title: Synthesis and pharmacological evaluation of novel tricyclic[2,1-f]theophylline derivatives.
abstract: The multireceptor strategy was implemented to obtain potential antipsychotics and/or antidepressants in a series of long-chain arylpiperazines bearing a tricyclic theophylline fragment. Their binding profile toward monoaminergic receptors (α1, 5-HT(1A), 5-HT(2A), 5-HT6, 5-HT7, D2, D3) was determined as well. The selected compounds 7 and 9 were tested in functional in vivo models and showed, like atypical antipsychotic drugs, presynaptic 5-HT(1A) receptor agonistic and postsynaptic 5-HT(1A), 5-HT(2A), and D2 receptor antagonistic activity.
authors.affiliation: Department of Pharmaceutical Chemistry, Jagiellonian University Medical College, Kraków, Poland.
authors.forename: Agnieszka
authors.initials: A
authors.lastname: Zagórska
authors.forename: Maciej
authors.initials: M
authors.lastname: Pawłowski
authors.forename: Agata
authors.initials: A
authors.lastname: Siwek
authors.forename: Grzegorz
authors.initials: G
authors.lastname: Kazek
authors.forename: Anna
authors.initials: A
authors.lastname: Partyka
authors.forename: Dagmara
authors.initials: D
authors.lastname: Wróbel
authors.forename: Magdalena
authors.initials: M
authors.lastname: Jastrzębska-Więsek
authors.forename: Anna
authors.initials: A
authors.lastname: Wesołowska
mesh_terms: D000818:Animals; D000929:Antidepressive Agents, Tricyclic / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology*; D014150:Antipsychotic Agents / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology*; D001522:Behavior, Animal / Q000187:drug effects; D001833:Body Temperature Regulation / Q000187:drug effects; D065127:Dopamine D2 Receptor Antagonists / Q000138:chemical synthesis / Q000494:pharmacology; D008297:Male; D051379:Mice; D015394:Molecular Structure; D009043:Motor Activity / Q000187:drug effects; D017208:Rats, Wistar; D011954:Receptors, Dopamine / Q000187:drug effects / Q000378:metabolism; D011985:Receptors, Serotonin / Q000187:drug effects / Q000378:metabolism; D058825:Serotonin 5-HT1 Receptor Agonists / Q000138:chemical synthesis / Q000494:pharmacology; D058829:Serotonin 5-HT1 Receptor Antagonists / Q000138:chemical synthesis / Q000494:pharmacology; D058830:Serotonin 5-HT2 Receptor Antagonists / Q000138:chemical synthesis / Q000494:pharmacology; D013329:Structure-Activity Relationship; D013806:Theophylline / Q000031:analogs & derivatives / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology*
chemical_list: D000929:Antidepressive Agents, Tricyclic; D014150:Antipsychotic Agents; D065127:Dopamine D2 Receptor Antagonists; D011954:Receptors, Dopamine; D011985:Receptors, Serotonin; D058825:Serotonin 5-HT1 Receptor Agonists; D058829:Serotonin 5-HT1 Receptor Antagonists; D058830:Serotonin 5-HT2 Receptor Antagonists; D013806:Theophylline
keywords: Depression; Imidazo[2,1-f]purine-2,4-diones; Long-chain arylpiperazines; Schizophrenia; Serotonin