
C21H24ClNO2 · HCl
CAS番号:
分子量:
394.33
MDL番号:
UNSPSCコード:
12352200
PubChem Substance ID:
フォーム
solid
色
white
溶解性
DMSO: soluble (Solutions must be freshly prepared.)
aqueous base: unstable
SMILES記法
Cl[H].ClCCN1CCC(CC1)OC(=O)C(c2ccccc2)c3ccccc3
遺伝子情報
human ... CHRM1(1128) , CHRM2(1129) , CHRM3(1131) , CHRM4(1132) , CHRM5(1133)
生物化学的／生理学的作用
ムスカリン性アセチルコリンレセプタ-の不可逆的なアンタゴニストであり、 M1, M3, M4, M5レセプタ-に対する親和性はほぼ同じですが、M2レセプタ-に対してはかなり低親和性です。
注意
吸湿性です。
保管分類コード
13 - Non Combustible Solids
WGK
WGK 3
引火点(°F)
Not applicable
引火点(℃)
Not applicable
個人用保護具 (PPE)
Eyeshields, Gloves, type N95 (US)
最新バージョンのいずれかを選択してください：
F J Ehlert et al.
Life sciences, 62(17-18), 1659-1664 (1998-05-19)
Irreversible ligands are useful tools for investigating the function of receptor subtypes in various physiological processes. The mechanism for alkylation involves the formation of a reversible receptor complex followed by a covalent reaction. The extent of receptor alkylation is determined
E A Thomas et al.
Molecular pharmacology, 44(1), 102-110 (1993-07-01)
A functional role for the M2 muscarinic receptor in smooth muscle contraction was investigated in isolated guinea pig ileum. Contractile responses to the muscarinic agonist oxotremorine-M (oxo-M) were measured in isolated ilea that had been pretreated with histamine (0.32 microM)
N Watson et al.
European journal of pharmacology, 278(3), 195-201 (1995-05-24)
Muscarinic M2 receptors account for more than half the muscarinic receptor population in smooth muscles of a number of species and yet it is the smaller M3 receptor population that mediates contraction of many of these tissues. The role of
F J Ehlert
Life sciences, 58(22), 1971-1978 (1996-01-01)
The compound 4-DAMP mustard (N-2-chloroethyl-4-piperidinyl diphenylacetate) is a 2-chloroethylamine derivative of the selective muscarinic antagonist 4-DAMP (N,N-dimethyl-4-piperidinyl diphenylacetate). At neutral pH, 4-DAMP mustard cyclizes spontaneously into an oziridinium ion that binds covalently with muscarinic receptors. Analysis of the kinetics of
Johannes Bodenstein et al.
The Journal of pharmacology and experimental therapeutics, 314(2), 891-905 (2005-04-29)
Many irreversible antagonists have been shown to inactivate G protein-coupled receptors (GPCRs) and used to study agonists and spare receptors. Presumably, they bind to primary (agonist) binding sites on the GPCR, although noncompetitive mechanisms of antagonism have been demonstrated but
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