Biomaterial Database

Effects of N-methyl-D-aspartate receptor antagonists on the analgesia and tolerance to D-Ala2, Glu4 deltorphin II, a delta 2-opioid receptor agonist in mice. 1996

H N Bhargava, and G M Zhao

Department of Pharmaceutics and Pharmacodynamics, University of Illinois at Chicago 60612, USA.

The effects of MK-801, a noncompetitive antagonist of the N-methyl-D-aspartate (NMDA) receptor and of LY 235959, a competitive antagonist of the NMDA receptor on the analgesic action and development of tolerance to the analgesic action of D-Ala2, Glu4 deltorphin II (deltorphin II), a delta 2-opioid receptor agonist were determined in mice. Tolerance to deltorphin II was induced in male Swiss-Webster mice by twice daily intracerebroventricular (i.c.v.) injections of the drug (20 micrograms/mouse) for 4 days. To determine the effects of NMDA receptor antagonists, the drugs were injected intraperitoneally in appropriate doses 10 min before each injection of deltorphin II. The doses of MK-801 were 0.01, 0.03 or 0.10 mg/kg whereas those of LY 235959 were 1, 2 or 4 mg/kg. Chronic administration of NMDA receptor antagonists by themselves did not alter the tail-flick latency or the analgesic effect of deltorphin II. MK-801 given concurrently with deltorphin II inhibited the development of tolerance to deltorphin II, the significant effects were observed at 0.03 and 0.10 mg/kg doses. Similar inhibitory effect of development of tolerance to deltorphin II were observed with LY 235959 at 4 mg/kg dose. MK-801 and LY 235959 also antagonized the analgesic action of deltorphin II. It is concluded that antagonism of NMDA receptors attenuates the analgesic action as well as development of tolerance to the analgesic action of delta 2-opioid receptor agonist in the mouse.

UI	MeSH Term	Description	Entries
D007546	Isoquinolines	A group of compounds with the heterocyclic ring structure of benzo(c)pyridine. The ring structure is characteristic of the group of opium alkaloids such as papaverine. (From Stedman, 25th ed)
D008297	Male		Males
D008815	Mice, Inbred Strains	Genetically identical individuals developed from brother and sister matings which have been carried out for twenty or more generations, or by parent x offspring matings carried out with certain restrictions. All animals within an inbred strain trace back to a common ancestor in the twentieth generation.	Inbred Mouse Strains,Inbred Strain of Mice,Inbred Strain of Mouse,Inbred Strains of Mice,Mouse, Inbred Strain,Inbred Mouse Strain,Mouse Inbred Strain,Mouse Inbred Strains,Mouse Strain, Inbred,Mouse Strains, Inbred,Strain, Inbred Mouse,Strains, Inbred Mouse
D009842	Oligopeptides	Peptides composed of between two and twelve amino acids.	Oligopeptide
D004347	Drug Interactions	The action of a drug that may affect the activity, metabolism, or toxicity of another drug.	Drug Interaction,Interaction, Drug,Interactions, Drug
D000701	Analgesics, Opioid	Compounds with activity like OPIATE ALKALOIDS, acting at OPIOID RECEPTORS. Properties include induction of ANALGESIA or NARCOSIS.	Opioid,Opioid Analgesic,Opioid Analgesics,Opioids,Full Opioid Agonists,Opioid Full Agonists,Opioid Mixed Agonist-Antagonists,Opioid Partial Agonists,Partial Opioid Agonists,Agonist-Antagonists, Opioid Mixed,Agonists, Full Opioid,Agonists, Opioid Full,Agonists, Opioid Partial,Agonists, Partial Opioid,Analgesic, Opioid,Full Agonists, Opioid,Mixed Agonist-Antagonists, Opioid,Opioid Agonists, Full,Opioid Agonists, Partial,Opioid Mixed Agonist Antagonists,Partial Agonists, Opioid
D000818	Animals	Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA.	Animal,Metazoa,Animalia
D016194	Receptors, N-Methyl-D-Aspartate	A class of ionotropic glutamate receptors characterized by affinity for N-methyl-D-aspartate. NMDA receptors have an allosteric binding site for glycine which must be occupied for the channel to open efficiently and a site within the channel itself to which magnesium ions bind in a voltage-dependent manner. The positive voltage dependence of channel conductance and the high permeability of the conducting channel to calcium ions (as well as to monovalent cations) are important in excitotoxicity and neuronal plasticity.	N-Methyl-D-Aspartate Receptor,N-Methyl-D-Aspartate Receptors,NMDA Receptor,NMDA Receptor-Ionophore Complex,NMDA Receptors,Receptors, NMDA,N-Methylaspartate Receptors,Receptors, N-Methylaspartate,N Methyl D Aspartate Receptor,N Methyl D Aspartate Receptors,N Methylaspartate Receptors,NMDA Receptor Ionophore Complex,Receptor, N-Methyl-D-Aspartate,Receptor, NMDA,Receptors, N Methyl D Aspartate,Receptors, N Methylaspartate
D016291	Dizocilpine Maleate	A potent noncompetitive antagonist of the NMDA receptor (RECEPTORS, N-METHYL-D-ASPARTATE) used mainly as a research tool. The drug has been considered for the wide variety of neurodegenerative conditions or disorders in which NMDA receptors may play an important role. Its use has been primarily limited to animal and tissue experiments because of its psychotropic effects.	Dizocilpine,MK-801,MK 801,MK801
D017465	Receptors, Opioid, delta	A class of opioid receptors recognized by its pharmacological profile. Delta opioid receptors bind endorphins and enkephalins with approximately equal affinity and have less affinity for dynorphins.	Opioid Receptors, delta,Receptors, delta,Receptors, delta Opioid,delta Receptors,delta Opioid Receptor,delta Receptor,Opioid Receptor, delta,Receptor, delta,Receptor, delta Opioid,delta Opioid Receptors