Asimadoline

SKU: orb1222652

Description

Asimadoline is a proprietary small molecule therapeutic. Asimadoline was originally developed to treat peripheral pain such as arthritis. Asimadoline is an orally administered agent that acts as a kappa opioid receptor agonist. It has shown encouraging clinical efficacy for the treatment of IBS in a barostat study in IBS patients and has the potential for treating other gastrointestinal diseases.

Key Properties

• CAS Number: 153205-46-0
• MW: 414.54
• Purity: >98% (HPLC)
• Formula: C₂₇H₃₀N₂O₂
• SMILES: CN([C@H](CN1CC[C@@H](C1)O)C2=CC=CC=C2)C(=O)C(C3=CC=CC=C3)C4=CC=CC=C4
• Target: DNA/RNA Synthesis
• Solubility: DMSO : ≥ 103.3 mg/mL; 249.19 mM

Bioactivity

• In Vivo:
  Asimadoline (EMD-61753; 1, 5, 15 mg/kg; s. c.) acutely ameliorates both formalin-evoked hyperalgesia and tactile allodynia in diabetic rats. The absorption rate following oral administration is 80% in rats and >90% in dogs and monkeys. The metabolism of Asimadoline is rapid and appears similar in animals and man. Asimadoline has peripheral anti-inflammatory actions that are partly mediated through increase in joint fluid substance P levels. Treatment with Asimadoline (5 mg/kg/day; i.p.) produces marked (and sustained) attenuation of the disease with all three time regimes. Animal model: Adult female Sprague-Dawley rats. Dosage: 1, 5, 15 mg/kg. Administration: SC; single dose. Result: Acutely ameliorated both formalin-evoked hyperalgesia and tactile allodynia in diabetic rats.
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• In Vitro:
  Asimadoline (EMD-61753) has high selectively in κ: μ: δ opioid binding ratios of 1: 501: 498 in human recombinant receptors. The IC50 for Asimadoline binding to μ-opioid receptors is 3 μM and to δ-opioid receptors is 0.7 μM. The IC50 values for D1, D2, kainate, σ, PCP/NMDA, H1, α1, α2, M1/M2, glycine, 5HT1A, 5HT1C, 5HT1D, 5HT2, 5HT3, AMPA and kainate/AMPA receptors are all >10 μM. Asimadoline has affinity to sodium and L type Ca2+ ion channels at IC50 concentrations 150 to 800 fold the IC50 for the κ receptors. At high concentrations, Asimadoline demonstrates spasmolytic action against 400 μM barium chloride in the rat duodenum (IC50 = 4.2 μM), suggesting that Asimadoline may block the direct stimulant effects of barium on smooth muscle through mechanisms that are not identified.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Asimadoline

Quick Database Links

Gene Symbol

DNA/RNA Synthesis