N-[(1S)-2-[(3S)-3-Hydroxy-1-pyrrolidinyl]-1-phenylethyl]-N-methyl-alpha-phenylbenzeneacetamide

Name	ASIMADOLINE
Synonyms	EMD61753 EMD-61753 EMD 61753 ASIMADOLINE Asimadoline (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
CAS	153205-46-0

Molecular Formula	C27H30N2O2
Molar Mass	414.54
Density	1.170±0.06 g/cm3(Predicted)
Boling Point	605.8±55.0 °C(Predicted)
pKa	14.79±0.20(Predicted)
Storage Condition	2-8°C
In vitro study	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. Asimadoline 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.

Last Update：2024-01-02 23:10:35

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CAS: 153205-46-0
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N-[(1S)-2-[(3S)-3-Hydroxy-1-pyrrolidinyl]-1-phenylethyl]-N-methyl-alpha-phenylbenzeneacetamide Request for Quotation