Iperoxo

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. Iperoxo can be used for direct probing activation-related conformational transitions of muscarinic receptors when labeled with tritium[1][2].

Product Specifications

CAS Number

[247079-84-1]

UNSPSC

12352005

Hazard Statement

H315, H319, H335

Target

MAChR

Type

Reference compound

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/iperoxo.html

Purity

99.48

Solubility

DMSO : 62.5 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

C[N+](C)(C)CC#CCOC1=NOCC1.[I-]

Molecular Formula

C10H17IN2O2

Molecular Weight

324.16

Precautions

H315, H319, H335

References & Citations

[1]Schrage R, et, al. Agonists with supraphysiological efficacy at the muscarinic M2 ACh receptor. Br J Pharmacol. 2013 May;169 (2) :357-70.|[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.|[3]Kruse AC, et al., Activation and allosteric modulation of a muscarinic acetylcholine receptor. Nature. 2013 Dec 5;504 (7478) :101-6.|[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.