Arecaidine but-2-ynyl ester tosylate是一种选择性的毒蕈碱型乙酰胆碱受体（mAChR）M2激动剂。
Cas No.:119630-77-2
Sample solution is provided at 25 µL, 10mM.
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Arecaidine but-2-ynyl ester tosylate is a selective muscarinic acetylcholine receptor (mAChR) M2 agonist[1-2]. Arecaidine but-2-ynyl ester tosylate dose-dependently reduces mean arterial pressure and heart rate by activating M2 receptors. Arecaidine but-2-ynyl ester tosylate can be used in research related to cardiovascular diseases[3-4].
In vitro, MDA-MB-231 and MCF-7 breast cancer cells were treated with Arecaidine but-2-ynyl ester tosylate (0.01μM – 1mM) for 24 hours. Arecaidine but-2-ynyl ester tosylate significantly inhibited cell viability, proliferation, clonogenicity, and migratory capacity, while also downregulating the expression of cell cycle-related genes (CCND1, CDK6, MKI67). Arecaidine but-2-ynyl ester tosylate caused cell cycle arrest in MDA-MB-231 cells and induced apoptosis in MCF-7 cells[5]. In anticholinesterase-pretreated rat diaphragm neuromuscular junction preparations, Arecaidine but-2-ynyl ester tosylate (0.5–50μM) did not significantly alter non-quantal acetylcholine release as measured by the H-effect (endplate hyperpolarization amplitude)[6].
In vivo, Arecaidine but-2-ynyl ester tosylate (3, 10, 30mM) was microinjected (0.5μl) into the cerebellar cortex (lobule VI) of anesthetized SD rats. Arecaidine but-2-ynyl ester tosylate dose-dependently reduced mean arterial pressure and heart rate, with this cardiovascular inhibitory effect recovering within approximately 2.5 minutes[7]. Intrathecal injection of Arecaidine but-2-ynyl ester tosylate (0.3–30nmol/mouse) dose-dependently suppressed leukocyte migration in a zymosan-induced air pouch model in ICR mice and selectively increased Fos expression (a neuronal activation marker) in sympathetic preganglionic neurons of the T7-T11 spinal segments (which primarily project to the adrenal medulla)[8].
References:
[1] Liu J, Evans MS, Lee TJ. Presynaptic muscarinic M(2)-receptor-mediated inhibition of N-type Ca(2+) channels in cultured sphenopalatine ganglion: direct evidence for acetylcholine inhibition of cerebral nitrergic neurogenic vasodilation. J Pharmacol Exp Ther. 2002 Jul;302(1):397-405
[2] Chiang PH, Yeh WC, Lee CT, et al. M(1)-like muscarinic acetylcholine receptors regulate fast-spiking interneuron excitability in rat dentate gyrus. Neuroscience. 2010 Aug 11;169(1):39-51.
[3] Shi H, Yang B, Xu D, et al. Electrophysiological characterization of cardiac muscarinic acetylcholine receptors: different subtypes mediate different potassium currents. Cell Physiol Biochem. 2003;13(2):59-74.
[4] Finney SM, Stewart LH, Gillespie JI. Cholinergic activation of phasic activity in the isolated bladder: possible evidence for M3- and M2-dependent components of a motor/sensory system. BJU Int. 2007 Sep;100(3):668-78.
[5] Yavuz M, Kahyaogullari BN, Demircan T. Anti-carcinogenic effects of arecaidine but-2-ynyl ester tosylate on breast cancer: proliferation inhibition and activation of apoptosis. Mol Biol Rep. 2025 Mar 4;52(1):278.
[6] Malomouzh AI, Mukhtarov MR, Nikolsky EE, et al. Muscarinic M1 acetylcholine receptors regulate the non-quantal release of acetylcholine in the rat neuromuscular junction via NO-dependent mechanism. J Neurochem. 2007 Sep;102(6):2110-2117
[7] Zhang C, Sun T, Zhou P, et al. Role of Muscarinic Acetylcholine Receptor-2 in the Cerebellar Cortex in Cardiovascular Modulation in Anaesthetized Rats. Neurochem Res. 2016 Apr;41(4):804-12.
[8] Yoon SY, Kwon YB, Kim HW, et al. A spinal muscarinic M2 receptor-GABAergic disinhibition pathway that modulates peripheral inflammation in mice. Neuropharmacology. 2007 Oct;53(5):677-86.
Arecaidine but-2-ynyl ester tosylate是一种选择性的毒蕈碱型乙酰胆碱受体（mAChR）M2激动剂[1-2]。Arecaidine but-2-ynyl ester tosylate通过激活M2受体来剂量依赖性地降低平均动脉压和心率。Arecaidine but-2-ynyl ester tosylate可用于心血管疾病的相关研究[3-4]。
在体外，Arecaidine but-2-ynyl ester tosylate（0.01μM–1mM）处理MDA-MB-231和MCF-7乳腺癌细胞24小时。Arecaidine but-2-ynyl ester tosylate显著抑制细胞活力、增殖、克隆形成及迁移能力，同时降低细胞周期相关基因（CCND1，CDK6，MKI67）的表达；在MDA-MB-231细胞中引起细胞周期阻滞，在MCF-7细胞中诱导细胞凋亡[5]。Arecaidine but-2-ynyl ester tosylate（0.5–50μM）处理抗胆碱酯酶预处理的大鼠膈肌神经肌肉接头标本，未显著改变由H效应（终板超极化幅度）衡量的非量子性乙酰胆碱释放[6]。
在体内，Arecaidine but-2-ynyl ester tosylate（3、10、30mM）微量注射（0.5μl）至麻醉SD大鼠的小脑皮层（小叶VI）。Arecaidine but-2-ynyl ester tosylate可剂量依赖性地降低平均动脉压和心率，此心血管抑制效应可在约2.5分钟内恢复[7]。鞘内注射Arecaidine but-2-ynyl ester tosylate（0.3–30nmol/只）可剂量依赖性地抑制酵母聚糖诱导的ICR小鼠气囊模型中白细胞的迁移，并选择性增加T7-T11脊髓节段（主要投射至肾上腺髓质）交感节前神经元中Fos（神经元激活标志物）的表达[8]。
| Cell experiment [1]: | |
Cell lines | MDA-MB-231 (human triple-negative breast adenocarcinoma cell line) and MCF-7 (human estrogen receptor-positive breast adenocarcinoma cell line) |
Preparation Method | MDA-MB-231 and MCF-7 cells were maintained in Dulbecco's Modified Eagle Medium (DMEM) supplemented with 10% heat-inactivated fetal bovine serum (FBS) and 1% penicillin/streptomycin at 37°C, 5% CO₂. Cells were treated with Arecaidine but-2-ynyl ester tosylate (0.01μM–1mM) for 24 hours. |
Reaction Conditions | 0.01μM–1mM; 24h. |
Applications | Arecaidine but-2-ynyl ester tosylate significantly inhibits cell viability, proliferation, clonogenicity, and migratory capacity in breast cancer cells. Arecaidine but-2-ynyl ester tosylate induces cell cycle arrest in MDA-MB-231 cells and promotes apoptotic cell death in MCF-7 cells. Arecaidine but-2-ynyl ester tosylate downregulates the expression of key proliferation- and cell cycle-associated genes, including CCND1, CDK6, and MKI67. |
| Animal experiment [2]: | |
Animal models | Male ICR mice |
Preparation Method | Mice received an intrathecal injection of Arecaidine but-2-ynyl ester tosylate (0.3, 1, 3, 10, 30nmol/mouse in 0.5μl) 5 minutes before the induction of local inflammation via zymosan injection into a preformed subcutaneous air pouch. Leukocyte migration into the pouch was quantified 4 hours post-zymosan. In a separate immunohistochemical analysis, animals were perfused 4 hours after zymosan injection to assess neuronal activation. |
Dosage form | 0.3, 1, 3, 10, 30nmol/mouse in 0.5μl; i.t.; single injection. |
Applications | Intrathecal Arecaidine but-2-ynyl ester tosylate dose-dependently suppressed zymosan-induced leukocyte migration and selectively increased Fos expression (a marker of neuronal activation) in sympathetic preganglionic neurons of the T7-T11 spinal segments. Arecaidine but-2-ynyl ester tosylate anti-inflammatory effect is mediated by the suppression of spinal GABAB receptor-mediated inhibitory input, leading to the disinhibition of sympathetic preganglionic neurons and subsequent release of anti-inflammatory catecholamines from the adrenal medulla. |
References: | |
| Cas No. | 119630-77-2 | SDF | |
| 化学名 | but-2-yn-1-yl 1-methyl-1,2,5,6-tetrahydropyridine-3-carboxylate 4-methylbenzenesulfonate | ||
| Canonical SMILES | CC#CCOC(C(C1)=CCCN1C)=O.CC2=CC=C(S(O)(=O)=O)C=C2 | ||
| 分子式 | C11H15NO2.C7H8SO3 | 分子量 | 365.44 |
| 溶解度 | Soluble to 100 mM in sterile water | 储存条件 | Store at -20°C |
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| 1 mM | 2.7364 mL | 13.6821 mL | 27.3643 mL |
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| 10 mM | 273.6 μL | 1.3682 mL | 2.7364 mL |
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