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
Identifiers and Pagination:Year: 2008
First Page: 54
Last Page: 62
Publisher Id: TOPHARMJ-2-54
Article History:Received Date: 7/4/2008
Revision Received Date: 14/5/2008
Acceptance Date: 19/5/2008
Electronic publication date: 3/6/20082
Collection year: 2008
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.
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.