{"database":"biostudies-literature","file_versions":[],"scores":null,"additional":{"submitter":["Latacz G"],"funding":["Narodowe Centrum Nauki"],"pagination":["1882-1890"],"full_dataset_link":["https://www.ebi.ac.uk/biostudies/studies/S-EPMC6256855"],"repository":["biostudies-literature"],"omics_type":["Unknown"],"volume":["9(11)"],"pubmed_abstract":["Close structural analogues of 5-carboxamidotryptamine (5-CT) based on the newly discovered indole-imidazole scaffold were synthesized and evaluated to search for a 5-HT7 receptor agonist of higher selectivity. In vitro drug-likeness studies and in vivo pharmacological evaluation of potent and selective low-basicity 5-HT7 receptor agonists, previously published 7 (3-(1-ethyl-1H-imidazol-5-yl)-1H-indole-5-carboxamide, AH-494) and 13 (3-(1-methyl-1H-imidazol-5-yl)-1H-indole-5-carboxamide), have supported their usefulness as pharmacological tools. Comprehensive in vitro comparison studies between 7, 13 and the commonly used 5-CT showed their very similar ADMET properties. Compound 7 at 1 mg kg-1 reversed MK-801-induced disruption in novel object recognition in mice and alleviated stress-induce"],"journal":["MedChemComm"],"pubmed_title":["Search for a 5-CT alternative. In vitro and in vivo evaluation of novel pharmacological tools: 3-(1-alkyl-1H-imidazol-5-yl)-1H-indole-5-carboxamides, low-basicity 5-HT7 receptor agonists."],"pmcid":["PMC6256855"],"funding_grant_id":["OPUS 2017/25/B/NZ7/02929"],"pubmed_authors":["Cieslik P","Wozniak M","Hogendorf A","Lubelska A","Wieronska JM","Handzlik J","Hogendorf AS","Kiec-Kononowicz K","Bojarski AJ","Latacz G"],"additional_accession":[]},"is_claimable":false,"name":"Search for a 5-CT alternative. In vitro and in vivo evaluation of novel pharmacological tools: 3-(1-alkyl-1H-imidazol-5-yl)-1H-indole-5-carboxamides, low-basicity 5-HT7 receptor agonists.","description":"Close structural analogues of 5-carboxamidotryptamine (5-CT) based on the newly discovered indole-imidazole scaffold were synthesized and evaluated to search for a 5-HT7 receptor agonist of higher selectivity. In vitro drug-likeness studies and in vivo pharmacological evaluation of potent and selective low-basicity 5-HT7 receptor agonists, previously published 7 (3-(1-ethyl-1H-imidazol-5-yl)-1H-indole-5-carboxamide, AH-494) and 13 (3-(1-methyl-1H-imidazol-5-yl)-1H-indole-5-carboxamide), have supported their usefulness as pharmacological tools. Comprehensive in vitro comparison studies between 7, 13 and the commonly used 5-CT showed their very similar ADMET properties. Compound 7 at 1 mg kg-1 reversed MK-801-induced disruption in novel object recognition in mice and alleviated stress-induce","dates":{"release":"2018-01-01T00:00:00Z","publication":"2018 Nov","modification":"2025-04-18T11:42:26.799Z","creation":"2019-10-11T07:18:30Z"},"accession":"S-EPMC6256855","cross_references":{"pubmed":["30568756"],"doi":["10.1039/c8md00313k"]}}