Premium
Effects of competitive and noncompetitive antagonists of the N‐methyl‐D‐aspartate receptor on the analgesic action of δ 1 ‐ and δ 2 ‐opioid receptor agonists in mice
Author(s) -
Bhargava Hemendra N.,
Zhao GuoMin
Publication year - 1996
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1111/j.1476-5381.1996.tb16076.x
Subject(s) - nmda receptor , analgesic , enkephalin , chemistry , pharmacology , competitive antagonist , opioid receptor , receptor , antagonist , receptor antagonist , agonist , opioid , medicine , biochemistry
1 The effects of MK‐801, a noncompetitive antagonist of the N‐methyl‐D‐aspartate (NMDA) receptor and LY 235959, a competitive antagonist of the NMDA receptor on the analgesic actions of [D‐Pen 2 , D‐Pen 5 ]enkephalin (DPDPE) and [D‐Ala 2 , Glu 4 ] deltorphin II (deltorphin II), the putative δ 1 ‐ and δ 2 ‐opioid receptor agonists, respectively, were determined in the male Swiss‐Webster mice. 2 Intracerebroventricular administration of DPDPE or deltorphin II produced analgesia. MK‐801 administered intraperitoneally 10 min before the injection of DPDPE or deltorphin II, dose‐dependently antagonized the analgesic actions of both drugs. 3 LY 235959 also dose‐dependently antagonized the analgesic actions of DPDPE and deltorphin II. 4 The effects of MK‐801 and LY 235959 on the binding of [ 3 H]‐DPDPE to mouse brain membranes were also determined. Neither of the NMDA receptor antagonists had any effect on the binding of [ 3 H]‐DPDPE. 5 It is concluded that competitive and noncompetitive antagonists of the NMDA receptor antagonize the analgesic action of δ 1 ‐ and δ 2 ‐opioid receptor agonists and that such effects are not mediated via a direct interaction with brain δ‐opioid receptors.