5-HT<sub>2</sub> receptor affinity, docking studies and pharmacological evaluation of a series of 1,3-disubstituted thiourea derivatives

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5-HT₂ receptor affinity, docking studies and pharmacological evaluation of a series of 1,3-disubstituted thiourea derivatives

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作者：Anna Bielenica^a ; ^{abielenica@wum.edu.pl" class="auth_mail" title="E-mail the corresponding author} ; Ewa Kędzierska^b ; Michał Koliński^c ; Sebastian Kmiecik^d ; Andrzej Koliński^d ; Ferdinando Fiorino^e ; Beatrice Severino^e ; Elisa Magli^e ; Angela Corvino^e ; Ilaria Rossi^f ; Paola Massarelli^f ; Anna E. Kozioł^g ; Aleksandra Sawczenko^g ; Marta Struga^h
关键词：5-HT2A receptor ligands ; 5-HT2C receptor ligands ; Docking studies ; Thiourea ; CNS activity
刊名：European Journal of Medicinal Chemistry
出版年：2016
出版时间：30 June 2016
年：2016
卷：116
期：Complete
页码：173-186
全文大小：1863 K

文摘

•: Design, synthesis and in vitro activity of 1,3-disubstituted thioureas was presented.
•: 5">Compounds 1 and 5 possessed subnanomolar affinity for the 5-HT_2A receptor.
•: Pharmacophore model for 5-HT_2A receptor antagonists was generated.
•: 5">The in vivo activities of selected derivatives were evaluated.
•: Compounds are effective inhibitors of DOI-evoked head twitch responses.

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