A potent κ-opioid receptor agonist
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Asimadoline

Item No. 26411

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[(1S)-2-[(3S)-3-hydroxy-1-pyrrolidinyl]-1-phenylethyl]-N-methyl-α-phenyl-benzeneacetamide
CAS Number
153205-46-0
Synonyms
  • EMD 61753
Molecular Formula
C27H30N2O2
Formula Weight
414.5
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: 103 mg/ml
SMILES
O=C(N([C@H](CN1C[C@@H](O)CC1)C2=CC=CC=C2)C)C(C3=CC=CC=C3)C4=CC=CC=C4
InChi Code
InChI=1S/C27H30N2O2/c1-28(25(21-11-5-2-6-12-21)20-29-18-17-24(30)19-29)27(31)26(22-13-7-3-8-14-22)23-15-9-4-10-16-23/h2-16,24-26,30H,17-20H2,1H3/t24-,25+/m0/s1
InChi Key
JHLHNYVMZCADTC-LOSJGSFVSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $36

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    5 mg

    $120

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    10 mg

    $219

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    25 mg

    $462

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    Product Description

    Asimadoline is a potent κ-opioid receptor (KOR) agonist (IC50s = 5.6 and 1.2 nM for guinea pig and human receptors, respectively).1 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.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Camilleri, M. Asimadoline, a κ-opioid agonist, and visceral sensation. Neurogastroenterol. Motil. 20(9), 971-979 (2008).

    2. Larsson, M.H., Bayati, A., Lindström, E., et al. Involvement of kappa-opioid receptors in visceral nociception in mice. Neurogastroenterol. Motil. 20(10), 1157-1164 (2008).