Spiradoline

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]

Spiradoline
Clinical data
Routes of
administration		N/A
ATC code
  • none
Identifiers
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
UNII
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC22H30Cl2N2O2
Molar mass425.39 g·mol−1
3D model (JSmol)
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See also

References
  1. 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.
  2. 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.
  3. 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.
  4. 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.
  5. 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.
  6. 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.
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