Synthesis and binding properties of novel selective 5-HT3 receptor ligands
| Autor: | Filippo Russo, Róbert Gáspár, Luisa Materia, Giuseppe Romeo, Maria N. Modica, Ferenc Fülöp, Tiziana Mennini, Alfredo Cagnotto, George Falkay |
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| Rok vydání: | 2004 |
| Předmět: |
Male
Magnetic Resonance Spectroscopy Spectrophotometry Infrared Pyrimidine Stereochemistry Guinea Pigs Clinical Biochemistry Pharmaceutical Science In Vitro Techniques Ligands Biochemistry Chemical synthesis 5-HT3 receptor chemistry.chemical_compound Serotonin Agents Drug Discovery polycyclic compounds Animals heterocyclic compounds Receptor Molecular Biology 5-HT receptor Thieno[2 3-d]pyrimidine derivatives 3-d]pyrimidine derivatives Bicyclic molecule biology Chemistry Organic Chemistry musculoskeletal system Affinities Rats Lactam biology.protein Molecular Medicine Thieno[2 Receptors Serotonin 5-HT3 Protein Binding |
| Zdroj: | Bioorganic & Medicinal Chemistry. 12:3891-3901 |
| ISSN: | 0968-0896 |
| DOI: | 10.1016/j.bmc.2004.04.043 |
| Popis: | This work reports on the synthesis and affinities for the 5-HT(3) versus the 5-HT(4) receptor of new piperazinyl-substituted thienopyrimidine derivatives 20-45 with a view to identify potent and selective ligands for the 5-HT(3) receptor. Some of the new compounds show good affinity for the 5-HT(3) receptor and, notably, do not display any affinity for the 5-HT(4) receptor. 4-(4-Methyl-1-piperazinyl)-2-methylthio-6,7-dihydro-5H-cyclopenta[4,5]thieno[2,3-d]pyrimidine 31 exhibits the highest affinity for the 5-HT(3) receptor (Ki = 33 nM) and behaves as noncompetitive antagonist. |
| Databáze: | OpenAIRE |
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