The antinociceptive action of etorphine in the dorsal horn is due to a direct spinal action and not to activation of descending inhibition.
1--Etorphine, microinjected into the brainstem or administered intravenously, inhibited the firing of dorsal horn neurones to noxious heat in spinal or non-spinal anaesthetized cats and in decerebrate, non-anaesthetized cats with intact spinal cords. 2--Small doses of etorphine sometimes caused facilitation, especially when the cord was intact, but this was invariably followed by inhibition at higher doses. 3--The ED50 for inhibition (mean 3.9 micrograms/kg) after microinjection into nucleus raphe magnus, nucleus reticularis magnocellularis or the lateral tegmental field was similar at all sites in anaesthetized, non-spinal cats. 4--The ED50 for microinjection was not increased by spinal transection in anaesthetized cats (mean ED50, 2.6 micrograms/kg) and was similar to the ED50 in decerebrate, non-anaesthetized cats. 5--Intravenous administration was 2 to 3 times more effective than microinjection and the time course of inhibition was faster after intravenous administration than after microinjection. 6--It is concluded that etorphine inhibits dorsal horn neurones after microinjection or intravenous administration by a direct action on the spinal cord and not by activating a descending inhibition. After microinjection it rapidly enters the general circulation and subsequently distributes into the spinal cord. 7--It is also concluded that naloxone readily gains entry to the circulation from the brain because microinjection antagonized the effects of systemic etorphine on dorsal horn neurones in spinal cats.
D000700:Analgesics; D000818:Animals; D002415:Cats; D003655:Decerebrate State; D005048:Etorphine / Q000494:pharmacology*; D005260:Female; D006358:Hot Temperature; D008297:Male; D008845:Microinjections; D009019:Morphinans / Q000494:pharmacology*; D009270:Naloxone / Q000494:pharmacology; D009433:Neural Inhibition / Q000187:drug effects; D013126:Spinal Nerve Roots / Q000187:drug effects*; D013238:Stereotaxic Techniques
D000700:Analgesics; D009019:Morphinans; D009270:Naloxone; D005048:Etorphine