High-affinity neuropeptide Y receptor antagonists
| Autor: | Johann Leban, Marilyn Jansen, A Tadepalli, Antonio Landavazo, Dennis Heyer, W Harrington, Andrew Spaltenstein, O H Viveros, R J Slepetis, Alejandro J. Daniels, J E Matthews |
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| Jazyk: | angličtina |
| Rok vydání: | 1995 |
| Předmět: |
Male
medicine.medical_specialty Swine Molecular Sequence Data Biology Kidney Calcium in biology Cell Line Rats Sprague-Dawley Norepinephrine Neuroblastoma Structure-Activity Relationship In vivo Internal medicine mental disorders medicine Tumor Cells Cultured Animals Humans Neuropeptide Y Amino Acid Sequence Receptor Mammals Multidisciplinary Kidney metabolism Brain Biological activity Neuropeptide Y receptor humanities Rats Receptors Neuropeptide Y Kinetics Endocrinology Organ Specificity Calcium Leukemia Erythroblastic Acute Rabbits Peptides Ex vivo medicine.drug Research Article |
| Popis: | Neuropeptide Y (NPY) is one of the most abundant peptide transmitters in the mammalian brain. In the periphery it is costored and coreleased with norepinephrine from sympathetic nerve terminals. However, the physiological functions of this peptide remain unclear because of the absence of specific high-affinity receptor antagonists. Three potent NPY receptor antagonists were synthesized and tested for their biological activity in in vitro, ex vivo, and in vivo functional assays. We describe here the effects of these antagonists inhibiting specific radiolabeled NPY binding at Y1 and Y2 receptors and antagonizing the effects of NPY in human erythroleukemia cell intracellular calcium mobilization perfusion pressure in the isolated rat kidney, and mean arterial blood pressure in anesthetized rats. |
| Databáze: | OpenAIRE |
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