• Functional selectivity and antidepressant activity of serotonin 1A receptor ligands 

      Chilmonczyk, Zdzislaw; Bojarski, Andrzej Jacek; Pilc, Andrzej; Sylte, Ingebrigt (Journal article; Tidsskriftartikkel; Peer reviewed, 2015)
      Serotonin (5-HT) is a monoamine neurotransmitter that plays an important role in physiological functions. 5-HT has been implicated in sleep, feeding, sexual behavior, temperature regulation, pain, and cognition as well as in pathological states including disorders connected to mood, anxiety, psychosis and pain. 5-HT1A receptors have for a long time been considered as an interesting target for the ...
    • Identification of novel serotonin transporter compounds by virtual Screening 

      Gabrielsen, Mari; Kurczab, Rafal; Siwek, Agata; Wolak, Malgorzata; Ravna, Aina Westrheim; Kristiansen, kurt; Kufareva, Irina; Abagyan, Ruben; Nowak, Gabriel; Chilmonczyk, Zdzislaw; Sylte, Ingebrigt; Bojarski, Andrzej J. (Journal article; Tidsskriftartikkel; Peer reviewed, 2014-02-12)
      The serotonin (5-hydroxytryptamine, 5-HT) transporter (SERT) plays an essential role in the termination of serotonergic neurotransmission by removing 5-HT from the synaptic cleft into the presynaptic neuron. It is also of pharmacological importance being targeted by antidepressants and psychostimulant drugs. Here, five commercial databases containing approximately 3.24 million drug-like compounds ...
    • A linear combination of pharmacophore hypotheses as a new tool in search or new active compounds - An application for 5-HT1a receptor ligands 

      Warszycki, Dawid; Mordalski, Stefan; Kristiansen, kurt; Kafel, Rafal; Sylte, Ingebrigt; Chilmonczyk, Zdzislaw; Bojarski, Andrzej J. (Journal article; Tidsskriftartikkel; Peer reviewed, 2013)
      This study explores a new approach to pharmacophore screening involving the use of an optimized linear combination of models instead of a single hypothesis. The implementation and evaluation of the developed methodology are performed for a complete known chemical space of 5-HT1AR ligands (3616 active compounds with Ki < 100 nM) acquired from the ChEMBL database. Clusters generated from three different ...
    • Mass-spectrometric studies of new 6-nitroquipazines-serotonin transporter inhibitors 

      Witowska-Jarosz, Janina; Jaronczyk, Malgorzata; Mazurek, Aleksander P; Sylte, Ingebrigt; Bojarski, Andrezej J; Chilmonczyk, Zdzislaw; Jarosz, Maciej (Journal article; Tidsskriftartikkel; Peer reviewed, 2012)
      Six synthesized 6-nitroquipazine derivatives were examined by electron ionization (EI) and electrospray ionization (ESI) mass spectrometry in positive and negative ion mode. The compounds exhibit high affinity for the serotonin transporter (SERT) and belong to a new class of SERT inhibitors. The EI mass spectra registered in negative ion mode showed prominent molecular ions for all the compounds ...