Action of H1and H2Inhibitors on the Response of Histamine Sensitive Adenylyl Cyclase from Guinea-Pig Mucosa
| Autor: | C. V. Perrier, M. Griessen |
|---|---|
| Rok vydání: | 1976 |
| Předmět: |
medicine.medical_specialty
Prostaglandin Antagonists Receptors Drug Guinea Pigs Clinical Biochemistry Mepyramine Biochemistry Cyclase chemistry.chemical_compound Histamine receptor Histamine H2 receptor Burimamide Internal medicine medicine Animals Histamine H4 receptor Pyrilamine Histamine N-methyltransferase Chemistry General Medicine Endocrinology Gastric Mucosa Histamine H1 Antagonists Prostaglandins Female Histamine Adenylyl Cyclases medicine.drug |
| Zdroj: | European Journal of Clinical Investigation. 6:113-120 |
| ISSN: | 1365-2362 0014-2972 |
| DOI: | 10.1111/j.1365-2362.1976.tb00500.x |
| Popis: | In the guinea-pig, it has been shown that homogenates of mucosa from the fundus contain an adenylyl cyclase system that is activated by histamine as well as by prostaglandins PGE1 and PGA1. The effects of burimamide, an H2-inhibitor, and mepyramine and chlorpheniramide, both H1-inhibitors, were tested. Both H1 and H2 inhibitors behaved kinetically as competitive inhibitors of histamine, but the Km derived for burimamide (2.5 - 4.1 . 10(-5)) was significantly lower than that for either chlorpheniramine (0.9 - 1.9 . 10(-4)) or mepyramine (1.3 - 1.4 . 10(-4)). On the other hand none of the three inhibitors influenced the cyclase activation by PGE1 and PGA1. These results suggest that there are at least two types of receptors in the preparation studied, one responsive to histamine and the other to the prostaglandins, and that the specificity of H1- and H2-receptors is not absolute in the broken cell preparation. |
| Databáze: | OpenAIRE |
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