Spiradoline (U-62066) is a drug which acts as a highly selective κ-opioid agonist. It has analgesic,diuretic and antitussive effects, and produces subjective effects in animals similar to those of ketocyclazocine and allylnormetazocine. The main effect in humans is sedation, along with analgesic and diuretic effects, but significant side effects such as dysphoria and hallucinations have stopped it from being used clinically. Kappa-agonists have been shown to react negatively with the Mu-receptor, instead of having an assumed synergy since they are both opiate receptors, such as with the Mu and Delta receptors(which both mediate pain-relief, euphoria(mainly Mu) and overall potency of Opiate/Opioid effects).

Spiradoline synthesis.png

Kaplan, L. J.; 1984, U.S. Patent 4,588,591.




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