ASIMADOLINE
- CAS NO.：153205-46-0
- Empirical Formula: C27H30N2O2
- Molecular Weight: 414.54
- MDL number: MFCD00925628
- SAFETY DATA SHEET (SDS)
- Update Date: 2026-01-05 11:31:08
What is ASIMADOLINE?
The Uses of ASIMADOLINE
Acimadolin is a K-opioid agonist that raises the sensitivity threshold in patients with irritable bowel syndrome (IBS), barely crosses the blood-brain barrier, and is well tolerated. It cannot significantly improve the pain threshold of patients, Can significantly reduce pain intensity.
Biological Activity
Asimadoline (EMD-61753) is an orally active, selective, peripherally active κ-opioid agonist with IC50s of 5.6 nM and 1.2 nM for guinea pig and human recombinant κ-opioid, respectively. It has low permeability to the blood-brain barrier and has peripheral anti-inflammatory effects. Also Asimadoline improves allodynia in diabetic rats and has potential for irritable bowel syndrome (IBS) research.
in vitro
Asimadoline (EMD-61753) has high selectively in κ: μ: δ opioid binding ratios of 1:501:498 in human recombinant receptors. The IC 50 for Asimadoline binding to μ -opioid receptors is 3 μM and to δ-opioid receptors is 0.7 μM. The IC 50 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.
It has affinity to sodium and L type Ca 2+ ion channels at IC 50 concentrations 150 to 800 fold the IC 50 for the κ receptors.
At high concentrations, Asimadoline demonstrates spasmolytic action against 400 μM barium chloride in the rat duodenum (IC 50 =4.2 μM), suggesting that Asimadoline may block the direct stimulant effects of barium on smooth muscle through mechanisms that are not identified.
in vivo
Asimadoline (EMD-61753; 1, 5, 15 mg/kg; sc) 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.
Properties of ASIMADOLINE
| Boiling point: | 605.8±55.0 °C(Predicted) |
| Density | 1.170±0.06 g/cm3(Predicted) |
| storage temp. | 2-8°C |
| solubility | DMSO: 103 mg/ml |
| form | A crystalline solid |
| pka | 14.79±0.20(Predicted) |
| color | White to off-white |
Safety information for ASIMADOLINE
| Signal word | Warning |
| Pictogram(s) |
 Environment GHS09 |
| GHS Hazard Statements |
H410:Hazardous to the aquatic environment, long-term hazard |
| Precautionary Statement Codes |
P273:Avoid release to the environment. P391:Collect spillage. Hazardous to the aquatic environment |
Computed Descriptors for ASIMADOLINE
New Products
4-Iodo-3,5-dimethylbenzonitrile 2-fluoro-4-iodoaniline 2-(3-Methyl-1,2,4-oxadiazol-5-yl)acetic acid (as potassium salt) 6,6'-methylenebis(9-methyl-3-((2-methyl-1H-imidazol-1-yl)methyl)-2,3-dihydro-1H-carbazol-4(9H)-one) 3-Bromo-2-fluorobenzoic acid Quinuclidine-4-carbonitrile N,N CARBONYL DIIMIDAZOLE 2-Amino-5-bromo-4-(trifluoromethyl)pyridine（RM for Indian lab) (RS)-beta-Amino-beta-(4-bromophenyl)propionic acid Tetrabutylammonium perchlorate N,O-Dimethylhydroxylamine hydrochloride (R)-1-Benzyl-3-pyrrolidinecarbonitrile Bupropian related compound F Lantanoprost rc B Clidinium Bromide Impurity Noradrenaline EP Impurity D/Noradrenaline Methyl Ether Cetirizine EP Impurity A/Cetirizine CBHP Impurity N-Nitroso hydroxy Cetrizine EP Impurity-A 4-(5-amino-1-methyl-1h-benzoimidazol-2-yl)-butyric acid isopropyl ester. 1,4-bis(methylsulfonyl)butane 4-Cyano-N-Methacryloyl-3-Trifluoromethyl Aniline 5-Methyl-1,3-benzenediacetonitrile 4-Fluorothiophenol 1-methyl amino-2,4-dinitro benzeneRelated products of tetrahydrofuran
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