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A κ-opioid agonist drug
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
References
- ^ Vonvoigtlander PF, Lewis RA (July 1988). "Analgesic and mechanistic evaluation of spiradoline, a potent kappa opioid". The Journal of Pharmacology and Experimental Therapeutics. 246 (1): 259–62. PMID 2839665.
- ^ Kunihara M, Ohyama M, Nakano M, Hayashi S (1989). "Analgesic activity of spiradoline mesylate (U-62,066E), a kappa opioid agonist in mice". Life Sciences. 45 (13): 1191–8. doi:10.1016/0024-3205(89)90508-0. PMID 2796604.
- ^ Yamada K, Imai M, Yoshida S (January 1989). "Mechanism of diuretic action of U-62,066E, a kappa opioid receptor agonist". European Journal of Pharmacology. 160 (2): 229–37. doi:10.1016/0014-2999(89)90495-0. PMID 2547626.
- ^ Kamei J, Tanihara H, Kasuya Y (October 1990). "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. doi:10.1016/0014-2999(90)90014-w. PMID 2272363.
- ^ Holtzman SG (July 2000). "Further characterization of the discriminative stimulus effects of spiradoline". Pharmacology, Biochemistry, and Behavior. 66 (3): 517–22. doi:10.1016/s0091-3057(00)00172-6. PMID 10899364. S2CID 27712517.
- ^ Wadenberg ML (2003). "A review of the properties of spiradoline: a potent and selective kappa-opioid receptor agonist". CNS Drug Reviews. 9 (2): 187–98. doi:10.1111/j.1527-3458.2003.tb00248.x. PMC 6741666. PMID 12847558.
μ-opioid (MOR) |
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δ-opioid (DOR) |
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κ-opioid (KOR) |
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Nociceptin (NOP) |
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Others |
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