FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2076753181> ?p ?o ?g. }

• W2076753181 endingPage "246" @default.
• W2076753181 startingPage "237" @default.
• W2076753181 abstract "The pharmacological profile of PF-00885706, a selective 5-HT(4) receptor partial agonist, was investigated. PF-00885706 displayed a high binding affinity for the human 5-HT(4d) receptor with a K(i) of 3.7 nM that translates to functional agonist activity in vitro with EC(50) values of 4.0 nM and 6.6 nM in cell-based assays of human recombinant 5-HT(4d) receptors and rat tunica muscularis mucosae tissues, respectively. In both assays, partial agonism was confirmed with E(max) values of 84% and 78%, respectively. Notably, PF-00885706 was highly selective, displaying >1000-fold higher affinity for 5-HT(4d) receptors compared to 5-HT(1A), 5-HT(1B), 5-HT(1D), 5-HT(2A), 5-HT(2B), 5-HT(2C), 5-HT(3), 5-HT(7), and D(2long) receptors. Furthermore, in vitro binding assays demonstrated that PF-00885706 had no biologically significant interaction with physiologically important enzymes, ion channels including hERG channel, or receptors at concentrations up to 10 microM except for binding to the sigma(2) receptor. PF-00885706 exhibited weak binding affinity for the sigma(2) receptor yielding a K(i) value of 3 microM, which is more than 800-fold weaker than that for the 5-HT(4d) receptor. Oral administration of PF-00885706 to dogs resulted in marked and long-lasting stimulation of gastric motility with a minimum effective dose of 0.001 mg/kg. Pharmacokinetic analysis revealed that PF-00885706 has a low to moderate volume of distribution and the complete absorption in dogs. Pharmacokinetic and pharmacodynamic analysis of PF-00885706 in the dog gastric motility model showed a correlation between plasma concentrations and enhancement of gastric motility. Thus, PF-00885706 is an orally active, highly selective partial agonist for 5-HT(4) receptors that is expected to be effective for the treatment with gastrointestinal dysmotility disorders with reduced adverse effects mediated by other related receptors." @default.
• W2076753181 created "2016-06-24" @default.
• W2076753181 creator A5010172641 @default.
• W2076753181 creator A5022123374 @default.
• W2076753181 creator A5027749039 @default.
• W2076753181 creator A5034526773 @default.
• W2076753181 creator A5044611259 @default.
• W2076753181 creator A5049351305 @default.
• W2076753181 creator A5059906767 @default.
• W2076753181 creator A5059962047 @default.
• W2076753181 creator A5060631314 @default.
• W2076753181 creator A5063705695 @default.
• W2076753181 creator A5086115460 @default.
• W2076753181 date "2009-10-01" @default.
• W2076753181 modified "2023-09-23" @default.
• W2076753181 title "Pharmacological characterization and determination of pharmacokinetic and pharmacodynamic relationship of PF-00885706, a novel partial agonist selective for the 5-HT4 receptor" @default.
• W2076753181 cites W161356906 @default.
• W2076753181 cites W1702556248 @default.
• W2076753181 cites W1858131570 @default.
• W2076753181 cites W1918687998 @default.
• W2076753181 cites W1965625617 @default.
• W2076753181 cites W1966746671 @default.
• W2076753181 cites W1968098810 @default.
• W2076753181 cites W1975661708 @default.
• W2076753181 cites W1976200262 @default.
• W2076753181 cites W1977859950 @default.
• W2076753181 cites W1992768650 @default.
• W2076753181 cites W1994624994 @default.
• W2076753181 cites W1999933643 @default.
• W2076753181 cites W2000535235 @default.
• W2076753181 cites W2002858990 @default.
• W2076753181 cites W2003117333 @default.
• W2076753181 cites W2004862250 @default.
• W2076753181 cites W2008373894 @default.
• W2076753181 cites W2011345948 @default.
• W2076753181 cites W2017815761 @default.
• W2076753181 cites W2019678016 @default.
• W2076753181 cites W2028221809 @default.
• W2076753181 cites W2029232191 @default.
• W2076753181 cites W2029982117 @default.
• W2076753181 cites W2030183206 @default.
• W2076753181 cites W2041238628 @default.
• W2076753181 cites W2043829453 @default.
• W2076753181 cites W2044025853 @default.
• W2076753181 cites W2051712524 @default.
• W2076753181 cites W2053124111 @default.
• W2076753181 cites W2053958220 @default.
• W2076753181 cites W2059219549 @default.
• W2076753181 cites W2066900142 @default.
• W2076753181 cites W2068454300 @default.
• W2076753181 cites W2069643295 @default.
• W2076753181 cites W2072967140 @default.
• W2076753181 cites W2073461076 @default.
• W2076753181 cites W2074705578 @default.
• W2076753181 cites W2076239091 @default.
• W2076753181 cites W2076826596 @default.
• W2076753181 cites W2078852369 @default.
• W2076753181 cites W2085048839 @default.
• W2076753181 cites W2085104727 @default.
• W2076753181 cites W2085374754 @default.
• W2076753181 cites W2086925294 @default.
• W2076753181 cites W2090842596 @default.
• W2076753181 cites W2100471791 @default.
• W2076753181 cites W2111017095 @default.
• W2076753181 cites W2145533362 @default.
• W2076753181 cites W2159947898 @default.
• W2076753181 cites W2161121905 @default.
• W2076753181 cites W2163161835 @default.
• W2076753181 cites W2171818436 @default.
• W2076753181 cites W2213953966 @default.
• W2076753181 cites W2225465581 @default.
• W2076753181 cites W2227487616 @default.
• W2076753181 cites W2232346553 @default.
• W2076753181 cites W2308049205 @default.
• W2076753181 cites W317690388 @default.
• W2076753181 doi "https://doi.org/10.1016/j.phrs.2009.03.013" @default.
• W2076753181 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/19717010" @default.
• W2076753181 hasPublicationYear "2009" @default.
• W2076753181 type Work @default.
• W2076753181 sameAs 2076753181 @default.
• W2076753181 citedByCount "2" @default.
• W2076753181 countsByYear W20767531812012 @default.
• W2076753181 countsByYear W20767531812020 @default.
• W2076753181 crossrefType "journal-article" @default.
• W2076753181 hasAuthorship W2076753181A5010172641 @default.
• W2076753181 hasAuthorship W2076753181A5022123374 @default.
• W2076753181 hasAuthorship W2076753181A5027749039 @default.
• W2076753181 hasAuthorship W2076753181A5034526773 @default.
• W2076753181 hasAuthorship W2076753181A5044611259 @default.
• W2076753181 hasAuthorship W2076753181A5049351305 @default.
• W2076753181 hasAuthorship W2076753181A5059906767 @default.
• W2076753181 hasAuthorship W2076753181A5059962047 @default.
• W2076753181 hasAuthorship W2076753181A5060631314 @default.
• W2076753181 hasAuthorship W2076753181A5063705695 @default.
• W2076753181 hasAuthorship W2076753181A5086115460 @default.
• W2076753181 hasConcept C126322002 @default.
• W2076753181 hasConcept C134018914 @default.
• W2076753181 hasConcept C170493617 @default.

• next