Structure-antinociceptive activity of neurotensin and some novel analogues in the periaqueductal gray region of the brainstem
| Autor: | Nayef R.F. Al-Rodhan, Kiyoko S. Kanba, Judith A. Gilbert, Elliott Richelson, Al Nelson, Michael A. Pfenning, Daniel J. McCormick, Tony L. Yaksh, Eric W. Larson |
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| Rok vydání: | 1991 |
| Předmět: |
Microinjections
Central nervous system Stimulation Pharmacology In Vitro Techniques Periaqueductal gray chemistry.chemical_compound Neuroblastoma Structure-Activity Relationship medicine Reaction Time Tumor Cells Cultured Animals Humans Periaqueductal Gray Receptors Neurotensin Neurotransmitter metabolism Neurotensin receptor Receptor Molecular Biology Cyclic GMP Neurotensin Analgesics Chemistry General Neuroscience digestive oral and skin physiology Rats Inbred Strains Rats Receptors Neurotransmitter medicine.anatomical_structure Nociception Female Neurology (clinical) Neuroscience hormones hormone substitutes and hormone antagonists Developmental Biology Brain Stem |
| Zdroj: | Brain research. 557(1-2) |
| ISSN: | 0006-8993 |
| Popis: | Neurotensin, an endogenous tridecapeptide, produces a potent, naloxone-insensitive antinociceptive response when it is microinjected into the periaqueductal gray region of the rat brainstem. In the present study, the ED50 for neurotensin in inducing antinociception was 1.5 nmol, two times more potent than morphine. We sought to find whether neurotensin's antinociceptive effects were mediated by the same receptor that mediates its other functions. We found that the structure-activity relationship of neurotensin-induced antinociception was different from that required for the stimulation of intracellular cyclic GMP production in neuroblastoma clone N1E-115 and the binding to N1E-115 cells, human brain tissue, or rat periaqueductal gray. These data suggest there exists a subtype of neurotensin receptors in neural tissue that mediates its antinociceptive actions. |
| Databáze: | OpenAIRE |
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