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Equine veterinary journal1988; 20(2); 114-118; doi: 10.1111/j.2042-3306.1988.tb01471.x

Dose related effects of the kappa agonist U-50, 488H on behaviour, nociception and autonomic response in the horse.

Abstract: Current opiate receptor theory suggests that kappa agonists should provide good analgesia without producing marked central nervous system stimulation. U-50,488H is an experimental narcotic analgesic that is a selective kappa agonist. In the present study, U-50,488H produced good analgesia in horses using both the skin twitch and hoof withdrawal reflex assays. Further, the analgesia was relatively long lasting (120 mins) compared to other mu-agonists tested in horses. The locomotor response to U-50,488H was less than observed with ethylketazocine and butorphanol, and has yielded the smallest locomotor response of any of the narcotic analgesics tested to date. Other work showed that the autonomic responses to U-50,488H were less than those of other narcotic analgesics, and that the analgesic response to this drug was blocked by naloxone. Based on its ability to produce analgesia with little other stimulatory action, U-50,488H shows promise of becoming a useful narcotic analgesic in equine medicine.
Publication Date: 1988-03-01 PubMed ID: 3286243DOI: 10.1111/j.2042-3306.1988.tb01471.xGoogle Scholar: Lookup
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  • Journal Article
  • Research Support
  • Non-U.S. Gov't

Summary

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The research article investigates the effects of the kappa agonist U-50, 488H on behaviour, nociception, and autonomic response in horses, suggesting it as a prospective analgesic for equine medicine due to its fewer stimulatory actions.

About kappa agonist U-50,488H

  • U-50,488H is an experimental narcotic analgesic that works as a selective kappa agonist. Kappa agonists are considered to provide effective pain relief without causing substantial central nervous system stimulation.
  • This research explored the effects of U-50,488H on horses and found it to provide good and long-lasting analgesia for at least 120 minutes, surpassing the effectiveness of other mu-agonists that were tested on horses.

Effect on locomotor response

  • The researchers assessed the locomotor response of the horses to U-50,488H. The response was notably lower than that observed with other narcotic analgesics, like ethylketazocine and butorphanol.
  • U-50,488H resulted in the least locomotor response among all the narcotic analgesics that were tested, suggesting fewer stimulatory side effects.

Autonomic responses and naloxone

  • The study also indicated that the autonomic responses to U-50,488H were less extreme than those to other narcotic analgesics. Autonomic responses relate to the involuntary functions of the body, such as heart rate or pupil dilation.
  • Furthermore, it was discovered that the analgesic response induced by U-50,488H could be blocked by naloxone, a medication used to reverse the effects of opioids.

Prompting Future Applications

  • Given the analgesic abilities of U-50,488H with fewer stimulatory actions, the researchers proposed that U-50,488H could potentially serve as a useful narcotic analgesic in equine medicine.
  • The findings underscore the need for further exploration and evaluation of U-50,488H for its therapeutic potential in treating pain in horses.

Cite This Article

APA
Kamerling S, Weckman T, Donahoe J, Tobin T. (1988). Dose related effects of the kappa agonist U-50, 488H on behaviour, nociception and autonomic response in the horse. Equine Vet J, 20(2), 114-118. https://doi.org/10.1111/j.2042-3306.1988.tb01471.x

Publication

ISSN: 0425-1644
NlmUniqueID: 0173320
Country: United States
Language: English
Volume: 20
Issue: 2
Pages: 114-118

Researcher Affiliations

Kamerling, S
  • Department of Veterinary Physiology, College of Veterinary Medicine, Louisiana State University, Baton Rouge 70803.
Weckman, T
    Donahoe, J
      Tobin, T

        MeSH Terms

        • 3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cyclohexyl)-benzeneacetamide, (trans)-Isomer
        • Analgesics / pharmacology
        • Animals
        • Autonomic Nervous System / drug effects
        • Body Temperature / drug effects
        • Chemical Phenomena
        • Chemistry
        • Cyclazocine / analogs & derivatives
        • Cyclazocine / pharmacology
        • Dose-Response Relationship, Drug
        • Ethylketocyclazocine
        • Female
        • Fentanyl / pharmacology
        • Heart Rate / drug effects
        • Horses / physiology
        • Locomotion / drug effects
        • Male
        • Nociceptors / drug effects
        • Pupil / drug effects
        • Pyrrolidines / pharmacology
        • Respiration / drug effects

        Citations

        This article has been cited 3 times.
        1. Lesimple C. Indicators of Horse Welfare: State-of-the-Art. Animals (Basel) 2020 Feb 13;10(2).
          doi: 10.3390/ani10020294pubmed: 32069888google scholar: lookup
        2. Mama KR, Pascoe PJ, Steffey EP. Evaluation of the interaction of mu and kappa opioid agonists on locomotor behavior in the horse. Can J Vet Res 1993 Apr;57(2):106-9.
          pubmed: 8490803
        3. Roger T, Bardon T, Ruckebusch Y. Comparative effects of mu and kappa opiate agonists on the cecocolic motility in the pony. Can J Vet Res 1994 Jul;58(3):163-6.
          pubmed: 7954116