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Luis Berrade, a researcher with the Drug R&D Unit of the University of Navarra, has discovered new compounds with the potential for anti-depressant activity. All told, the chemist of the School of Sciences synthesized 51 compounds whose biological characteristics were evaluated by two of the most prestigious groups in this area: the Mediterranean Institute of Neurobiology, located in Italy, and the Department of Pharmacology of the University of Oslo.
The results obtained formed part of his doctoral dissertation, entitled “Design, synthesis and preliminary biological evaluation of new derivatives of benzo[b]-thiophene in the Search for Agents for a New Anti-Depressant Therapy.”
As the researcher explained, the new molecules which he designed affect two brain targets which are considered to be keys in the development of processes of depression. One of these is the serotonin transporter, whose reuptake reduction has already been shown to improve mood; the other is the serotoninergic receptor 5-HT7, a therapeutic target for serotonin whose modulation can provoke anti-depressant effects.
Trials in vivo
In order to study these two key targets, Luis Berrade developed chemical structures via the fusion of two similar chemical compounds: the benzo[b]-thiophene ring and arilamine. Following this, he compared the new compounds with a drug currently on the market, Fluoxetine. As a result of this research, he explained, we discovered that nine of these compounds demonstrated greater affinity, in this sense, than the commercial drug. As a consequence of this discovery, in January in vivo trials were begun in order to test their anti-depressant activity in mice.
This study, one of the first in the world in this specialty, was undertaken in collaboration with the Department of Pharmacology of the University of Navarra. Among its objectives was discovering whether these new compounds could reduce the minimum time required for anti-depressant drugs to ameliorate the symptoms of the disease: Currently, the time for an antidepressant to take effect is from three to six weeks, and this is an important factor in patient refusal to continue with these treatments; as a result it is very important to shorten the time required for the positive effects to appear.