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

Asimadoline (Synonyms: EMD-61753)

Cat. No.: HY-107384
Handling Instructions

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).

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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Solution
10 mM * 1 mL in DMSO USD 92 Ask For Quote & Lead Time
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10 mg USD 156 Ask For Quote & Lead Time
25 mg USD 372 Ask For Quote & Lead Time

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Description

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].

IC50 & Target

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

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[1].
Asimadoline has affinity to sodium and L type Ca2+ ion channels at IC50 concentrations 150 to 800 fold the IC50 for the κ receptors[1].
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].

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

In Vivo

Asimadoline (EMD-61753; 1, 5, 15 mg/kg; s.c.) acutely ameliorates both formalin-evoked hyperalgesia and tactile allodynia in diabetic rats[3].
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].

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

Animal Model: Adult female Sprague-Dawley rats[3]
Dosage: 1, 5, 15 mg/kg
Administration: SC; single dose
Result: Acutely ameliorated both formalin-evoked hyperalgesia and tactile allodynia in diabetic rats.
Clinical Trial
Molecular Weight

414.54

Formula

C27H30N2O2

CAS No.
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

Shipping

Room temperature in continental US; may vary elsewhere.

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 : ≥ 100 mg/mL (241.23 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.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.03 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (6.03 mM); Suspended solution; Need ultrasonic

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.03 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation
References
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Asimadoline
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