Source:http://linkedlifedata.com/resource/pubmed/id/16162016
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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
19
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pubmed:dateCreated |
2005-9-15
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pubmed:abstractText |
Thyrotropin-releasing hormone (TRH) analogues in which the C-2 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). Several analogues were found to be selective agonists for TRH-R2 exhibiting no activation of TRH-R1. For example, analogue 4 (R= c-C3H5) was found to activate TRH-R2 with a potency (EC50) of 0.41 microM but did not activate TRH-R1 (potency > 100 microM). This study describes the first discovery of TRH-R2-specific agonists and provides impetus to design predominately CNS-effective TRH peptides.
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pubmed:commentsCorrections | |
pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Central Nervous System Agents,
http://linkedlifedata.com/resource/pubmed/chemical/Imidazoles,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Thyrotropin-Releasing...,
http://linkedlifedata.com/resource/pubmed/chemical/Thyrotropin-Releasing Hormone
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pubmed:status |
MEDLINE
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pubmed:month |
Sep
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pubmed:issn |
0022-2623
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:day |
22
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pubmed:volume |
48
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
6162-5
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:16162016-Cell Line,
pubmed-meshheading:16162016-Central Nervous System Agents,
pubmed-meshheading:16162016-Humans,
pubmed-meshheading:16162016-Imidazoles,
pubmed-meshheading:16162016-Receptors, Thyrotropin-Releasing Hormone,
pubmed-meshheading:16162016-Structure-Activity Relationship,
pubmed-meshheading:16162016-Thyrotropin-Releasing Hormone
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pubmed:year |
2005
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pubmed:articleTitle |
Thyrotropin-releasing hormone (TRH) analogues that exhibit selectivity to TRH receptor subtype 2.
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pubmed:affiliation |
Department of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research, Sector 67, S.A.S. Nagar--160 062, Punjab, India.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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