| pubmed-article:20462211 | rdf:type | pubmed:Citation | lld:pubmed |
| pubmed-article:20462211 | lifeskim:mentions | umls-concept:C1319313 | lld:lifeskim |
| pubmed-article:20462211 | lifeskim:mentions | umls-concept:C0679622 | lld:lifeskim |
| pubmed-article:20462211 | lifeskim:mentions | umls-concept:C1880355 | lld:lifeskim |
| pubmed-article:20462211 | lifeskim:mentions | umls-concept:C0205314 | lld:lifeskim |
| pubmed-article:20462211 | lifeskim:mentions | umls-concept:C2935022 | lld:lifeskim |
| pubmed-article:20462211 | pubmed:issue | 11 | lld:pubmed |
| pubmed-article:20462211 | pubmed:dateCreated | 2010-6-3 | lld:pubmed |
| pubmed-article:20462211 | pubmed:abstractText | Structural modification of a virtual screening hit led to the identification of a new series of 4-[3-aryl-2,2-dioxido-2,1,3-benzothiadiazol-1(3H)-yl]-1-(methylamino)butan-2-ols which are potent and selective inhibitors of the norepinephrine transporter over both the serotonin and dopamine transporters. One representative compound S-17b (WYE-103231) had low nanomolar hNET potency (IC(50) = 1.2 nM) and excellent selectivity for hNET over hSERT (>1600-fold) and hDAT (>600-fold). S-17b additionally had a good pharmacokinetic profile and demonstrated oral efficacy in rat models of ovariectomized-induced thermoregulatory dysfunction and morphine dependent flush as well as the hot plate and spinal nerve ligation (SNL) models of acute and neuropathic pain. | lld:pubmed |
| pubmed-article:20462211 | pubmed:language | eng | lld:pubmed |
| pubmed-article:20462211 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:20462211 | pubmed:citationSubset | IM | lld:pubmed |
| pubmed-article:20462211 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:20462211 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:20462211 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:20462211 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:20462211 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:20462211 | pubmed:status | MEDLINE | lld:pubmed |
| pubmed-article:20462211 | pubmed:month | Jun | lld:pubmed |
| pubmed-article:20462211 | pubmed:issn | 1520-4804 | lld:pubmed |
| pubmed-article:20462211 | pubmed:author | pubmed-author:DeecherDarlen... | lld:pubmed |
| pubmed-article:20462211 | pubmed:author | pubmed-author:ZhangPuwenP | lld:pubmed |
| pubmed-article:20462211 | pubmed:author | pubmed-author:FensomeAndrew... | lld:pubmed |
| pubmed-article:20462211 | pubmed:author | pubmed-author:LeventhalLiza... | lld:pubmed |
| pubmed-article:20462211 | pubmed:author | pubmed-author:AlfinitoPeter... | lld:pubmed |
| pubmed-article:20462211 | pubmed:author | pubmed-author:UvegesAlbert... | lld:pubmed |
| pubmed-article:20462211 | pubmed:author | pubmed-author:SpanglerTaylo... | lld:pubmed |
| pubmed-article:20462211 | pubmed:author | pubmed-author:McComasCasey... | lld:pubmed |
| pubmed-article:20462211 | pubmed:author | pubmed-author:CosmiScottS | lld:pubmed |
| pubmed-article:20462211 | pubmed:author | pubmed-author:AdedoyinAdeda... | lld:pubmed |
| pubmed-article:20462211 | pubmed:author | pubmed-author:O'NeillDavid... | lld:pubmed |
| pubmed-article:20462211 | pubmed:author | pubmed-author:WhitesideGart... | lld:pubmed |
| pubmed-article:20462211 | pubmed:author | pubmed-author:HarrisonJimJ | lld:pubmed |
| pubmed-article:20462211 | pubmed:author | pubmed-author:SullivanNicol... | lld:pubmed |
| pubmed-article:20462211 | pubmed:author | pubmed-author:BrayJenifer... | lld:pubmed |
| pubmed-article:20462211 | pubmed:author | pubmed-author:TrybulskiEuge... | lld:pubmed |
| pubmed-article:20462211 | pubmed:author | pubmed-author:MannCharlesC | lld:pubmed |
| pubmed-article:20462211 | pubmed:issnType | Electronic | lld:pubmed |
| pubmed-article:20462211 | pubmed:day | 10 | lld:pubmed |
| pubmed-article:20462211 | pubmed:volume | 53 | lld:pubmed |
| pubmed-article:20462211 | pubmed:owner | NLM | lld:pubmed |
| pubmed-article:20462211 | pubmed:authorsComplete | Y | lld:pubmed |
| pubmed-article:20462211 | pubmed:pagination | 4511-21 | lld:pubmed |
| pubmed-article:20462211 | pubmed:meshHeading | pubmed-meshheading:20462211... | lld:pubmed |
| pubmed-article:20462211 | pubmed:meshHeading | pubmed-meshheading:20462211... | lld:pubmed |
| pubmed-article:20462211 | pubmed:meshHeading | pubmed-meshheading:20462211... | lld:pubmed |
| pubmed-article:20462211 | pubmed:meshHeading | pubmed-meshheading:20462211... | lld:pubmed |
| pubmed-article:20462211 | pubmed:meshHeading | pubmed-meshheading:20462211... | lld:pubmed |
| pubmed-article:20462211 | pubmed:meshHeading | pubmed-meshheading:20462211... | lld:pubmed |
| pubmed-article:20462211 | pubmed:meshHeading | pubmed-meshheading:20462211... | lld:pubmed |
| pubmed-article:20462211 | pubmed:meshHeading | pubmed-meshheading:20462211... | lld:pubmed |
| pubmed-article:20462211 | pubmed:meshHeading | pubmed-meshheading:20462211... | lld:pubmed |
| pubmed-article:20462211 | pubmed:meshHeading | pubmed-meshheading:20462211... | lld:pubmed |
| pubmed-article:20462211 | pubmed:meshHeading | pubmed-meshheading:20462211... | lld:pubmed |
| pubmed-article:20462211 | pubmed:meshHeading | pubmed-meshheading:20462211... | lld:pubmed |
| pubmed-article:20462211 | pubmed:year | 2010 | lld:pubmed |
| pubmed-article:20462211 | pubmed:articleTitle | Discovery of novel selective norepinephrine reuptake inhibitors: 4-[3-aryl-2,2-dioxido-2,1,3-benzothiadiazol-1(3H)-yl]-1-(methylamino)butan-2-ols (WYE-103231). | lld:pubmed |
| pubmed-article:20462211 | pubmed:affiliation | Chemical Sciences, Pfizer Global Research & Development, 500 Arcola Road, Collegeville, Pennsylvania 19426, USA. david.oneill@pfizer.com | lld:pubmed |
| pubmed-article:20462211 | pubmed:publicationType | Journal Article | lld:pubmed |
| http://linkedlifedata.com/r... | http://linkedlifedata.com/r... | pubmed-article:20462211 | lld:chembl |
