Visualizing Pharmacological Activities of Antidepressants: A Novel Approach



Hieronymus J. Derijks1, 2, Eibert R. Heerdink1, Rob Janknegt2, Fred H.P. De Koning1, 3, Berend Olivier*, 4, Anton J.M. Loonen 5, Antoine C.G. Egberts 1, 6
1 Department of Pharmacoepidemiology and Pharmacotherapy, Utrecht Institute for Pharmaceutical Sciences (UIPS), Utrecht University, P.O. Box 80082, 3508 TB Utrecht, The Netherlands
2 Department of Clinical Pharmacy, Orbis Medical Center, P.O. Box 5500, 6130 MB, Sittard, The Netherlands
3 Kring Apotheken Nederland, P.O. Box 210, 5201 AE Den Bosch, The Netherlands
4 Division of Psychopharmacology, Utrecht Institute for Pharmaceutical Sciences, Faculty of Science, Utrecht University, P.O. Box 80-082, 3508 TB, Utrecht, The Netherlands.
5 Department of Pharmacotherapy and Pharmaceutical Care, Pharmacy and Pharmaceutical Sciences - Faculty of Mathematics and Natural Sciences, Groningen University, Antonius Deusinglaan 1, 9713 AV, Groningen, The Netherlands
6 Department of Clinical Pharmacy, University Medical Center Utrecht, P.O. Box 85500, 3508 GA Utrecht, The Netherlands


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© 2008 Derijks et al.

open-access license: This is an open access article distributed under the terms of the Creative Commons Attribution 4.0 International Public License (CC-BY 4.0), a copy of which is available at: https://creativecommons.org/licenses/by/4.0/legalcode. This license permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited.

* Address correspondence to this author at the Division of Psychopharmacology, Utrecht Institute for Pharmaceutical Sciences, Faculty of Science, Utrecht University, P.O. Box 80-082, 3508 TB, Utrecht, The Netherlands; Tel: +31 302533529; Fax: +31 302531599; E-mail: B.Olivier@uu.nl


Abstract

Antidepressants have different receptor binding profiles, which are related to therapeutic action and adverse drug reactions. We constructed a model to classify antidepressants on the basis of their binding properties of most common transporter- and receptor sites. Receptor binding was quantified by calculating receptor occupancy for the 5-HT (serotonin) reuptake transporter, norepinephrinic reuptake transporter, 5-HT2C-receptor, M3-receptor, H1-receptor and 􀀁1- receptor. To identify groups of antidepressants that show similar patterns of receptor occupancy for different receptors, hierarchical cluster analysis (HCA) and principle component analysis (PCA) were used. In addition, to visualize (a)symmetry between binding profiles of antidepressants, radar plots were constructed. On the basis of both analyses, four clusters of antidepressants which exert similar pharmacological properties were identified. Potentially, this model could be a helpful tool in medical practice and may be used as a prediction model for adverse effects of drugs entering the market.