ASIMADOLINE

CAS NO.：153205-46-0
Empirical Formula: C27H30N2O2
Molecular Weight: 414.54
MDL number: MFCD00925628
SAFETY DATA SHEET (SDS)
Update Date: 2024-10-23 13:36:13

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