Arecaidine propargyl ester (hydrobromide)

Arecaidine propargyl ester is an agonist of M₂ muscarinic acetylcholine receptors (mAChRs).¹ It selectively binds to M₂ over M₁, M₃, M₄, and M₅ mAChRs in CHO cells expressing the human receptors (K_is = 0.0871, 1.23, 0.851, 0.977, and 0.933 µM, respectively). Arecaidine propargyl ester induces contractions in isolated guinea pig atrium (pD₂ = 8.67). It induces apoptosis and the production of reactive oxygen species (ROS) in U87 and U251 glioblastoma cells when used at a concentration of 100 µM.² Arecaidine propargyl ester decreases mean arterial blood pressure in normotensive cats (ED₂₅ = 1.9 nmol/kg).³

WARNING This product is not for human or veterinary use.

1. Scapecchi, S., Matucci, R., Bellucci, C., 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. 49(6), 1925-1931 (2006).

2. Di Bari, M., Tombolillo, B., Conte, C., et al. Cytotoxic and genotoxic effects mediated by M2 muscarinic receptor activation in human glioblastoma cells. Neurochem. Int. 90, 261-270 (2015).

3. Porsius, A.J., and Van Zwieten, P.A. Central action of some cholinergic drugs (arecaidine esters) and nicotine on blood pressure and heart rate of cats. Prog. Brain Res. 47, 131-135 (1977).