| pubmed-article:9632357 | rdf:type | pubmed:Citation | lld:pubmed |
| pubmed-article:9632357 | lifeskim:mentions | umls-concept:C0034838 | lld:lifeskim |
| pubmed-article:9632357 | lifeskim:mentions | umls-concept:C1261322 | lld:lifeskim |
| pubmed-article:9632357 | lifeskim:mentions | umls-concept:C1621296 | lld:lifeskim |
| pubmed-article:9632357 | pubmed:issue | 13 | lld:pubmed |
| pubmed-article:9632357 | pubmed:dateCreated | 1998-7-9 | lld:pubmed |
| pubmed-article:9632357 | pubmed:abstractText | Benzylimidazolines may represent a class of 5-HT1D ligands that has yet to be exploited. On the basis of a previous report that the 2-(substituted-benzyl)imidazoline alpha-adrenergic agonist oxymetazoline (8) binds with high affinity at calf brain 5-HT1D receptors, we explored the structure-affinity relationships of a series of related derivatives. Each of the aromatic substituents was removed and then reinstated in a systematic manner to determine the influence of the individual substituents on binding. It was found that all of the aromatic substituents of 8 act in concert to impart high affinity. However, although the 3-hydroxy group could be removed without significantly reducing affinity for h5-HT1D (i.e., human 5-HT1Dalpha) receptors, this modification reduced h5-HT1B (i.e., human 5-HT1Dbeta) receptor affinity by nearly 50-fold. The 2, 6-dimethyl groups also contribute to binding but seem to play a greater role for h5-HT1B binding than h5-HT1D binding. With the appropriate structural modifications, several compounds were identified that display 20- to >100-fold selectivity for h5-HT1D versus h5-HT1B receptors. Preliminary functional data suggest that these compounds behave as agonists. Given that 5-HT1D agonists are currently being explored for their antimigraine action and that activation of h5-HT1B receptors might be associated with cardiovascular side effects, h5-HT1D-selective agents may offer a new lead for the development of therapeutically efficacious agents. | lld:pubmed |
| pubmed-article:9632357 | pubmed:language | eng | lld:pubmed |
| pubmed-article:9632357 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:9632357 | pubmed:citationSubset | IM | lld:pubmed |
| pubmed-article:9632357 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:9632357 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:9632357 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:9632357 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:9632357 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:9632357 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:9632357 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:9632357 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:9632357 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:9632357 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:9632357 | pubmed:status | MEDLINE | lld:pubmed |
| pubmed-article:9632357 | pubmed:month | Jun | lld:pubmed |
| pubmed-article:9632357 | pubmed:issn | 0022-2623 | lld:pubmed |
| pubmed-article:9632357 | pubmed:author | pubmed-author:GlennonR ARA | lld:pubmed |
| pubmed-article:9632357 | pubmed:author | pubmed-author:LawHH | lld:pubmed |
| pubmed-article:9632357 | pubmed:author | pubmed-author:LeeD KDK | lld:pubmed |
| pubmed-article:9632357 | pubmed:author | pubmed-author:TeitlerMM | lld:pubmed |
| pubmed-article:9632357 | pubmed:author | pubmed-author:DukatMM | lld:pubmed |
| pubmed-article:9632357 | pubmed:author | pubmed-author:RampersadVV | lld:pubmed |
| pubmed-article:9632357 | pubmed:author | pubmed-author:MazzoccoLL | lld:pubmed |
| pubmed-article:9632357 | pubmed:author | pubmed-author:KambojRR | lld:pubmed |
| pubmed-article:9632357 | pubmed:author | pubmed-author:PrisinzanoTT | lld:pubmed |
| pubmed-article:9632357 | pubmed:issnType | Print | lld:pubmed |
| pubmed-article:9632357 | pubmed:day | 18 | lld:pubmed |
| pubmed-article:9632357 | pubmed:volume | 41 | lld:pubmed |
| pubmed-article:9632357 | pubmed:owner | NLM | lld:pubmed |
| pubmed-article:9632357 | pubmed:authorsComplete | Y | lld:pubmed |
| pubmed-article:9632357 | pubmed:pagination | 2243-51 | lld:pubmed |
| pubmed-article:9632357 | pubmed:dateRevised | 2010-11-18 | lld:pubmed |
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| pubmed-article:9632357 | pubmed:meshHeading | pubmed-meshheading:9632357-... | lld:pubmed |
| pubmed-article:9632357 | pubmed:year | 1998 | lld:pubmed |
| pubmed-article:9632357 | pubmed:articleTitle | Benzylimidazolines as h5-HT1B/1D serotonin receptor ligands: a structure-affinity investigation. | lld:pubmed |
| pubmed-article:9632357 | pubmed:affiliation | Department of Medicinal Chemistry, School of Pharmacy, Medical College of Virginia Campus, Virginia Commonwealth University, Richmond, Virginia 23298-0540, USA. | lld:pubmed |
| pubmed-article:9632357 | pubmed:publicationType | Journal Article | lld:pubmed |
| pubmed-article:9632357 | pubmed:publicationType | In Vitro | lld:pubmed |
| http://linkedlifedata.com/r... | http://linkedlifedata.com/r... | pubmed-article:9632357 | lld:chembl |
