The novel kappa-opioid receptor agonist TRK-820 suppresses the rewarding and locomotor-enhancing effects of morphine in mice

Life Sci. 2001 Mar 2;68(15):1717-25. doi: 10.1016/s0024-3205(01)00957-2.

Abstract

The effects of the novel kappa-opioid receptor agonist TRK-820 on the rewarding and locomotor-enhancing effects of morphine were investigated in mice. Morphine (1-5 mg/kg, s.c.) caused a dose-related preference for the drug-associated place. In contrast, TRK-820 (0.003-0.03 mg/kg, s.c.) did not produce a significant preference for either compartment of the test box. In combination studies, co-injection of TRK-820 (0.01 and 0.03 mg/kg, s.c.) with morphine significantly suppressed the morphine (5 mg/kg, s.c.)-induced place preference, and this effect of TRK-820 was antagonized by pretreatment with nor-BN1 (3 mg/kg, s.c.), a selective kappa-opioid receptor antagonist. TRK-820 also suppressed morphine-induced hyperlocomotion, and this suppression was also blocked by nor-BNI. These results suggest that TRK-820 suppresses the rewarding and locomotor-enhancing effects of morphine through the activation of kappa-opioid receptors. Thus, we propose that TRK-820 may be useful for controlling pain while reducing undesirable side-effects.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Dose-Response Relationship, Drug
  • Male
  • Mice
  • Morphinans / pharmacology*
  • Morphine / pharmacology*
  • Motor Activity / drug effects*
  • Naltrexone / analogs & derivatives*
  • Naltrexone / pharmacology
  • Narcotics / pharmacology*
  • Receptors, Opioid, kappa / agonists*
  • Reward
  • Spiro Compounds / pharmacology*

Substances

  • Morphinans
  • Narcotics
  • Receptors, Opioid, kappa
  • Spiro Compounds
  • TRK 820
  • norbinaltorphimine
  • Naltrexone
  • Morphine