5-Hydroxytryptamine and dopamine transport by rat and human blood platelets

British Journal of Pharmacology
J L Gordon, H J Olverman

Abstract

1 Uptake of 5-hydroxytryptamine (5-HT) by rat platelets in plasma was very rapid and diffusion did not contribute significantly at substrate concentrations that did not saturate the active transport.2 Under conditions which allowed measurement of initial rates of uptake, kinetic analysis revealed a high affinity uptake mechanism for 5-HT (K(m) = 0.7 muM).3 Uptake of dopamine was relatively slow and involved a lower affinity (K(m) = 70 muM) active transport process. Diffusion contributed significantly at concentrations that did not saturate the active transport.4 5-HT competitively inhibited uptake of dopamine, and vice versa; K(i) values for both amines were similar to their respective K(m) values for uptake.5 Chlorimipramine, desmethylimipramine and benztropine were tested as uptake inhibitors. Each was equipotent against 5-HT and dopamine, although the absolute potency of the drugs varied greatly. Chlorimipramine was the most potent (K(i)## 100 nM), and kinetic analysis revealed that the inhibition was competitive against both 5-HT and dopamine.6 Similar results were obtained in studies with human platelets: K(m) values for 5-HT and dopamine were about 1 muM and 100 muM respectively. Activity profiles of inhibitors were also ...Continue Reading

References

Feb 1, 1992·Naunyn-Schmiedeberg's Archives of Pharmacology·R Wölfel, K H Graefe
Jul 1, 1981·Agents and Actions·O Lingjaerde, O Kildemo
Feb 5, 1981·Clinica Chimica Acta; International Journal of Clinical Chemistry·J M Feldman, J A Davis
May 5, 1981·Clinica Chimica Acta; International Journal of Clinical Chemistry·R C Arora, H Y Meltzer
Jan 31, 1990·Clinica Chimica Acta; International Journal of Clinical Chemistry·B DeanD L Copolov
Jun 4, 1987·European Journal of Pharmacology·M H Pietraszek, W Buczko
Dec 7, 1989·European Journal of Pharmacology·B Dean, D L Copolov
Oct 1, 1984·The Journal of Surgical Research·R A PrinzJ Wallenga
Jul 15, 1996·Thrombosis Research·D PawlakM Mysliwiec
Sep 1, 1996·Thrombosis Research·J MalyszkoM Mysliwiec
Jan 1, 1983·Progress in Neuro-psychopharmacology & Biological Psychiatry·A Rotman
Jan 1, 1983·Comparative Biochemistry and Physiology. C, Comparative Pharmacology and Toxicology·H J Olverman, D F Sharman
Jan 1, 1993·Biomedicine & Pharmacotherapy = Biomédecine & Pharmacothérapie·M A Barradas, D P Mikhailidis
Apr 1, 1997·Atherosclerosis·C C Smith, D J Betteridge
Mar 1, 1994·British Journal of Haematology·A McNicolJ M Gerrard
Jan 1, 1984·Clinical and Experimental Pharmacology & Physiology·P H Lee, M Y Chan
Apr 1, 1979·British Journal of Pharmacology·M Graf, A Pletscher
Jun 5, 2014·Journal of Clinical Biochemistry and Nutrition·Madoka ShimizuYukio Nagasaki
Feb 1, 1994·European Journal of Clinical Investigation·D J BetteridgeC C Smith
May 1, 1985·Journal of Cellular Physiology·W J ArmitageC J Hunt
Jun 1, 1989·European Journal of Clinical Investigation·C C SmithD J Betteridge
Oct 1, 1980·The British Journal of Psychiatry : the Journal of Mental Science·R C Arora, H Y Meltzer
Nov 1, 1989·The British Journal of Psychiatry : the Journal of Mental Science·J FlaskosA J George
Oct 1, 1981·Acta Pharmacologica Et Toxicologica·R Malmgren
Feb 1, 1985·Scandinavian Journal of Haematology·S CortellazzoG de Gaetano

Citations

Sep 1, 1976·The Journal of Pharmacy and Pharmacology·M WieloszS Garattini
Jul 1, 1975·The Biochemical Journal·A H Drummond, J L Gordon
Apr 1, 1976·British Journal of Pharmacology·A H Drummond, J L Gordon
Jan 1, 1973·Progress in Neurobiology·J N Sneddon
Sep 1, 1969·Clinical Pharmacology and Therapeutics·W B Abrams, H M Solomon
Nov 1, 1970·Clinical Pharmacology and Therapeutics·H M SolomonW B Abrams
Jan 1, 1968·British Journal of Pharmacology and Chemotherapy·A Pletscher
Aug 1, 1953·The Biochemical Journal·M DIXON
Jun 11, 1959·The Journal of Physiology·G V BORN, R E GILLSON
Dec 1, 1964·International Journal of Neuropharmacology·Z FUKSL S SCHANKER
Jun 1, 1961·British Journal of Pharmacology and Chemotherapy·R S Stacey

Related Concepts

Study
Dopaminergic Agents
Diffusion Weighted Imaging
Serotonin
Inhibitors
Uptake
Pharmacologic Substance
Neuronal
Dopamine
Plasma

Related Feeds

Basal Ganglia

Basal Ganglia are a group of subcortical nuclei in the brain associated with control of voluntary motor movements, procedural and habit learning, emotion, and cognition. Here is the latest research.