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

Asimadoline hydrochloride (Synonyms: EMD-61753 hydrochloride)

Cat. No.: HY-107384A Purity: 99.80%
Handling Instructions

Asimadoline (EMD-61753) hydrochloride 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 hydrochloride has low permeability across the blood brain barrier and has peripheral anti-inflammatory actions. Asimadoline hydrochloride 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 hydrochloride Chemical Structure

Asimadoline hydrochloride Chemical Structure

CAS No. : 185951-07-9

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10 mM * 1 mL in DMSO USD 92 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

Asimadoline (EMD-61753) hydrochloride 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 hydrochloride has low permeability across the blood brain barrier and has peripheral anti-inflammatory actions. Asimadoline hydrochloride 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) hydrochloride has high selectively in κ: μ: δ opioid binding ratios of 1:501:498 in human recombinant receptors. The IC50 for Asimadoline hydrochloride 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 hydrochloride 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 hydrochloride demonstrates spasmolytic action against 400 µM barium chloride in the rat duodenum (IC50=4.2 µM), suggesting that Asimadoline hydrochloride 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 hydrochloride; 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 hydrochloride is rapid and appears similar in animals and man. Asimadoline hydrochloride has peripheral anti-inflammatory actions that are partly mediated through increase in joint fluid substance P levels[1].
Treatment with Asimadoline hydrochloride (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

451.00

Formula

C₂₇H₃₁ClN₂O₂

CAS No.
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 : 240 mg/mL (532.15 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2173 mL 11.0865 mL 22.1729 mL
5 mM 0.4435 mL 2.2173 mL 4.4346 mL
10 mM 0.2217 mL 1.1086 mL 2.2173 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: ≥ 6 mg/mL (13.30 mM); Clear solution

  • 2.

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

    Solubility: ≥ 6 mg/mL (13.30 mM); Clear solution

  • 3.

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

    Solubility: ≥ 6 mg/mL (13.30 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Asimadoline hydrochloride
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