2-Nor-leukotriene analogs: Antagonists of the airway and vascular smooth muscle effects of leukotriene C4, D4 and E4
| Autor: | Barry M. Weichman, M A Wasserman, Barry A. Berkowitz, John G. Gleason, Bogdan Zabko-Potapovich, Thomas W. Ku, Mary E. McCarthy, Ruth R. Osborn, David A. Holden |
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| Rok vydání: | 1983 |
| Předmět: |
Agonist
Vascular smooth muscle medicine.drug_class Guinea Pigs Biophysics In Vitro Techniques Pharmacology Biology Biochemistry Muscle Smooth Vascular Guinea pig Structure-Activity Relationship chemistry.chemical_compound medicine Animals Molecular Biology Structural analog Leukotriene E4 Leukotriene Leukotriene C4 Airway Resistance Cell Biology Anatomy respiratory system chemistry Eicosanoid SRS-A lipids (amino acids peptides and proteins) Muscle Contraction |
| Zdroj: | Biochemical and Biophysical Research Communications. 117:732-739 |
| ISSN: | 0006-291X |
| DOI: | 10.1016/0006-291x(83)91658-3 |
| Popis: | A structural analog of LTD4, 4R-hydroxy-5S-cysteinylglycyl-6Z-nonadecenoic acid (4R, 5S, 6Z-2-nor-LTD1) has been synthesized and pharmacologically characterized. It significantly antagonized the contractile action of LTD4, LTC4 and LTE4 in guinea pig airways. In addition, this compound antagonized the in vitro vasoconstrictive effects of LTD4 in the guinea pig pulmonary artery. The study of a series of structural analogs of 4R, 5S, 6Z-2-nor-LTD1 suggests that the spatial separation of the C-1 (eicosanoid) carboxyl relative to the hydroxyl is a critical determinant in LTD4 agonist/antagonist activity. |
| Databáze: | OpenAIRE |
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