| Identification | Back Directory | [Name]
ASIMADOLINE | [CAS]
153205-46-0 | [Synonyms]
EMD 61753
ASIMADOLINE
Asimadoline (EMD-61753
EMD-61753;EMD61753;EMD 61753
N-((S)-2-((S)-3-Hydroxypyrrolidin-1-yl)-1-phenylethyl)-N-methyl-2,2-diphenylacetamide
Benzeneacetamide, N-[(1S)-2-[(3S)-3-hydroxy-1-pyrrolidinyl]-1-phenylethyl]-N-methyl-α-phenyl-
N-[(1S)-2-[(3S)-3-Hydroxy-1-pyrrolidinyl]-1-phenylethyl]-N-methyl-alpha-phenylbenzeneacetamide | [Molecular Formula]
C27H30N2O2 | [MDL Number]
MFCD00925628 | [MOL File]
153205-46-0.mol | [Molecular Weight]
414.54 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [Uses]
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. | [target]
IC50: 5.6 nM (guinea pig κ opioid), 1.2 nM (human recombinant κ opioid) |
|
| Company Name: |
Moltt Biocem Co., Ltd.
|
| Tel: |
+86-21-38682181 15900741819 |
| Website: |
www.approvedhomemanagement.com/ShowSupplierProductsList15856/0.htm |
|