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Effects of enkephalins versus opiates on locomotor activity of the horse.

Abstract: The enkephalins are small, pentapeptide neurotransmitter molecules which have reportedly been used in racing horses. In our experiments, D-Ala2-Metenkephalinamide and leucine enkephalin were administered to horses intravenously (IV) and intracisternally (IC). Leucine enkephalin had little effect on locomotor activity by either route at doses of 0.01 mg/Kg or less. Methionine enkephalinamide, an enzyme resistant enkephalin analog, had no significant effect when given IV (0.002 and 0.008 mg/kg). Other experiments involving intracisternal dosing with this long acting form at higher levels (0.005-.011 mg/Kg), elicited an initial increase in locomotor activity, a rise in temperature, a marked increase in blood pressure, hyperventilation, the appearance of a rapid eye blinking reflex, lack of coordination and quivering. In contrast, dosing with fentanyl either IV (0.01) mg/Kg) or Ic (0.0002 mg/Kg) produced a tenfold increase in locomotor activity without accompanying adverse clinical symptoms. The data suggest that very large doses of IV administered enkephalins or their analogs may be necessary to increase locomotor activity but such doses may also elicit a number of less desirable side effect.
Publication Date: 1982-03-01 PubMed ID: 7079572
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  • Comparative Study
  • Journal Article

Summary

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This research examines the effect of enkephalins and opiates on the locomotive behavior of horses, indicating that high dosages of enkephalins might increase locomotor activity but could also have potential negative side effects.

Introduction

  • The study revolves around enkephalins – small neurotransmitter molecules believed to be used in racing horses. The researchers intended to evaluate their impact on the locomotor activity of horses.

Methodology

  • The enkephalins D-Ala2-Metenkephalinamide and leucine enkephalin were administered to the horses through two methods – intravenous injection (IV) and intracisternal (IC).
  • The doses of leucine enkephalin administered were 0.01 mg/Kg or less. The doses of methionine enkephalinamide given were 0.002 and 0.008 mg/kg via IV, and 0.005-.011 mg/Kg through IC method.
  • On the other hand, the opiate fentanyl was administered IV (0.01 mg/Kg) or IC (0.0002 mg/Kg).

Findings

  • Leucine enkephalin showed little effect on the horses’ locomotive activity, regardless of the injection method – IV or IC.
  • Methionine enkephalinamide, an enzyme-resistant enkephalin analog, did not display significant effects when administered through IV. Administering it intracisternally at higher dosage, however, led to a number of physiological responses, including increased locomotor activity, rise in temperature, increase in blood pressure, hyperventilation, and noticeable rapid eye blinking reflex, lack of coordination, and quivering.
  • On the contrary, the use of fentanyl caused a tenfold increase in locomotor activity, with no accompanying negative clinical symptoms.

Conclusion

  • The study suggested that massive doses of IV-administered enkephalins or their analogs might enhance locomotor activity, but they may also incite several less desirable side effects. Further research is needed to study these effects and investigate potential ways to mitigate them.

Cite This Article

APA
Nugent TE, Combie JD, Weld JM, Burns P, Tobin T. (1982). Effects of enkephalins versus opiates on locomotor activity of the horse. Res Commun Chem Pathol Pharmacol, 35(3), 405-419.

Publication

ISSN: 0034-5164
NlmUniqueID: 0244734
Country: United States
Language: English
Volume: 35
Issue: 3
Pages: 405-419

Researcher Affiliations

Nugent, T E
    Combie, J D
      Weld, J M
        Burns, P
          Tobin, T

            MeSH Terms

            • Animals
            • Blinking / drug effects
            • Blood Pressure / drug effects
            • Body Temperature / drug effects
            • Endorphins / pharmacology
            • Enkephalin, Leucine
            • Enkephalin, Methionine / analogs & derivatives
            • Enkephalins / pharmacology
            • Female
            • Fentanyl / pharmacology
            • Horses / physiology
            • Morphine / pharmacology
            • Motor Activity / drug effects
            • Respiration / drug effects

            Citations

            This article has been cited 1 times.
            1. Toll L, Bruchas MR, Calo' G, Cox BM, Zaveri NT. Nociceptin/Orphanin FQ Receptor Structure, Signaling, Ligands, Functions, and Interactions with Opioid Systems. Pharmacol Rev 2016 Apr;68(2):419-57.
              doi: 10.1124/pr.114.009209pubmed: 26956246google scholar: lookup