The effects of dihydropyridine calcium antagonists on heme biosynthesis in chick embryo liver cell culture
| Autor: | D. R. Goldman, Gerald S. Marks, M. E. Lyon, S. A. McCluskey, E. P. Sutherland |
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| Rok vydání: | 1986 |
| Předmět: |
medicine.medical_specialty
Porphyrins animal structures Nifedipine Physiology Nicardipine Chick Embryo Heme Biology Hepatic porphyria Structure-Activity Relationship Nitrendipine Physiology (medical) Internal medicine medicine Animals Cells Cultured Pharmacology Liver cell Dihydropyridine Biological activity General Medicine Calcium Channel Blockers Kinetics Endocrinology Liver Cell culture embryonic structures medicine.drug |
| Zdroj: | Canadian Journal of Physiology and Pharmacology. 64:438-443 |
| ISSN: | 1205-7541 0008-4212 |
| DOI: | 10.1139/y86-070 |
| Popis: | A variety of 1,4-dihydropyridine calcium antagonists were tested for porphyrinogenic activity in chick embryo liver cell culture. 3,5-Dimethoxycarbonyl-1,4-dihydro-2,6-dimethyl-4-(ortho-nitrophenyl)pyridine (nifedipine) was shown to be a potent porphyrinogenic agent. This activity was shared by a number of related analogues, viz., the 4-phenyl, 4-(meta-nitrophenyl), 4-(para-nitrophenyl), 4-(ortho-methoxyphenyl), 4-(meta-trifluoromethylphenyl), and 4-(para-trifluoromethylphenyl) analogues and nitrendipine; nicardipine exhibited very weak activity. The porphyrinogenic potency of the 1,4-dihydropyridines did not parallel their calcium antagonist activity. Nifedipine did not exhibit ferrochelatase-lowering activity in chick embryo liver cell culture and uroporphyrin and heptacarboxylic acid porphyrin were the major porphyrins to accumulate. Nifedipine did not cause suicidal destruction of cytochrome P-450 in chick embryo hepatic microsomes. Because nifedipine possesses comparable porphyrinogenic activity to sodium secobarbital in chick embryo liver cell culture, caution is required if nifedipine or related drugs are administered to patients with hereditary hepatic porphyria. |
| Databáze: | OpenAIRE |
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