β-Adrenergic activities of octopamine and synephrine stereoisomers on guinea-pig atria and trachea
| Autor: | C. Mohan Thonoor, Clyde M. Williams, Roy Jordan, John M. Midgley |
|---|---|
| Rok vydání: | 1987 |
| Předmět: |
Male
medicine.medical_specialty Adrenergic receptor Adrenergic beta-Antagonists Guinea Pigs Pharmaceutical Science In Vitro Techniques Guinea pig chemistry.chemical_compound Internal medicine Receptors Adrenergic beta medicine Animals Potency Octopamine Pharmacology Synephrine β adrenergic Heart Muscle Smooth Stereoisomerism Octopamine (drug) Adrenergic beta-Agonists Orders of magnitude (mass) Guinea pig atria Trachea Endocrinology chemistry medicine.drug |
| Zdroj: | Journal of Pharmacy and Pharmacology. 39:752-754 |
| ISSN: | 2042-7158 0022-3573 |
| DOI: | 10.1111/j.2042-7158.1987.tb06986.x |
| Popis: | The activities of the (-)- and (+)-forms of m- and p-octopamine and m- and p-synephrine on β1- and β2- adrenoceptors in guinea-pig atria and trachea have been compared with that of noradrenaline. The rank order of potency of the (-)-forms on β1-adrenoceptors was noradrenaline > m-synephrine. m-octopamine = p-octopamine > p-synephrine. m-Synephrine was 100-fold, m-and p-octopamine about 6000-fold, and p-synephrine about 40 000-fold less active than noradrenaline. The (+)-forms were 1-2 orders of magnitude less active than their (-)-counterparts. The four (-)-compounds were more than four orders of magnitude less active than noradrenaline on β2,-adrenoceptors, and the (+)-forms had no detectable activity in concentrations as high as 10−4 M. If m-and p-octopamine are co-released with noradrenaline in amounts proportional to their concentration, their activities at these structures are too low to be physiologically significant. |
| Databáze: | OpenAIRE |
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