Stereoselective Interaction of Mianserin with 5-HT3 Receptors
| Autor: | D R Thomas, M D Wood, C J Watkins, N R Newberry |
|---|---|
| Rok vydání: | 1993 |
| Předmět: |
Male
Stereochemistry Pharmaceutical Science Mianserin In Vitro Techniques Tritium Granisetron Models Biological Rats Sprague-Dawley Radioligand Assay medicine Animals Drug Interactions Receptor Pharmacology Chemistry Stereoisomerism Vagus Nerve In vitro Rats Kinetics Mechanism of action Receptors Serotonin Stereoselectivity Enantiomer medicine.symptom Selectivity medicine.drug |
| Zdroj: | Journal of Pharmacy and Pharmacology. 45:711-714 |
| ISSN: | 2042-7158 0022-3573 |
| DOI: | 10.1111/j.2042-7158.1993.tb07094.x |
| Popis: | The interaction of the enantiomers of mianserin with the 5-HT3 receptor was determined. Using [3H]granisetron binding, (–)-mianserin was more potent than (+)-mianserin (pKi 8·46 and 6·95, respectively). The enantiomers competitively antagonized the depolarizing effect of 5-hydroxytryptamine in the rat vagus nerve preparation (pKapp: (–)-mianserin 8·13, (+)-mianserin 6·58). This stereoselectivity was maintained in-vivo as determined using ex-vivo inhibition of [3H]granisetron binding. Therefore, in contrast to its enantiomeric selectivity for the 5-HT1C and 5-HT2 receptors, where the (+)-isomer is more potent, the enantiomeric selectivity of mianserin for the 5-HT3 receptor was reversed. This differential selectivity of the enantiomers of mianserin may be useful in elucidating its utility in anxiety states. |
| Databáze: | OpenAIRE |
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