PK 11195, an antagonist of peripheral type benzodiazepine receptors, modulates BAY K8644 sensitive but not β- or H2-receptor sensitive voltage operated calcium channels in the guinea pig heart
| Autor: | Gervais Neliat, G. Le Fur, C. Gueremy, Marie-Christine Dubroeucq, Adam Doble, Andre Uzan, T. Carriot, M. Mestre, Christian Renault |
|---|---|
| Rok vydání: | 1986 |
| Předmět: |
Male
PK-11195 medicine.medical_specialty Nifedipine Guinea Pigs Action Potentials chemistry.chemical_element Stimulation In Vitro Techniques Calcium Pharmacology Ion Channels General Biochemistry Genetics and Molecular Biology chemistry.chemical_compound Neurotransmitter receptor Internal medicine Receptors Adrenergic beta medicine Animals Receptors Histamine H2 General Pharmacology Toxicology and Pharmaceutics Receptor Benzodiazepinones Voltage-dependent calcium channel GABAA receptor Isoproterenol General Medicine 3-Pyridinecarboxylic acid 1 4-dihydro-2 6-dimethyl-5-nitro-4-(2-(trifluoromethyl)phenyl)- Methyl ester Papillary Muscles Isoquinolines Receptors GABA-A Myocardial Contraction Bay K8644 Endocrinology chemistry Barium Receptors Histamine Female |
| Zdroj: | Life Sciences. 39:329-339 |
| ISSN: | 0024-3205 |
| DOI: | 10.1016/0024-3205(86)90651-x |
| Popis: | In a partially depolarized guinea pig papillary muscle preparation, BAY K8644 stimulated voltage-operated calcium channels, promoting slow action potentials; this effect was dose-dependent over a concentration range of 3 × 10 −7 M to 3 × 10 −6 M. Isoproterenol and histamine also induced slow action potentials by stimulating β or H 2 receptors, respectively. PK 11195, the antagonist of peripheral type benzodiazepine receptors, inhibited the effect of BAY K8644, but not those of histamine or isoproterenol. Moreover, PK 11195 “dose-dependently” antagonized the ability of R05-4864 to inhibit the slow action potentials elicited by barium chloride. Thus, in the heart, PK 11195, an antagonist of peripheral type benzodiazepine receptors, can modulate voltage-operated calcium channels when they are activated directly, but not when they are activated by stimulation of neurotransmitter receptors. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|