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Iperoxo is a potent superagonist of muscarinic acetylcholine receptor (mAChR) that activates M1, M2 and M3 receptors with pEC50 of 9.87, 10.1 and 9.78. [3H]Iperoxo can be used for direct probing activation-related conformational transitions of muscarinic receptors[1][2]. Iperoxo is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Iperoxo forms an important building block for the class of G protein-coupled receptors modulators. Iperoxo specifically binds to the orthosteric site of the muscarinic acetylcholine receptor. It has a higher efficacy than the endogenous agonist acetylcholine.

mAChR2: 10.1 (pEC₅₀); mAChR1: 9.87 (pEC₅₀); mAChR3: 9.78 (pEC₅₀)

[1] Schrage R, et, al. Agonists with supraphysiological efficacy at the muscarinic M2 ACh receptor. Br J Pharmacol. 2013 May;169(2):357-70. DOI:10.1111/bph.12003
[2] Schrage R, et, al. New insight into active muscarinic receptors with the novel radioagonist [3H]iperoxo. Biochem Pharmacol. 2014 Aug 1;90(3):307-19. DOI:10.1016/j.bcp.2014.05.012
[3] Kruse AC, et al., Activation and allosteric modulation of a muscarinic acetylcholine receptor. Nature. 2013 Dec 5;504(7478):101-6. DOI:10.1038/nature12735
[4] Matera C, et al., Bis(ammonio)alkane-type agonists of muscarinic acetylcholine receptors: synthesis, in vitro functional characterization, and in vivo evaluation of their analgesic activity. Eur J Med Chem. 2014 Mar 21;75:222-32. DOI:10.1016/j.ejmech.2014.01.032