Identity of inhibitory presynaptic 5-hydroxytryptamine (5-HT) autoreceptors in the rat brain cortex with 5-HT1B binding sites

  title={Identity of inhibitory presynaptic 5-hydroxytryptamine (5-HT) autoreceptors in the rat brain cortex with 5-HT1B binding sites},
  author={Georg Engel and Manfred Göthert and Daniel Hoyer and E Schlicker and K. Hillenbrand},
  journal={Naunyn-Schmiedeberg's Archives of Pharmacology},
Summary1.In rat brain cortex slices preincubated with [3H]5-HT, the potencies of 17 5-HT receptor agonists to inhibit the electrically evoked3H overflow and the affinities of 13 antagonists (including several β-adrenoceptor blocking agents) to antagonize competitively the inhibitory effect of unlabelled 5-HT on evoked3H overflow were determined.2.The affinities of the compounds for 5-HT1B and 5-HT2 binding sites in rat brain cortex membranes (labelled by [125I]cyanopindolol = [125I]-CYP in the… 
The pharmacological properties of the presynaptic serotonin autoreceptor in the pig brain cortex conform to the 5-HT1D receptor subtype
The pig brain cortical 5-HT autoreceptor probably belongs to the 5- HT1D subtype and was excluded by the low potency of mianserin as an antagonist and, in particular, by the ineffectiveness of the5-HT1c receptor antagonist mesulergine.
5-HT1A-receptors mediate stimulation of adenylate cyclase in rat hippocampus
Data support the concept that 5-HT stimulated adenylate cyclase activity in rat hippocampus is mediated by a5-HT1A receptor, as pharmacologically characterised with a series of agonists and antagonists of various structural classes.
Serotonin autoreceptor in rat hippocampus: Pharmacological characterization as a subtype of the 5-HT1 receptor
5-HT nerve terminals of rat hippocampus possess autoreceptors which appear to belong to the 5-HT1B subtype, which is characterized pharmacologically in terms of 5- HT receptor subtype by using superfused synaptosomes depolarized with 15 mM KCl.
A 5-HT7 Heteroreceptor-Mediated Inhibition of [3H]Serotonin Release in Raphe Nuclei Slices of the Rat: Evidence for a Serotonergic–Glutamatergic Interaction
It is suggested that the axon terminals of the glutamatergic cortico-raphe neurons may possess 5-HT7 receptors that inhibit glutamate release, which consequently leads to decreased activity of serotonergic neurons and thus may serve as heteroreceptors in regulation of 5- HT release in the raphe nuclei.
Inhibition of noradrenaline release via presynaptic 5-HT1B receptors of the rat vena cava
The results suggest that the inhibitory presynaptic 5-HT receptors on the sympathetic nerve terminals of the rat vena cava appear to belong to the5-HT1B subtype, which may act as a partial agonist at these receptors, as it does at the facilitatory prosynaptic β-adrenoceptors.
Inhibitory presynaptic 5-hydroxytryptamine (5-HT) receptors on the sympathetic nerves of the human saphenous vein
It is suggested that both 5-HT and 8-OH-DPAT inhibit noradrenaline release by activating inhibitory 5- HT receptors on the sympathetic nerves of the human saphenous vein.
Facilitation of serotonin (5-HT) release in the rat brain cortex by cAMP and probable inhibition of adenylate cyclase in 5-HT nerve terminals by presynaptic α2-adrenoceptors
The present results suggest that the serotoninergic nerve terminals in the rat brain cortex are endowed with an adenylate cyclase, which is negatively coupled to the presynaptic α2-adrenoceptors, but is not linked to the Presynaptic autoreceptors.
Identification of presynaptic 5-HT1 autoreceptors in pig brain cortex synaptosomes and slices
The present results suggest that the serotoninergic nerve fibres of the pig brain cortex are endowed with presynaptic 5- HT1 receptors, which can be activated by endogenous and exogenous 5-HT.
5.HT1 receptors in the vertebrate brain
The regional distribution of high affinity [33H]5-HT recognition sites in the brain of several vertebrates (pigeon, rat, mouse, guinea-pig, cat, dog, monkey and human) was analyzed using in vitro autoradiography and suggested that the majority of 5-HT1 sites belong to the 5- HT1D subtype in the pigeon brain.
Modulation of 5-hydroxytryptamine release by presynaptic inhibitory α2-adrenoceptors in the human cerebral cortex
It is concluded that release-inhibiting adrenoceptors of the α2-subtype exist on 5-hydrpxytryptamine terminals innervating the cerebral cortex in human and guinea-pig brain.


Evidence for common pharmacological properties of [3H]5-hydroxytryptamine binding sites, presynaptic 5-hydroxytryptamine autoreceptors in CNS and inhibitory presynaptic 5-hydroxytryptamine receptors on sympathetic nerves
The results are compatible with the suggestion that there may exist even more than two subtypes of [3H]5-HT1 binding sites in the rat brain cortex and inhibitory presynaptic 5-HT receptors on sympathetic nerve endings in the canine saphenous vein possess common pharmacological properties.
Comparison of the pharmacological characteristics of 5 HT1 and 5 HT2 binding sites with those of serotonin autoreceptors which modulate serotonin release
Results demonstrate that the 5HT autoreceptor and the 5 HT1 binding site have similar pharmacological characteristics and it is suggested that 5 HT autoreceptors and the5 HT1binding site may be related 5 HT receptor sites.
8-Hydroxy-2-(di-n-propylamino) tetralin is devoid of activity at the 5-hydroxytryptamine autoreceptor in rat brain. Implications for the proposed link between the autoreceptor and the [3H] 5-HT recognition site
  • D. Middlemiss
  • Biology
    Naunyn-Schmiedeberg's Archives of Pharmacology
  • 2004
Experiments have failed to provide direct evidence for agonist activity of 8-OH-DPAT at the 5-HT autoreceptor and alternative explanations must be sought for its biochemical and behavioural effects in vivo.
Characterization of the receptor subtype involved in alpha-adrenoceptor-mediated modulation of serotonin release from rat brain cortex slices
The results suggest that the α-adrenoceptors on the serotoninergic nerve fibres belong to the α2-subtype, which is similar to that of the noradrenaline subtype.
Identification of presynaptic serotonin autoreceptors using a new ligand: 3H-PAT
3H-PAT seems to be a useful ligand for studying the biochemical and pharmacological characteristics of presynaptic autoreceptors in selected regions of rat brain.