35516-99-5
Chemical Structure
Arecaidine-propargyl ester
- CAS No.: 35516-99-5
- Formula:C10H13NO2
- Molecular Weight:179.22
InChIKey: SPHRJZBOFYIKMC-UHFFFAOYSA-N
SMILES: O=C(C1=CCCN(C1)C)OCC#C
Biological Activity: Arecaidine-propargyl ester is a selective M2 muscarinic receptor agonist with blood-brain barrier permeability, with a pKi of 5.91 for hm1, 7.06 for hm2, 6.07 for hm3, 6.01 for hm4, and 6.03 for hm5. Arecaidine-propargyl ester stimulates central and peripheral muscarinic receptors. Arecaidine-propargyl ester increases intracellular ROS, induces DNA damage and Apoptosis, and upregulates the expression of MnSOD and SIRT1. Arecaidine-propargyl ester reduces sympathetic nerve outflow, induces dose-dependent hypotension, and triggers negative chronotropic effects at high peripheral doses. Arecaidine-propargyl ester can be used in research related to Alzheimer's disease and glioblastoma[1][2][3].
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Arecaidine-propargyl ester | Arecaidine-propargyl ester is a selective M2 muscarinic receptor agonist with blood-brain barrier permeability, with a pKi of 5.91 for hm1, 7.06 for hm2, 6.07 for hm3, 6.01 for hm4, and 6.03 for hm5. Arecaidine-propargyl ester stimulates central and peripheral muscarinic receptors. Arecaidine-propargyl ester increases intracellular ROS, induces DNA damage and Apoptosis, and upregulates the expression of MnSOD and SIRT1. Arecaidine-propargyl ester reduces sympathetic nerve outflow, induces dose-dependent hypotension, and triggers negative chronotropic effects at high peripheral doses. Arecaidine-propargyl ester can be used in research related to Alzheimer's disease and glioblastoma. | |||||||||||||||||||||
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- [1]. Porsius AJ, et al. Central action of some cholinergic drugs (arecaidine esters) and nicotine on blood pressure and heart rate of cats. Prog Brain Res. 1977;47:131-5. [Content Brief]
- [2]. Scapecchi S, et al. Highly chiral muscarinic ligands: the discovery of (2S,2'R,3'S,5'R)-1-methyl-2-(2-methyl-1,3-oxathiolan-5-yl)pyrrolidine 3-sulfoxide methyl iodide, a potent, functionally selective, M2 partial agonist. J Med Chem. 2006 Mar 23;49(6):1925-31. [Content Brief]
- [3]. Di Bari M, et al. Cytotoxic and genotoxic effects mediated by M2 muscarinic receptor activation in human glioblastoma cells. Neurochem Int. 2015;90:261-270. [Content Brief]
Keywords
