Detail of "137433-06-8"

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Differential effects of LY235959, a competitive antagonist of the NMDA receptor on k-opioid receptor agonist induced responses in mice and rats

Differential effects of LY235959, a competitive antagonist of the NMDA receptor on k-opioid receptor agonist induced responses in mice and rats. Bhargava, Hemendra N.; Thorat, Sanjay N. (Department of Pharmaceutics and Pharmacodynamics (M/C 865), The University of Illinois at Chicago, Health Sciences Center, 833 South Wood Street, Chicago, IL 60612, USA). Brain Research, 747(2), 246-251 (English) 1997 Elsevier. CODEN: BRREAP. ISSN: 0006-8993. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) The effects of the competitive antagonist of the N-methyl-D-aspartate (NMDA) receptor, LY235959, were detd. on the analgesic and hypothermic effects as well as on the development of tolerance to these effects of U-50,488H, a k-opioid receptor agonist in mice and rats. In the mouse, a single injection of LY235959 given 10 min prior to U-50,488H did not modify the analgesic action of the latter. Similarly, chronic administration of LY235959 twice a day for 4 days did not modify U-50,488H-induced analgesia in mice. Repeated pretreatment of mice with LY235959 dose-dependently attenuated the development of tolerance to the analgesic actions of U-50,488H. In the rat, LY235959 by itself produced a significant analgesia and prior treatment of rats with LY235959 enhanced the analgesic action of U-50,488H. Similar effects were seen with the hypothermic action. Pretreatment of rats with LY235959 attenuated the development of tolerance to the analgesic but not to the hypothermic action of U-50,488H. 83913-06-8 and 137433-06-8 which are cas registry numbers of chemicals are mentioned. These results provide evidence that LY235959 produces differential actions on nociception and thermic responses by itself and when given acutely with U-50,488H in mice and rats. However, when the animals are pretreated with LY235959, similar inhibitory effects are obsd. on the development of tolerance to the analgesic action of U-50,488H in both the species. These studies demonstrate an involvement of the NMDA receptor in the development of k-opioid tolerance and suggest that the biochem. consequences of an opioid's interaction with the opioid receptor are not the only factors that contribute to the acute and chronic actions of opioid analgesic drugs. .

Effects of competitive and noncompetitive antagonists of the N-methyl-D-aspartate receptor on the analgesic action of d1- and d2-opioid receptor agonists in mice

Effects of competitive and noncompetitive antagonists of the N-methyl-D-aspartate receptor on the analgesic action of d1- and d2-opioid receptor agonists in mice.Some chemicals with cas registry numbers like 137433-06-8 and 88373-73-3 are also used. Bhargava, Hemendra N.; Zhao, Guo-Min (Health Sci. Cent., Univ. Illinois Chicago, Chicago, IL 60612, USA). British Journal of Pharmacology, 119(8), 1586-1590 (English) 1996 Stockton. CODEN: BJPCBM. ISSN: 0007-1188. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) 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-Pen2,D-Pen5]enkephalin (DPDPE) and [D-Ala2,Glu4] deltorphin II (deltorphin II), the putative d1- and d2-opioid receptor agonists, resp., were detd. in the male Swiss-Webster mice. Intracerebroventricular administration of DPDPE or deltorphin II produced analgesia. MK-801 administered i.p. 10 min before the injection of DPDPE or deltorphin II, dose-dependently antagonized the analgesic actions of both drugs. LY 235959 also dose-dependently antagonized the analgesic actions of DPDPE and deltorphin II. The effects of MK-801 and LY 235959 on the binding of [3H]-DPDPE to mouse brain membranes were also detd. Neither of the NMDA receptor antagonists had any effect on the binding of [3H]-DPDPE. It is concluded that competitive and noncompetitive antagonists of the NMDA receptor antagonize the analgesic action of d1- and d2-opioid receptor agonists and that such effects are not mediated via a direct interaction with brain d-opioid receptors. .