McN-A343,M1毒蕈碱激动剂结构式
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常用名 | McN-A343,M1毒蕈碱激动剂 | 英文名 | McN-A 343 |
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| CAS号 | 55-45-8 | 分子量 | 317.21100 | |
| 密度 | N/A | 沸点 | N/A | |
| 分子式 | C14H18Cl2N2O2 | 熔点 | N/A | |
| MSDS | 中文版 美版 | 闪点 | N/A |
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Central muscarinic cholinergic activation alters interaction between splenic dendritic cell and CD4+CD25- T cells in experimental colitis.
PLoS ONE 9(10) , e109272, (2014) The cholinergic anti-inflammatory pathway (CAP) is based on vagus nerve (VN) activity that regulates macrophage and dendritic cell responses in the spleen through alpha-7 nicotinic acetylcholine receptor (a7nAChR) signaling. Inflammatory bowel disease (IBD) p... |
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Functional activation of G-proteins coupled with muscarinic acetylcholine receptors in rat brain membranes.
J. Pharmacol. Sci. 125(2) , 157-68, (2014) The functional activation of Gi/o proteins coupled to muscarinic acetylcholine receptors (mAChRs) was investigated with the conventional guanosine-5'-O-(3-[(35)S]thio) triphosphate ([(35)S]GTPγS) binding assay in rat brain membranes. The most efficacious stim... |
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Investigating the interaction of McN-A-343 with the M2 muscarinic receptor using its nitrogen mustard derivative.
Biochem. Pharmacol. 79(7) , 1025-35, (2010) We investigated whether the aziridinium ion formed from a nitrogen mustard derivative (4-[(2-bromoethyl)methyl-amino]-2-butynyl N-(3-chlorophenyl)carbamate; BR384) structurally related to McN-A-343 (4-(trimethyl-amino)-2-butynyl N-(3-chlorophenyl)carbamate) i... |
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Investigating the interaction of McN-A-343 with the M muscarinic receptor using its nitrogen mustard derivative and ACh mustard.
Br. J. Pharmacol. 160(6) , 1534-49, (2010) We investigated how McN-A-343 inhibited the alkylation of the M(1) muscarinic receptor by its nitrogen mustard derivative and that of ACh to identify whether it interacts allosterically or orthosterically.We incubated the M(1) muscarinic receptor expressed in... |
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Negative crosstalk between M1 and M2 muscarinic autoreceptors involves endogenous adenosine activating A1 receptors at the rat motor endplate.
Neurosci. Lett. 459 , 127-131, (2009) At the rat motor nerve terminals, activation of muscarinic M(1) receptors negatively modulates the activity of inhibitory muscarinic M(2) receptors. The present work was designed to investigate if the negative crosstalk between muscarinic M(1) and M(2) autore... |
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Use of acetylcholine mustard to study allosteric interactions at the M(2) muscarinic receptor.
J. Pharmacol. Exp. Ther. 327(2) , 518-28, (2008) We explored the interaction of a nitrogen mustard derivative of acetylcholine with the human M(2) muscarinic receptor expressed in Chinese hamster ovary cells using the muscarinic radioligand, [3H]N-methylscopolamine (NMS). Acetylcholine mustard caused a conc... |
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M-type potassium channels modulate Schaffer collateral-CA1 glutamatergic synaptic transmission.
J. Physiol. 590(Pt 16) , 3953-64, (2012) Previous studies have suggested that muscarinic receptor activation modulates glutamatergic transmission. M-type potassium channels mediate the effects of muscarinic activation in the hippocampus, and it has been proposed that they modulate glutamatergic syna... |
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[Acetylcholine induces human detrusor muscle cell proliferation: molecular and pharmacological characterization].
Urologia 79(2) , 102-8, (2012) The purpose of the study is to understand whether the cholinergic stimulation is important, not only in inducing contraction of the detrusor muscle, but also in modulating the proliferation of smooth muscle cells. These results could help to better understand... |
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Pharmacological characterization of muscarinic receptor subtypes mediating vasoconstriction of human umbilical vein.
Br. J. Pharmacol. 147(5) , 516-23, (2006) The present study attempted to pharmacologically characterize the muscarinic receptor subtypes mediating contraction of human umbilical vein (HUV).HUV rings were mounted in organ baths and concentration-response curves were constructed for acetylcholine (ACh)... |
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Mutagenesis of nucleophilic residues near the orthosteric binding pocket of M1 and M2 muscarinic receptors: effect on the binding of nitrogen mustard analogs of acetylcholine and McN-A-343.
Mol. Pharmacol. 78(4) , 745-55, (2010) Investigating how a test drug alters the reaction of a site-directed electrophile with a receptor is a powerful method for determining whether the drug acts competitively or allosterically, provided that the binding site of the electrophile is known. In this ... |