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ChemicalBook--->CAS DataBase List--->185951-07-9

185951-07-9

185951-07-9 Structure

185951-07-9 Structure
IdentificationBack Directory
[Name]

Asimadoline-HCl
[CAS]

185951-07-9
[Synonyms]

Asimadoline-HCl
EMD-61753 hydrochloride
Asimadoline hydrochloride
Asimadoline Hydrochlorine
N-[(1S)-2-[(3S)-3-hydroxypyrrolidin-1-yl]-1-phenylethyl]-N-methyl-2,2-diphenylacetamide
[Molecular Formula]

C27H30N2O2
[MDL Number]

MFCD28987467
[MOL File]

185951-07-9.mol
[Molecular Weight]

414.539
Chemical PropertiesBack Directory
[storage temp. ]

Store at -20°C
[solubility ]

DMSO: 240 mg/mL (532.15 mM)
[form ]

Solid
[color ]

Off-white to light yellow
Hazard InformationBack Directory
[Uses]

Asimadoline Hydrochlorine is used in the treatment of IBS, a disorder associated with pain and altered bowel function.
[Biological Activity]

Asimadoline is a potent and selective K-opioid agonist th at does not penetrate the blood-brain barrier. Asimadoline produces both analgesic and antidiarrheal effects.
[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].

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.
[IC 50]

κ Opioid Receptor/KOR
Spectrum DetailBack Directory
[Spectrum Detail]

Asimadoline-HCl(185951-07-9)1HNMR
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