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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.
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