Evidence for various tryptamines and related compounds acting as substrates of the platelet 5-hydroxytryptamine transporter

  title={Evidence for various tryptamines and related compounds acting as substrates of the platelet 5-hydroxytryptamine transporter},
  author={Reinhard W{\"o}lfel and Karl Heinz Graefe},
  journal={Naunyn-Schmiedeberg's Archives of Pharmacology},
  • R. Wölfel, K. Graefe
  • Published 1 February 1992
  • Biology
  • Naunyn-Schmiedeberg's Archives of Pharmacology
SummaryThe aim of the present study was to answer the question whether amines other than 5-hydroxytryptamine (5-HT) and tryptamine act as substrates of the platelet 5-HT transporter. To this end, a large number of tryptamines, 5-HT receptor agonists and phenethylamines (which had IC50 values for 3H-5-HT uptake inhibition of 145–24500 nmol l−1) was examined in rabbit platelets in order to determine their ability to induce an outward transport of 3H-5-HT Platelets (the MAO of which was blocked… 
Conclusive evidence for distinct transporters for 5-hydroxytryptamine and noradrenaline in pulmonary endothelial cells of the rat
5-HT uptake in rat lungs occurs, at least predominantly, by a 5-HT transporter which is very similar to or the same as that in other tissues, such as the brain, and provide further evidence for transport of noradrenaline by uptake1.
Regulation of Serotonin Transport in Human Platelets by Tyrosine Kinase Syk
It is concluded that, in addition to the phosphorylation of SERT mediated by various other kinases, also that catalyzed by Syk might play an important role in the 5-HT transport, likely favoring the transporter conformation exposing the neurotransmitter binding sites.
Serotonin (5-HT) Transport in Human Platelets is Modulated by Src-Catalysed Tyr-Phosphorylation of the Plasma Membrane Transporter SERT
It was concluded that the Src-mediated SERT Tyr-phosphorylation regulates the 5-HT transport by affecting the neurotransmitter binding sites.
Anorectic effect and brain concentrations of D-fenfluramine in the marmoset: relationship to the in vivo and in vitro effects on serotonergic mechanisms
Brain concentrations of d-F and d-NF at anorectic doses exceeded the concentrations required in vitro to influence the serotoninergic system and might possibly be explained by an interaction with the 5-HT system.
The recreational tryptamine 5-MeO-DALT (N,N-diallyl-5-methoxytryptamine): A brief review
Inter-relationships of intermediate phenotypes for serotonin function, impulsivity, and a 5-HT2A candidate allele: His452Tyr
Investigating the role of His452Tyr and the 102T>C in behavior and in vivo intermediate biochemical phenotypes found no significant effects of either polymorphism were associated with altered 5-HT-induced calcium response or fenfluramine-stimulated prolactin release.


Effects of imipramine and some tryptamine derivatives on the efflux of 3H-5-hydroxytryptamine from rabbit platelets.
It is concluded that tryptamines that are more effective in releasing 3H-5-HT than imipramine have the property of being substrates of the 5-HT transporter.
On the 5-hydroxytryptamine transport across the plasma membrane of rabbit platelets and its inhibition by imipramine
The results indicate that true initial rates of 3H-5-HT uptake were determined, since the pretreatment with reserpine did not affect any of the kinetic parameters for uptake.
Neurochemical characterization of a new potent and selective serotonin uptake inhibitor: Lu 10-171
  • J. Hyttel
  • Chemistry, Biology
  • 2004
Due to the selective action on 5-HT uptake, Lu 10-171 seems to be a valuable tool in studying the role of central 5- HT neurone systems in experimental neuropharmacology as well as in the ethiology of depressive illness.
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.
Urapidil and some analogues with hypotensive properties show high affinities for 5-hydroxytryptamine (5-HT) binding sites of the 5-HT1A subtype and for α1-adrenoceptor binding sites
5-methyl-urapidil is one of the most potent ligands at 5-HT1A recognition sites known to date and is relevant to the hypotensive properties of these compounds.
Uptake of 5-hydroxytryptamine by platelets.
  • R. S. Stacey
  • Biology, Chemistry
    British journal of pharmacology and chemotherapy
  • 1961
The antagonism of tryptamine was found to be competitive, and the possible site of its action is discussed, as well as a number of other substances on the uptake of 5-hydroxytryptamine by platelets.
Mechanism of imipramine inhibition of platelet 5-hydroxytryptamine transport.
Results are consistent with the proposal that imipramine binds to the substrate site of the 5-hydroxytryptamine transporter but cannot be transported.
Saturable uptake of [3H]-tryptamine in rabbit platelets is inhibited by 5-hydroxytryptamine uptake blockers
Results indicate that [3H]-tryptamine is actively transported through the membrane of blood platelets by the same carrier that transports 5-HT.
Citalopram — Pharmacological profile of a specific serotonin uptake inhibitor with antidepressant activity
  • J. Hyttel
  • Chemistry, Psychology
    Progress in Neuro-Psychopharmacology and Biological Psychiatry
  • 1982
D dopamine is actively transported by platelets via the 5‐HT uptake mechanism, but with a much lower affinity than that in the corpus striatum, and platelets should not be regarded as models for the dopamine transport mechanism found in dopaminergic neurones.