Willem Soudijn

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The present paper reviews the evidence for anxiolytic activity of 5-HT(3) receptor antagonists in animal models of anxiety and in clinical trials in humans. Compared to the established anxiolytics (benzodiazepine receptor agonists and, to a lesser extent, 5-HT(1A) receptor agonists) 5-HT(3) receptor antagonists display a different anxiolytic profile. They(More)
The purpose of the investigation was to develop a pharmacokinetic-pharmacodynamic model for the characterization of the cardiovascular effects of the adenosine A1 receptor agonist N6-cyclopentyladenosine (CPA) in individual normotensive rats. After the i.v. administration of 200 micrograms/kg (0.60 mumol/kg) of CPA, the time course of heart rate and(More)
We have adopted a practical three-step route for the synthesis of 2'- and 3'-deoxy analogues of N6-substituted adenosines: protection of the hydroxyl groups, replacement of the N6-amino by a better leaving group, and combined deprotection and N6-amination in the last step. This route was used to synthesize deoxy analogues of CPA, CHA, and R- and S-PIA. The(More)
An overview is presented on progress made in the research on neuronal transporters of serotonin, dopamine and norepinephrine in the central nervous system. Tools developed by molecular biology, such as expression of cloned transporters, their mutants and chimera in non-neuronal cells offered the opportunity to study the putative domains for binding of(More)
1. The purpose of the present study was to develop an experimental strategy for the quantification of the cardiovascular effects of non-selective adenosine receptor ligands at the adenosine A1 and A2a receptor in vivo. 2-Chloroadenosine (CADO) was used as a model compound. 2. Three groups of normotensive conscious rats received an short intravenous infusion(More)
Allosteric modulation of G protein-coupled receptors has recently been recognized as an alternative approach to gain selectivity in drug action. In this overview, allosteric modulators that enhance or diminish the effects of (endogenous) agonists or antagonists on a variety of G protein-coupled receptors are described. Emphasis is placed on the latest(More)
1. The purpose of the present study was to quantify the cardiovascular effects of the 2'-, 3'-, 5'-deoxyribose analogues of the selective adenosine A1 receptor agonist, N6-cyclopentyladenosine (CPA) in vivo. The blood concentration-effect relationships of the compounds were assessed in individual rats and correlated to their receptor binding(More)
The purpose of the present study was to quantify the in vivo potency of the selective adenosine A2a antagonist CSC [8-(3-chlorostyryl)caffeine]. Four groups of conscious, normotensive rats received a continuous i.v. infusion of 0, 6, 12 and 24 micrograms/min/kg of CSC. During a steady-state infusion of CSC, the animals received 1000 micrograms/kg of the(More)