Stereoselective blockade of central [3H]5-hydroxytryptamine binding to multiple sites (5-HT1A, 5-HT1B and 5-HT1C) by mianserin and propranolol
- 1 August 1987
- journal article
- research article
- Published by Oxford University Press (OUP) in Journal of Pharmacy and Pharmacology
- Vol. 39 (8), 664-666
- https://doi.org/10.1111/j.2042-7158.1987.tb03452.x
Abstract
The interaction of the enantiomers of mianserin and propranolol with the binding of [3H]5-hydroxytryptamine ([3H]5-HT) to the 5-HT1A, 5-HT1B and 5-HT1C sites, and with the binding of [3H]ketanserin to the 5-HT2 site, has been evaluated in rat brain membranes. A stereoselective interaction at the 5-HT1A, 5-HT1B and 5-HT1C sites was demonstrated for both compounds, with (-)-mianserin being a more potent displacer than (-)–mianserin and (-)-propranolol being more potent than (+)-propranolol. Only mianserin interacted in a stereoselective manner with the 5-HT2 site, (+)-mianserin being the more potent isomer. The stereoselective association of mianserin and propranolol with the 5-HT1A, 5-HT1B and 5-HT1C sites may prove useful in the characterization of these sites.This publication has 11 references indexed in Scilit:
- Identification of Multiple Binding Sites for [3H]5‐Hydroxytryptamine in the Rat CNSJournal of Neurochemistry, 1986
- Species variations in RU 24969 interactions with non-5-HT1A binding sitesEuropean Journal of Pharmacology, 1986
- Identity of inhibitory presynaptic 5-hydroxytryptamine (5-HT) autoreceptors in the rat brain cortex with 5-HT1B binding sitesNaunyn-Schmiedebergs Archiv für experimentelle Pathologie und Pharmakologie, 1986
- Stereoselective blockade at the 5-HT autoreceptor and inhibition of radioligand binding to central 5-HT recognition sites by the optical isomers of methiothepinNeuropharmacology, 1986
- Molecular pharmacology of 5-HT1 and 5-HT2 recognition sites in rat and pig brain membranes: Radioligand binding studies with [3H]5-HT, [3H]8-OH-DPAT, (−)[125I]iodocyanopindolol, [3H]mesulergine and [3H]KetanserinEuropean Journal of Pharmacology, 1985
- Quantitative autoradiographic mapping of serotonin receptors in the rat brain. I. Serotonin-1 receptorsBrain Research, 1985
- Two 5-HT receptors linked to adenylate cyclase in guinea pig hippocampus are discriminated by 5-carboxamidotryptamine and spiperoneEuropean Journal of Pharmacology, 1985
- A microcomputer program for analysis of nucleic acid hybridizatoin dataNucleic Acids Research, 1982
- Presynaptic α-block and inhibition of noradrenaline and 5-hydroxytryptamine reuptake by a series of compounds related to mianserinJournal of Pharmacy and Pharmacology, 1981
- Enzyme changes in neonatal skeletal muscle: effect of thyroid deficiencyAmerican Journal of Physiology-Cell Physiology, 1978