Effects of intrathecal injection of the adenosine receptor agonists R-phenylisopropyl-adenosine and N-ethylcarboxamide-adenosine on nociception and motor function in the rat

Anesth Analg. 1990 Jul;71(1):60-4. doi: 10.1213/00000539-199007000-00010.

Abstract

R-phenylisopropyl-adenosine, which has an affinity for the adenosine A1 receptor higher than that for the A2 receptor, and N-ethylcarboxamide-adenosine, which has near equal affinity for the A1 and A2 receptors, were injected intrathecally into rats to evaluate differences in antinociceptive effect and motor impairment. Using the tail-immersion test, both compounds had antinociceptive effects. Motor function was evaluated during spontaneous movement in a free space. N-ethylcarboxamide-adenosine rapidly impaired motor function even after low intrathecal doses. R-phenylisopropyl-adenosine also induced motor impairment, but only after high intrathecal doses, and onset was much slower. These results suggest that the receptor selectivity of R-phenylisopropyl-adenosine is diminished at higher doses and that the motor impairment is an A2-receptor-mediated effect. A selective A1 receptor agonist, e.g., R-phenylisopropyl-adenosine, which produces a good antinociceptive effect without motor impairment, is more promising as a drug of possible use for the future treatment of clinical pain.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adenosine / analogs & derivatives*
  • Adenosine / pharmacology
  • Adenosine-5'-(N-ethylcarboxamide)
  • Analgesics / pharmacology*
  • Animals
  • Dose-Response Relationship, Drug
  • Injections, Spinal
  • Male
  • Motor Activity / drug effects*
  • Phenylisopropyladenosine / administration & dosage
  • Phenylisopropyladenosine / pharmacology*
  • Rats
  • Rats, Inbred Strains
  • Receptors, Purinergic / drug effects*
  • Vasodilator Agents / pharmacology*

Substances

  • Analgesics
  • Receptors, Purinergic
  • Vasodilator Agents
  • Phenylisopropyladenosine
  • Adenosine-5'-(N-ethylcarboxamide)
  • Adenosine