Quantitative studies of N-methyl-D-aspartate, 2-amino-5- phosphonovalerate and cis-2,3-piperidine dicarboxylate interactions on the neonatal rat spinal cord in vitro
| Autor: | Philip L. Wheatley, Karen J. Collins |
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| Rok vydání: | 1986 |
| Předmět: |
Agonist
medicine.medical_specialty N-Methylaspartate medicine.drug_class Stereochemistry education Population In Vitro Techniques Partial agonist Drug Administration Schedule Membrane Potentials Internal medicine medicine Animals Drug Interactions 2-Amino-5-phosphonovalerate Pharmacology Aspartic Acid education.field_of_study Dose-Response Relationship Drug Chemistry Rats Inbred Strains Valine Rats Electrophysiology Schild regression Endocrinology Animals Newborn Spinal Cord Competitive antagonist Pipecolic Acids Excitatory postsynaptic potential NMDA receptor |
| Zdroj: | European Journal of Pharmacology. 121:257-263 |
| ISSN: | 0014-2999 |
| DOI: | 10.1016/0014-2999(86)90497-8 |
| Popis: | The interactions between N-methyl-D-aspartate (NMDA), (+/-)2-amino-5-phosphonovalerate (2AP5) and (+/-)cis-2.3-piperidine dicarboxylate (cis-PDA) were examined quantitatively in the neonatal rat spinal cord in vitro. NMDA and cis-PDA evoked concentration-dependent motoneuronal depolarizations. The maximal cis-PDA-evoked response was approximately 60% of that evoked by NMDA. When applied in combination with fixed concentrations of cis-PDA, NMDA evoked concentration-dependent depolarizations superimposed upon the basal cis-PDA-evoked depolarizations, the dose-response curve for which intercepted the control dose-response curve and was subsequently moved to the right compared with the control curve. 2AP5 shifted the NMDA dose-response curves to the right and Schild regression analysis gave a pKB of 5.0 with a slope of 1.00. 2AP5 also moved the cis-PDA dose-response-curve (apparent KB 3.1 X 10(-5) M) to the right and abolished the cis-PDA component of the NMDA + cis-DPA dose-response curve. These results are consistent with the predictions of drug-receptor theory for the interactions of a full agonist (NMDA), competitive antagonist (2AP5) and partial agonist (cis-PDA) and represent further evidence for a population of excitatory amino acid receptors for which NMDA is a selective agonist. |
| Databáze: | OpenAIRE |
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