| pubmed-article:12392732 | rdf:type | pubmed:Citation | lld:pubmed |
| pubmed-article:12392732 | lifeskim:mentions | umls-concept:C0243071 | lld:lifeskim |
| pubmed-article:12392732 | lifeskim:mentions | umls-concept:C1880022 | lld:lifeskim |
| pubmed-article:12392732 | lifeskim:mentions | umls-concept:C1880355 | lld:lifeskim |
| pubmed-article:12392732 | lifeskim:mentions | umls-concept:C1259613 | lld:lifeskim |
| pubmed-article:12392732 | lifeskim:mentions | umls-concept:C0205460 | lld:lifeskim |
| pubmed-article:12392732 | lifeskim:mentions | umls-concept:C0231449 | lld:lifeskim |
| pubmed-article:12392732 | pubmed:issue | 22 | lld:pubmed |
| pubmed-article:12392732 | pubmed:dateCreated | 2002-10-23 | lld:pubmed |
| pubmed-article:12392732 | pubmed:abstractText | New tert-butyl, picolyl and fluorinated analogues of capromorelin (3), a short-acting growth hormone secretagogue (GHS), were prepared as part of a program to identify long-acting GHSs that increase 24-h plasma IGF-1 levels. Compounds 4c and 4d (ACD LogD values >or=2.9) displayed extended plasma elimination half-lives in dogs, primarily due to high volumes of distribution, but showed weak GH secretagogue activities in rats (ED(50)s>10 mg/kg). A less lipophilic derivative 4 (ACD LogD=1.6) exhibited a shorter canine half-life, but stimulated GH secretion in two animal species. Repeat oral dosing of 4 in dogs for 29 days (6 mg/kg) resulted in a significant down-regulation of the post dose GH response and a 60 and 40% increase in IGF-1 levels relative to pre-dose levels at the 8- and 24-h post dose time points. Compound 4 (CP-464709-18) has been selected as a development candidate for the treatment of frailty. | lld:pubmed |
| pubmed-article:12392732 | pubmed:language | eng | lld:pubmed |
| pubmed-article:12392732 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:12392732 | pubmed:citationSubset | IM | lld:pubmed |
| pubmed-article:12392732 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:12392732 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:12392732 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:12392732 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:12392732 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:12392732 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:12392732 | pubmed:status | MEDLINE | lld:pubmed |
| pubmed-article:12392732 | pubmed:month | Nov | lld:pubmed |
| pubmed-article:12392732 | pubmed:issn | 0960-894X | lld:pubmed |
| pubmed-article:12392732 | pubmed:author | pubmed-author:YuLiL | lld:pubmed |
| pubmed-article:12392732 | pubmed:author | pubmed-author:TolerSteven... | lld:pubmed |
| pubmed-article:12392732 | pubmed:author | pubmed-author:CarpinoPhilip... | lld:pubmed |
| pubmed-article:12392732 | pubmed:author | pubmed-author:LefkerBruce... | lld:pubmed |
| pubmed-article:12392732 | pubmed:author | pubmed-author:PanLydia CLC | lld:pubmed |
| pubmed-article:12392732 | pubmed:author | pubmed-author:HadcockJohn... | lld:pubmed |
| pubmed-article:12392732 | pubmed:author | pubmed-author:MurrayMariann... | lld:pubmed |
| pubmed-article:12392732 | pubmed:author | pubmed-author:CookEwell RER | lld:pubmed |
| pubmed-article:12392732 | pubmed:author | pubmed-author:DiBrinoJoseph... | lld:pubmed |
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| pubmed-article:12392732 | pubmed:author | pubmed-author:MullinsMichel... | lld:pubmed |
| pubmed-article:12392732 | pubmed:author | pubmed-author:NickersonDavi... | lld:pubmed |
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| pubmed-article:12392732 | pubmed:author | pubmed-author:RaganJohn AJA | lld:pubmed |
| pubmed-article:12392732 | pubmed:author | pubmed-author:RoseColin RCR | lld:pubmed |
| pubmed-article:12392732 | pubmed:author | pubmed-author:TessDavid ADA | lld:pubmed |
| pubmed-article:12392732 | pubmed:author | pubmed-author:WrightAnn SAS | lld:pubmed |
| pubmed-article:12392732 | pubmed:author | pubmed-author:ZawistoskiMic... | lld:pubmed |
| pubmed-article:12392732 | pubmed:author | pubmed-author:PettersenJohn... | lld:pubmed |
| pubmed-article:12392732 | pubmed:author | pubmed-author:DaSilva-Jardi... | lld:pubmed |
| pubmed-article:12392732 | pubmed:author | pubmed-author:WilsonTheresa... | lld:pubmed |
| pubmed-article:12392732 | pubmed:author | pubmed-author:ThompsonDavid... | lld:pubmed |
| pubmed-article:12392732 | pubmed:issnType | Print | lld:pubmed |
| pubmed-article:12392732 | pubmed:day | 18 | lld:pubmed |
| pubmed-article:12392732 | pubmed:volume | 12 | lld:pubmed |
| pubmed-article:12392732 | pubmed:owner | NLM | lld:pubmed |
| pubmed-article:12392732 | pubmed:authorsComplete | Y | lld:pubmed |
| pubmed-article:12392732 | pubmed:pagination | 3279-82 | lld:pubmed |
| pubmed-article:12392732 | pubmed:dateRevised | 2010-11-18 | lld:pubmed |
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| pubmed-article:12392732 | pubmed:meshHeading | pubmed-meshheading:12392732... | lld:pubmed |
| pubmed-article:12392732 | pubmed:meshHeading | pubmed-meshheading:12392732... | lld:pubmed |
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| pubmed-article:12392732 | pubmed:meshHeading | pubmed-meshheading:12392732... | lld:pubmed |
| pubmed-article:12392732 | pubmed:year | 2002 | lld:pubmed |
| pubmed-article:12392732 | pubmed:articleTitle | Discovery and biological characterization of capromorelin analogues with extended half-lives. | lld:pubmed |
| pubmed-article:12392732 | pubmed:affiliation | Pfizer Global Research & Development, Groton Labs, MS8220-3004, Groton, CT 06340, USA. philip_a_carpino@groton.pfizer.com | lld:pubmed |
| pubmed-article:12392732 | pubmed:publicationType | Journal Article | lld:pubmed |
| http://linkedlifedata.com/r... | http://linkedlifedata.com/r... | pubmed-article:12392732 | lld:chembl |
| http://linkedlifedata.com/r... | pubmed:referesTo | pubmed-article:12392732 | lld:pubmed |
