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ASIMADOLINE

Product Name
ASIMADOLINE
CAS No.
153205-46-0
Chemical Name
ASIMADOLINE
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
CBNumber
CB6228855
Molecular Formula
C27H30N2O2
Formula Weight
414.54
MOL File
153205-46-0.mol
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ASIMADOLINE Property

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)
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H410Very toxic to aquatic life with long lasting effects

Precautionary statements

P273Avoid release to the environment.

P391Collect spillage. Hazardous to the aquatic environment

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N-Bromosuccinimide Price

Cayman Chemical
Product number
26411
Product name
Asimadoline
Packaging
5mg
Price
$109
Updated
2024/03/01
Cayman Chemical
Product number
26411
Product name
Asimadoline
Packaging
25mg
Price
$420
Updated
2024/03/01
Cayman Chemical
Product number
26411
Product name
Asimadoline
Packaging
1mg
Price
$32
Updated
2024/03/01
Cayman Chemical
Product number
26411
Product name
Asimadoline
Packaging
10mg
Price
$199
Updated
2024/03/01
ChemScene
Product number
CS-8053
Product name
Asimadoline
Purity
99.36%
Packaging
10mg
Price
$156
Updated
2021/12/16
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ASIMADOLINE Chemical Properties,Usage,Production

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)

ASIMADOLINE Preparation Products And Raw materials

Raw materials

Preparation Products

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ASIMADOLINE Suppliers

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153205-46-0, ASIMADOLINERelated Search:

(R)-(-)-N-METHYL-1-PHENYL-2-(1-PYRROLIDINO)ETHYLAMINE 1,2-Ethanediamine,N2,N2-dimethyl-1-phenyl-,(1S)-(9CI) (3S)-1-(2-AMINOETHYL)-3-PYRROLIDINOL (2'S,3S)-1-(2-METHYLAMINO-2-PHENYL-ETHYL)-PYRROLIDIN-3-OL ASIMADOLINE N-(2-diethylaminoethyl)-2,2-diphenyl-acetamide (S)-ALPHA-PHENYL-1-PYRROLIDINEETHANAMINE Asimadoline Impurity 1

  • ASIMADOLINE
  • N-[(1S)-2-[(3S)-3-Hydroxy-1-pyrrolidinyl]-1-phenylethyl]-N-methyl-alpha-phenylbenzeneacetamide
  • EMD 61753
  • EMD-61753;EMD61753;EMD 61753
  • Asimadoline (EMD-61753
  • Benzeneacetamide, N-[(1S)-2-[(3S)-3-hydroxy-1-pyrrolidinyl]-1-phenylethyl]-N-methyl-α-phenyl-
  • N-((S)-2-((S)-3-Hydroxypyrrolidin-1-yl)-1-phenylethyl)-N-methyl-2,2-diphenylacetamide
  • 153205-46-0
  • C27H30N2O2
  • Pharmaceutical intermediate