FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2110726089> ?p ?o ?g. }

• W2110726089 endingPage "55" @default.
• W2110726089 startingPage "47" @default.
• W2110726089 abstract "5-Hydroxytryptamine (serotonin) (5-HT) is a neurotransmitter with both central and peripheral functions, including the modulation of mood, appetite, hemodynamics, gastrointestinal (GI) sensation, secretion, and motility. Its synthesis is initiated by the enzyme tryptophan hydroxylase (TPH). Two isoforms of TPH have been discovered: TPH1, primarily expressed in the enterochromaffin cells of the gastrointestinal tract, and TPH2, expressed exclusively in neuronal cells. Mice lacking <i>Tph1</i> contain little to no 5-HT in the blood and GI tract while maintaining normal levels in the brain. Because GI 5-HT is known to play important roles in normal and pathophysiology, we set out to discover and characterize novel compounds that selectively inhibit biosynthesis of GI 5-HT. Here, we describe two of a series of these inhibitors that are potent for TPH activity both in biochemical and cell-based assays. This class of compounds has unique properties with respect to pharmacokinetic and pharmacodynamic effects on GI serotonin production. Similar to the <i>Tph1</i> knockout results, these TPH inhibitors have the ability to selectively reduce 5-HT levels in the murine GI tract without affecting brain 5-HT levels. In addition, administration of these compounds in a ferret model of chemotherapy-induced emesis caused modest reductions of intestinal serotonin levels and a decreased emetic response. These findings suggest that GI-specific TPH inhibitors may provide novel treatments for various gastrointestinal disorders associated with dysregulation of the GI serotonergic system, such as chemotherapy-induced emesis and irritable bowel syndrome." @default.
• W2110726089 created "2016-06-24" @default.
• W2110726089 creator A5003064330 @default.
• W2110726089 creator A5005570920 @default.
• W2110726089 creator A5014171512 @default.
• W2110726089 creator A5015488978 @default.
• W2110726089 creator A5016524661 @default.
• W2110726089 creator A5021988425 @default.
• W2110726089 creator A5022261026 @default.
• W2110726089 creator A5033822294 @default.
• W2110726089 creator A5040261977 @default.
• W2110726089 creator A5041015251 @default.
• W2110726089 creator A5041036914 @default.
• W2110726089 creator A5050931511 @default.
• W2110726089 creator A5051610149 @default.
• W2110726089 creator A5053275832 @default.
• W2110726089 creator A5055135244 @default.
• W2110726089 creator A5056272117 @default.
• W2110726089 creator A5061616086 @default.
• W2110726089 creator A5063066884 @default.
• W2110726089 creator A5063553304 @default.
• W2110726089 creator A5069183135 @default.
• W2110726089 creator A5080253618 @default.
• W2110726089 date "2008-01-11" @default.
• W2110726089 modified "2023-10-11" @default.
• W2110726089 title "Discovery and Characterization of Novel Tryptophan Hydroxylase Inhibitors That Selectively Inhibit Serotonin Synthesis in the Gastrointestinal Tract" @default.
• W2110726089 cites W1569578194 @default.
• W2110726089 cites W1607870348 @default.
• W2110726089 cites W1821827363 @default.
• W2110726089 cites W1968415875 @default.
• W2110726089 cites W1969144895 @default.
• W2110726089 cites W1972869966 @default.
• W2110726089 cites W1976114760 @default.
• W2110726089 cites W2000090843 @default.
• W2110726089 cites W2004491989 @default.
• W2110726089 cites W2014814979 @default.
• W2110726089 cites W2028054765 @default.
• W2110726089 cites W2087576129 @default.
• W2110726089 cites W2087689799 @default.
• W2110726089 cites W2093313809 @default.
• W2110726089 cites W2099344864 @default.
• W2110726089 cites W2106848510 @default.
• W2110726089 cites W2134032226 @default.
• W2110726089 cites W2143952462 @default.
• W2110726089 cites W2339078872 @default.
• W2110726089 cites W2772887788 @default.
• W2110726089 cites W4233636985 @default.
• W2110726089 doi "https://doi.org/10.1124/jpet.107.132670" @default.
• W2110726089 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/18192499" @default.
• W2110726089 hasPublicationYear "2008" @default.
• W2110726089 type Work @default.
• W2110726089 sameAs 2110726089 @default.
• W2110726089 citedByCount "134" @default.
• W2110726089 countsByYear W21107260892012 @default.
• W2110726089 countsByYear W21107260892013 @default.
• W2110726089 countsByYear W21107260892014 @default.
• W2110726089 countsByYear W21107260892015 @default.
• W2110726089 countsByYear W21107260892016 @default.
• W2110726089 countsByYear W21107260892017 @default.
• W2110726089 countsByYear W21107260892018 @default.
• W2110726089 countsByYear W21107260892019 @default.
• W2110726089 countsByYear W21107260892020 @default.
• W2110726089 countsByYear W21107260892021 @default.
• W2110726089 countsByYear W21107260892022 @default.
• W2110726089 countsByYear W21107260892023 @default.
• W2110726089 crossrefType "journal-article" @default.
• W2110726089 hasAuthorship W2110726089A5003064330 @default.
• W2110726089 hasAuthorship W2110726089A5005570920 @default.
• W2110726089 hasAuthorship W2110726089A5014171512 @default.
• W2110726089 hasAuthorship W2110726089A5015488978 @default.
• W2110726089 hasAuthorship W2110726089A5016524661 @default.
• W2110726089 hasAuthorship W2110726089A5021988425 @default.
• W2110726089 hasAuthorship W2110726089A5022261026 @default.
• W2110726089 hasAuthorship W2110726089A5033822294 @default.
• W2110726089 hasAuthorship W2110726089A5040261977 @default.
• W2110726089 hasAuthorship W2110726089A5041015251 @default.
• W2110726089 hasAuthorship W2110726089A5041036914 @default.
• W2110726089 hasAuthorship W2110726089A5050931511 @default.
• W2110726089 hasAuthorship W2110726089A5051610149 @default.
• W2110726089 hasAuthorship W2110726089A5053275832 @default.
• W2110726089 hasAuthorship W2110726089A5055135244 @default.
• W2110726089 hasAuthorship W2110726089A5056272117 @default.
• W2110726089 hasAuthorship W2110726089A5061616086 @default.
• W2110726089 hasAuthorship W2110726089A5063066884 @default.
• W2110726089 hasAuthorship W2110726089A5063553304 @default.
• W2110726089 hasAuthorship W2110726089A5069183135 @default.
• W2110726089 hasAuthorship W2110726089A5080253618 @default.
• W2110726089 hasConcept C126322002 @default.
• W2110726089 hasConcept C134018914 @default.
• W2110726089 hasConcept C170493617 @default.
• W2110726089 hasConcept C2775864247 @default.
• W2110726089 hasConcept C2775951788 @default.
• W2110726089 hasConcept C2778271842 @default.
• W2110726089 hasConcept C2779999352 @default.
• W2110726089 hasConcept C2780512811 @default.
• W2110726089 hasConcept C37000724 @default.
• W2110726089 hasConcept C53910766 @default.
• W2110726089 hasConcept C71924100 @default.

• next