pubmed-article:17335185 | rdf:type | pubmed:Citation | lld:pubmed |
pubmed-article:17335185 | lifeskim:mentions | umls-concept:C0205147 | lld:lifeskim |
pubmed-article:17335185 | lifeskim:mentions | umls-concept:C0005456 | lld:lifeskim |
pubmed-article:17335185 | lifeskim:mentions | umls-concept:C0023688 | lld:lifeskim |
pubmed-article:17335185 | lifeskim:mentions | umls-concept:C0679622 | lld:lifeskim |
pubmed-article:17335185 | lifeskim:mentions | umls-concept:C1552603 | lld:lifeskim |
pubmed-article:17335185 | lifeskim:mentions | umls-concept:C1706202 | lld:lifeskim |
pubmed-article:17335185 | lifeskim:mentions | umls-concept:C0205314 | lld:lifeskim |
pubmed-article:17335185 | lifeskim:mentions | umls-concept:C0205923 | lld:lifeskim |
pubmed-article:17335185 | pubmed:issue | 7 | lld:pubmed |
pubmed-article:17335185 | pubmed:dateCreated | 2007-3-29 | lld:pubmed |
pubmed-article:17335185 | pubmed:abstractText | Novel N-substituted indol-3-ylglyoxylamides (10-37) were synthesized and evaluated as ligands of the benzodiazepine receptor (BzR). In an effort to achieve affinity-based selectivity among BzR subtypes, these compounds were designed to probe the LDi and L2 lipophilic regions. Taking the alpha1-selective benzylindolylglyoxylamides Ia and Ib as leads, we varied the substituent on the benzylamide phenyl ring (compounds 10-23) or replaced the benzyl moiety with alkyl groups (compounds 24-37). The above structural changes gave no shift of selectivity from the alpha1 toward the alpha2 or alpha5 subtypes, thus confirming that a ligand which occupies the LDi region probably exhibits alpha1 selectivity, despite its interactions with other lipophilic areas in the receptor binding cleft. Compound 11 (N-(p-methylbenzyl)-5-nitroindol-3-ylglyoxylamide), which selectively binds with a full agonist efficacy at the alpha1 receptor subtype and displays sedative action, can be regarded as an interesting potential zolpidem-like sedative-hypnotic agent. | lld:pubmed |
pubmed-article:17335185 | pubmed:language | eng | lld:pubmed |
pubmed-article:17335185 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:17335185 | pubmed:citationSubset | IM | lld:pubmed |
pubmed-article:17335185 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:17335185 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:17335185 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:17335185 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:17335185 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:17335185 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:17335185 | pubmed:status | MEDLINE | lld:pubmed |
pubmed-article:17335185 | pubmed:month | Apr | lld:pubmed |
pubmed-article:17335185 | pubmed:issn | 0022-2623 | lld:pubmed |
pubmed-article:17335185 | pubmed:author | pubmed-author:BesnardFranço... | lld:pubmed |
pubmed-article:17335185 | pubmed:author | pubmed-author:MartiniClaudi... | lld:pubmed |
pubmed-article:17335185 | pubmed:author | pubmed-author:CalderoneVinc... | lld:pubmed |
pubmed-article:17335185 | pubmed:author | pubmed-author:NovellinoEtto... | lld:pubmed |
pubmed-article:17335185 | pubmed:author | pubmed-author:CosimelliBarb... | lld:pubmed |
pubmed-article:17335185 | pubmed:author | pubmed-author:PrimofioreGia... | lld:pubmed |
pubmed-article:17335185 | pubmed:author | pubmed-author:Da... | lld:pubmed |
pubmed-article:17335185 | pubmed:author | pubmed-author:SimoriniFranc... | lld:pubmed |
pubmed-article:17335185 | pubmed:author | pubmed-author:MariniAnna... | lld:pubmed |
pubmed-article:17335185 | pubmed:author | pubmed-author:GrecoGiovanni... | lld:pubmed |
pubmed-article:17335185 | pubmed:author | pubmed-author:MontaliMarina... | lld:pubmed |
pubmed-article:17335185 | pubmed:author | pubmed-author:La... | lld:pubmed |
pubmed-article:17335185 | pubmed:author | pubmed-author:TalianiSabrin... | lld:pubmed |
pubmed-article:17335185 | pubmed:author | pubmed-author:PatriziMaria... | lld:pubmed |
pubmed-article:17335185 | pubmed:author | pubmed-author:SergianniVale... | lld:pubmed |
pubmed-article:17335185 | pubmed:issnType | Print | lld:pubmed |
pubmed-article:17335185 | pubmed:day | 5 | lld:pubmed |
pubmed-article:17335185 | pubmed:volume | 50 | lld:pubmed |
pubmed-article:17335185 | pubmed:owner | NLM | lld:pubmed |
pubmed-article:17335185 | pubmed:authorsComplete | Y | lld:pubmed |
pubmed-article:17335185 | pubmed:pagination | 1627-34 | lld:pubmed |
pubmed-article:17335185 | pubmed:dateRevised | 2010-11-18 | lld:pubmed |
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pubmed-article:17335185 | pubmed:meshHeading | pubmed-meshheading:17335185... | lld:pubmed |
pubmed-article:17335185 | pubmed:year | 2007 | lld:pubmed |
pubmed-article:17335185 | pubmed:articleTitle | Novel N-substituted indol-3-ylglyoxylamides probing the LDi and L1/L2 lipophilic regions of the benzodiazepine receptor site in search for subtype-selective ligands. | lld:pubmed |
pubmed-article:17335185 | pubmed:affiliation | Dipartimento di Scienze Farmaceutiche, Università di Pisa, Via Bonanno 6, 56126 Pisa, Italy. primofiore@farm.unipi.it | lld:pubmed |
pubmed-article:17335185 | pubmed:publicationType | Journal Article | lld:pubmed |
pubmed-article:17335185 | pubmed:publicationType | In Vitro | lld:pubmed |
pubmed-article:17335185 | pubmed:publicationType | Research Support, Non-U.S. Gov't | lld:pubmed |
http://linkedlifedata.com/r... | http://linkedlifedata.com/r... | pubmed-article:17335185 | lld:chembl |