1. GPCR/G Protein
    Neuronal Signaling
  2. Opioid Receptor
  3. Asimadoline

Asimadoline (Synonyms: EMD-61753)

Cat. No.: HY-107384 Purity: 99.36%
Handling Instructions

Asimadoline is a potent κ opioid receptor agonist with IC50s of 5.6 and 1.2 nM for guinea pig and human recombinant κ opioid receptor, respectively.

For research use only. We do not sell to patients.

Asimadoline Chemical Structure

Asimadoline Chemical Structure

CAS No. : 153205-46-0

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Based on 1 publication(s) in Google Scholar

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Description

Asimadoline is a potent κ opioid receptor agonist with IC50s of 5.6 and 1.2 nM for guinea pig and human recombinant κ opioid receptor, respectively.

IC50 & Target

IC50: 5.6 nM (guinea pig κ opioid), 1.2 nM (human recombinant κ opioid)[1]

In Vitro

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 IC50, suggesting no relevant antihistaminergic, antiserotonergic or anticholinergic effects. 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[1].

In Vivo

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[1]. Treatment with Asimadoline (5 mg/kg/day i.p.) produces marked (and sustained) attenuation of the disease with all three time regimes[2].

Clinical Trial
Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 103.3 mg/mL (249.19 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4123 mL 12.0616 mL 24.1231 mL
5 mM 0.4825 mL 2.4123 mL 4.8246 mL
10 mM 0.2412 mL 1.2062 mL 2.4123 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Animal Administration
[2]

Rats: Asimadoline (5 mg/kg/day, n=10 per group) or vehicle (2 mL/kg/day, n=10) is administered to DA rats by i.p. injection twice daily (i) during the primary inflammatory phase (days 1–3); (ii) once the disease is established (days 13–21); or (iii) throughout the entire time course (days 1-21). Non-arthritic control animals receive Asimadoline (5 mg/kg/day, n=5) or vehicle (2 mL/kg/day, n=5) 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 after the rats are killed (day 21)[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

414.54

Formula

C₂₇H₃₀N₂O₂

CAS No.

153205-46-0

SMILES

O[[email protected]]1CCN(C1)C[[email protected]](C2=CC=CC=C2)N(C)C(C(C3=CC=CC=C3)C4=CC=CC=C4)=O

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Room temperature in continental US; may vary elsewhere

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Product Name:
Asimadoline
Cat. No.:
HY-107384
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Asimadoline

Cat. No.: HY-107384