Asimadoline hydrochloride

SKU: orb1302648

Description

Asimadoline hydrochloride

Research Area

Metabolism Research, Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 185951-07-9
• MW: 451.01
• Purity: 98.94%
• Formula: C₂₇H₃₁ClN₂O₂
• SMILES: C(C(N([C@H](CN1CC[C@H](O)C1)C2=CC=CC=C2)C)=O)(C3=CC=CC=C3)C4=CC=CC=C4.Cl
• Target: Opioid Receptor
• Solubility: DMSO:60 mg/mL (133.03 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:5 mg/mL (11.09 mM)

Bioactivity

• Target IC50:
  κ opioid (Guinea pig):5.6 nM (EC50)|κ opioid (human recombinant):1.2 nM (EC50)
• In Vivo:
  The metabolism of Asimadoline is rapid and appears similar in animals and man the absorption rate following oral administration is 80% in rats and >90% in dogs and monkeys. Asimadoline has peripheral anti-inflammatory actions that are partly mediated through an increase in joint fluid substance P level. Treatment with Asimadoline (5 mg/kg/day i.p.) produces marked and sustained) attenuation o the disease with All three-time regime.
• In Vitro:
  The IC50 for Asimadoline binding to μ-opioid receptors is 3 μM and to δ-opioid receptors is 0.7 μM. At high concentration , Asimadoline demonstrates spasmolytic action against 400 μM barium chloride in the rat duodenum IC50 4.2 μM), suggesting that Asimadoline may bloc the Direct stimulant effects of barium on smooth musclee through mechanisms that are not identifie.
• Animal Research:
  Asimadoline (5 mg/kg/day, = 0 per group) or Vehicle (2 L/kg/day, = 0) is administered to DA rats by i.p. injection twice daily (i) durin the Primary inflammatory phase (days 1–3); (ii) onc the disease is established (days 13–21); or (iii) throughou the entire time course (days 1-21). Non-arthritic control animals receive Asimadoline (5 mg/kg/day, = ) or Vehicle (2 L/kg/day, = ) by i.p. injection twice daily. In All cases, disease parameters are assessed. In this experiment the SP content of joint tissue is assessed only afte the rats are killed (day 21.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Disclaimer: For research use only

Alternative Names

diabetic, allodynia, Asimadoline, Asimadoline hydrochloride, Asimadoline Hydrochloride, bowel, EMD61753, EMD-61753, EMD61753 Hydrochloride, EMD-61753 hydrochloride, EMD-61753 Hydrochloride, EMD 61753, EMD 61753 Hydrochloride, Inhibitor, irritable, inhibit, OpioidReceptor, Opioid Receptor, syndrome, κ-opioid receptor, κ-opioid, μ-opioid, δ-opioid

Compound Identifiers

PubChem CID

9846614