A potent κ-opioid receptor agonist (IC50s = 5.6 and 1.2 nM for guinea pig and human receptors

Asimadoline – 1 mg

Brand:
Cayman
CAS:
153205-46-0
Storage:
-20
UN-No:
Non-Hazardous - /

Asimadoline is a potent κ-opioid receptor (KOR) agonist (IC50s = 5.6 and 1.2 nM for guinea pig and human receptors, respectively).{47150} It is 501- and 498-fold selective for κ-opioid over μ- and δ-opioid receptors, respectively. Asimadoline is spasmolytic in isolated rat duodenum (IC50 = 4.2 μM) and inhibits spontaneous contractions of isolated rat uterus (IC50 = 12.7 μM). In vivo, asimadoline reduces joint damage in a rat model of arthritis induced by complete Freund’s adjuvant (CFA). Asimadoline (25 mg/kg) also reduces the abdominal withdrawal reflex in a model of visceral pain induced by colonic distension in wild-type, but not KOR-/-, mice.{47151}  

 

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SKU: 26411 - 1 mg Category:

Description

A potent κ-opioid receptor agonist (IC50s = 5.6 and 1.2 nM for guinea pig and human receptors, respectively); is 501- and 498-fold selective for κ-opioid over μ- and δ-opioid receptors, respectively; is spasmolytic in isolated rat duodenum (IC50 = 4.2 μM) and inhibits spontaneous contractions of isolated rat uterus (IC50 = 12.7 μM); reduces joint damage in a rat model of CFA-induced arthritis; reduces the abdominal withdrawal reflex in a model of visceral pain induced by colonic distension in wild-type mice at 25 mg/kg

Formal name: N-[(1S)-2-[(3S)-3-hydroxy-1-pyrrolidinyl]-1-phenylethyl]-N-methyl-α-phenyl-benzeneacetamide

Synonyms:  EMD 61753

Molecular weight: 414.5

CAS: 153205-46-0

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Agonists||Research Area|Immunology & Inflammation|Autoimmunity|Rheumatoid Arthritis||Research Area|Neuroscience|Pain Research

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