| pubmed-article:16735122 | rdf:type | pubmed:Citation | lld:pubmed |
| pubmed-article:16735122 | lifeskim:mentions | umls-concept:C0040162 | lld:lifeskim |
| pubmed-article:16735122 | lifeskim:mentions | umls-concept:C0220781 | lld:lifeskim |
| pubmed-article:16735122 | lifeskim:mentions | umls-concept:C1883254 | lld:lifeskim |
| pubmed-article:16735122 | lifeskim:mentions | umls-concept:C0597358 | lld:lifeskim |
| pubmed-article:16735122 | lifeskim:mentions | umls-concept:C0332256 | lld:lifeskim |
| pubmed-article:16735122 | lifeskim:mentions | umls-concept:C2603343 | lld:lifeskim |
| pubmed-article:16735122 | lifeskim:mentions | umls-concept:C0243071 | lld:lifeskim |
| pubmed-article:16735122 | lifeskim:mentions | umls-concept:C1879547 | lld:lifeskim |
| pubmed-article:16735122 | pubmed:issue | 17 | lld:pubmed |
| pubmed-article:16735122 | pubmed:dateCreated | 2006-7-25 | lld:pubmed |
| pubmed-article:16735122 | pubmed:abstractText | Thyrotropin-releasing hormone (TRH) analogues in which the N(1)-position of the imidazole ring of the centrally placed histidine residue is substituted with various alkyl groups were synthesized and studied as agonists for TRH receptor subtype 1 (TRH-R1) and subtype 2 (TRH-R2). Analogue 3 (R=C2H5) exhibited binding affinity (Ki) of 0.012 microM to TRH-R1 that is about 1.1-fold higher than that of TRH. Several analogues were found to selectively activate TRH-R2 with greater potency than TRH-R1. The most selective agonist of the series 5 [R=CH(CH3)2] was found to activate TRH-R2 with a potency (EC50) of 0.018 microM but could only activate TRH-R1 at EC50 value of 1.6 microM; that is, exhibited 88-fold greater potency for TRH-R2 versus TRH-R1. The results of this study indicate that modulation of central histidine residue is important for designing analogues which were selective agonist at TRH receptor subtypes. | lld:pubmed |
| pubmed-article:16735122 | pubmed:language | eng | lld:pubmed |
| pubmed-article:16735122 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:16735122 | pubmed:citationSubset | IM | lld:pubmed |
| pubmed-article:16735122 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:16735122 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:16735122 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:16735122 | pubmed:status | MEDLINE | lld:pubmed |
| pubmed-article:16735122 | pubmed:month | Sep | lld:pubmed |
| pubmed-article:16735122 | pubmed:issn | 0968-0896 | lld:pubmed |
| pubmed-article:16735122 | pubmed:author | pubmed-author:JainRahulR | lld:pubmed |
| pubmed-article:16735122 | pubmed:author | pubmed-author:GershengornMa... | lld:pubmed |
| pubmed-article:16735122 | pubmed:author | pubmed-author:KaurNavneetN | lld:pubmed |
| pubmed-article:16735122 | pubmed:author | pubmed-author:LuXinpingX | lld:pubmed |
| pubmed-article:16735122 | pubmed:author | pubmed-author:MongaVikramde... | lld:pubmed |
| pubmed-article:16735122 | pubmed:author | pubmed-author:JosanJatinder... | lld:pubmed |
| pubmed-article:16735122 | pubmed:issnType | Print | lld:pubmed |
| pubmed-article:16735122 | pubmed:day | 1 | lld:pubmed |
| pubmed-article:16735122 | pubmed:volume | 14 | lld:pubmed |
| pubmed-article:16735122 | pubmed:owner | NLM | lld:pubmed |
| pubmed-article:16735122 | pubmed:authorsComplete | Y | lld:pubmed |
| pubmed-article:16735122 | pubmed:pagination | 5981-8 | lld:pubmed |
| pubmed-article:16735122 | pubmed:dateRevised | 2006-11-15 | lld:pubmed |
| pubmed-article:16735122 | pubmed:meshHeading | pubmed-meshheading:16735122... | lld:pubmed |
| pubmed-article:16735122 | pubmed:meshHeading | pubmed-meshheading:16735122... | lld:pubmed |
| pubmed-article:16735122 | pubmed:meshHeading | pubmed-meshheading:16735122... | lld:pubmed |
| pubmed-article:16735122 | pubmed:meshHeading | pubmed-meshheading:16735122... | lld:pubmed |
| pubmed-article:16735122 | pubmed:meshHeading | pubmed-meshheading:16735122... | lld:pubmed |
| pubmed-article:16735122 | pubmed:year | 2006 | lld:pubmed |
| pubmed-article:16735122 | pubmed:articleTitle | Synthesis, receptor binding, and activation studies of N(1)-alkyl-L-histidine containing thyrotropin-releasing hormone (TRH) analogues. | lld:pubmed |
| pubmed-article:16735122 | pubmed:affiliation | Department of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research, Sector 67, S.A.S. Nagar, Punjab 160 062, India. | lld:pubmed |
| pubmed-article:16735122 | pubmed:publicationType | Journal Article | lld:pubmed |
| pubmed-article:16735122 | pubmed:publicationType | Research Support, Non-U.S. Gov't | lld:pubmed |
| pubmed-article:16735122 | pubmed:publicationType | Research Support, N.I.H., Intramural | lld:pubmed |
