Spiradoline Explained

Spiradoline (U-62066) is a drug which acts as a highly selective κ-opioid agonist.^[1] It has analgesic,^[2] diuretic,^[3] and antitussive effects,^[4] and produces subjective effects in animals similar to those of ketazocine and alazocine.^[5] 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.^[6]

See also

• Enadoline

Notes and References

1. Vonvoigtlander PF, Lewis RA . Analgesic and mechanistic evaluation of spiradoline, a potent kappa opioid . The Journal of Pharmacology and Experimental Therapeutics . 246 . 1 . 259–62 . July 1988 . 2839665 .
2. Kunihara M, Ohyama M, Nakano M, Hayashi S . Analgesic activity of spiradoline mesylate (U-62,066E), a kappa opioid agonist in mice . Life Sciences . 45 . 13 . 1191–8 . 1989 . 2796604 . 10.1016/0024-3205(89)90508-0 .
3. Yamada K, Imai M, Yoshida S . Mechanism of diuretic action of U-62,066E, a kappa opioid receptor agonist . European Journal of Pharmacology . 160 . 2 . 229–37 . January 1989 . 2547626 . 10.1016/0014-2999(89)90495-0 .
4. Kamei J, Tanihara H, Kasuya Y . Antitussive effects of two specific kappa-opioid agonists, U-50,488H and U-62,066E, in rats . European Journal of Pharmacology . 187 . 2 . 281–6 . October 1990 . 2272363 . 10.1016/0014-2999(90)90014-w .
5. Holtzman SG . Further characterization of the discriminative stimulus effects of spiradoline . Pharmacology, Biochemistry, and Behavior . 66 . 3 . 517–22 . July 2000 . 10899364 . 10.1016/s0091-3057(00)00172-6 . 27712517 .
6. Wadenberg ML . A review of the properties of spiradoline: a potent and selective kappa-opioid receptor agonist . CNS Drug Reviews . 9 . 2 . 187–98 . 2003 . 12847558 . 6741666 . 10.1111/j.1527-3458.2003.tb00248.x .