Asimadoline

Asimadoline (EMD-61753) is an orally active, selective and peripherally active κ-opioid agonist with IC50s of 5.6 nM (guinea pig) and 1.2 nM (human recombinant) . Asimadoline has low permeability across the blood brain barrier and has peripheral anti-inflammatory actions. Asimadoline ameliorates allodynia in diabetic rats and has the potential for irritable bowel syndrome (IBS) [1][2][3].

Product Specifications

CAS Number

[153205-46-0]

Product Name Alternative

EMD-61753

UNSPSC

12352005

Hazard Statement

H302, H317

Target

Opioid Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

COVID-19-immunoregulation

Field of Research

Metabolic Disease; Inflammation/Immunology; Neurological Disease

Assay Protocol

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

Purity

99.36

Solubility

10 mM in DMSO

Smiles

O[C@H]1CCN(C1)C[C@H](C2=CC=CC=C2)N(C)C(C(C3=CC=CC=C3)C4=CC=CC=C4)=O

Molecular Formula

C27H30N2O2

Molecular Weight

414.54

Precautions

H302, H317

References & Citations

[1]Camilleri M, et al. Asimadoline, a κ-Opioid Agonist, and Visceral Sensation. Neurogastroenterol Motil. 2008 Sep; 20 (9) : 971–979.|[2]Binder W, et al. Involvement of substance P in the anti-inflammatory effects of the peripherally selective kappa-opioid asimadoline and the NK1 antagonist GR205171. Eur J Neurosci. 1999 Jun;11 (6) :2065-72.|[3]C G Jolivalt, et al. Dynorphin A, kappa opioid receptors and the antinociceptive efficacy of asimadoline in streptozotocin-induced diabetic rats. Diabetologia. 2006 Nov;49 (11) :2775-85.