Pharmacological Profile of a Non-peptidic Dual Inhibitor of Neutral Endopeptidase 24.11 and Endothelin-Converting Enzyme
| Autor: | R. D. Ghai, Randy L. Webb, S. Delombaert, Arco Y. Jeng, Angelo J. Trapani |
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| Rok vydání: | 1994 |
| Předmět: |
Male
medicine.medical_specialty Mean arterial pressure Kidney Cortex Phenylalanine Molecular Sequence Data Organophosphonates Biophysics Tetrazoles Blood Pressure Endothelin-Converting Enzymes Pharmacology Inhibitory postsynaptic potential Biochemistry Substrate Specificity Atrial natriuretic peptide Rats Inbred SHR Internal medicine medicine Animals Aspartic Acid Endopeptidases Amino Acid Sequence Protein Precursors Molecular Biology Neprilysin chemistry.chemical_classification Endothelin-1 Chemistry Endothelins Cell Membrane Metalloendopeptidases Cell Biology In vitro Rats Kinetics Endocrinology Enzyme Neutral Endopeptidase 24.11 Endothelin receptor Oligopeptides Atrial Natriuretic Factor |
| Zdroj: | Biochemical and Biophysical Research Communications. 204:407-412 |
| ISSN: | 0006-291X |
| DOI: | 10.1006/bbrc.1994.2473 |
| Popis: | CGS 26303 is a potent and structurally unique non-peptidic inhibitor of neutral endopeptidase (NEP) capable of protecting atrial natriuretic peptide (ANP) from enzymatic degradation. In addition, CGS 26303 displays modest endothelin-converting enzyme (ECE) inhibitory activity in vitro. Unlike CGS 24592, a potent but selective NEP inhibitor, CGS 26303 significantly blocks endothelin-1 production in rats after exogenous administration of big ET-1 and reduces the mean arterial pressure in spontaneously hypertensive rats during chronic administration. These results suggest that CGS 26303 represents a new class of therapeutic agents with potential benefits for the treatment of cardiovascular and renal disorders. |
| Databáze: | OpenAIRE |
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