trimethyl-[4-(2-oxopyrrolidin-1-yl)but-2-ynyl]azanium:iodide

Description

Oxotremorine M is a non-selective muscarinic (M) acetylcholine receptor agonist that induces phosphoinositide hydrolysis in mouse ileum isolated from wild-type, M₂, M₃, and M₂/M₃ knockout mice (EC₅₀s = 0.36, 0.52, 1.62, and 1.48 μM, respectively). It also increases M₄-induced inhibition of calcium currents in NG108-15 mouse neuroblastoma X rat glioma hybrid cells (EC₅₀ = 0.14 μM). Oxotremorine M inhibits KCNQ2/3 potassium currents in Xenopus oocytes expressing M₁ receptors and KCNQ2/3 potassium channels (IC₅₀ = 1.1 μM). It also directly inhibits KCNQ2/3 potassium channels, decreasing KCNQ2/3 potassium currents in Xenopus oocytes lacking muscarinic receptors in a dose-dependent manner.

Uses

Oxotremorine M is a muscarinic receptor agonist.

in vivo

storage

Desiccate at -20°C

References

[1] JOHN A TRAN F J E Minoru Matsui. Differential coupling of muscarinic M1, M2, and M3 receptors to phosphoinositide hydrolysis in urinary bladder and longitudinal muscle of the ileum of the mouse.[J]. Journal of Pharmacology and Experimental Therapeutics, 2006, 318 2: 649-656. DOI: 10.1124/jpet.106.103093
[2] M.P. CAULFIELD  D. A B. Pharmacology of the putative M4 muscarinic receptor mediating Ca-current inhibition in neuroblastoma × glioma hybrid (NG 108–15) cells[J]. British Journal of Pharmacology, 1991, 104 1: 39-44. DOI: 10.1111/j.1476-5381.1991.tb12381.x
[3] RUUD ZWART. A novel muscarinic receptor-independent mechanism of KCNQ2/3 potassium channel blockade by Oxotremorine-M[J]. European journal of pharmacology, 2016, 791: Pages 221-228. DOI: 10.1016/j.ejphar.2016.08.037