Effect of antagonism of the NMDA receptor on tolerance to [d-Pen2,d-Pen5]enkephalin, a δ1-Opioid receptor agonist

Peptides ◽  
1996 ◽  
Vol 17 (2) ◽  
pp. 233-236 ◽  
Author(s):  
Guo-Min Zhao ◽  
Hemendra N. Bhargava
1996 ◽  
Vol 76 (3) ◽  
pp. 2093-2096 ◽  
Author(s):  
X. M. Wang ◽  
S. S. Mokha

1. The present study investigated opioid-mediated modulation of N-methyl-D-aspartic acid (NMDA)-evoked responses of trigeminothalamic neurons in the superficial and deeper dorsal horn of the medulla (trigeminal nucleus caudalis) in rats anesthetized with urethane. 2. Microiontophoretic application of NMDA activated 18/19 trigeminothalamic neurons. Administration of [D-Ala2, N-Me-Phe4,Gly5-ol]-Enkephalin, a selective mu-opioid receptor agonist, reduced the NMDA-evoked responses in 77% of trigeminothalamic neurons. [D-Pen2,5]-Enkephalin, a selective delta-opioid receptor agonist, produced inhibition of NMDA-evoked responses in 36% of neurons. 3. We suggest that 1) NMDA-receptor activation excites trigeminothalamic nociceptive neurons and may, therefore, mediate nociceptive transmission in the medullary dorsal horn; and 2) the predominantly inhibitory modulation of NMDA-receptor-mediated responses of nociceptive trigeminothalamic neurons by activation of mu- and delta-opioid receptors may provide a neural mechanism for the antinociceptive actions of opioids.


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