Matches in SemOpenAlex for { <https://semopenalex.org/work/W4319338553> ?p ?o ?g. }
Showing items 1 to 97 of
97
with 100 items per page.
- W4319338553 endingPage "2978" @default.
- W4319338553 startingPage "2964" @default.
- W4319338553 abstract "GPR88 is an orphan G protein-coupled receptor mainly expressed in the brain, whose endogenous ligand has not yet been identified. To elucidate GPR88 functions, our group has developed RTI-13951-33 (1b) as the first in vivo active GPR88 agonist, but its poor metabolic stability and moderate brain permeability remain to be further optimized. Here, we report the design, synthesis, and pharmacological characterization of a new series of RTI-13951-33 analogues with the aim of improving pharmacokinetic properties. As a result, we identified a highly potent GPR88 agonist RTI-122 (30a) (cAMP EC50 = 11 nM) with good metabolic stability (half-life of 5.8 h) and brain permeability (brain/plasma ratio of >1) in mice. Notably, RTI-122 was more effective than RTI-13951-33 in attenuating the binge-like alcohol drinking behavior in the drinking-in-the-dark paradigm. Collectively, our findings suggest that RTI-122 is a promising lead compound for drug discovery research of GPR88 agonists." @default.
- W4319338553 created "2023-02-08" @default.
- W4319338553 creator A5006323154 @default.
- W4319338553 creator A5018268684 @default.
- W4319338553 creator A5026978522 @default.
- W4319338553 creator A5031112700 @default.
- W4319338553 creator A5036778176 @default.
- W4319338553 creator A5049083915 @default.
- W4319338553 creator A5065409960 @default.
- W4319338553 creator A5068613321 @default.
- W4319338553 creator A5083021000 @default.
- W4319338553 date "2023-02-07" @default.
- W4319338553 modified "2023-09-26" @default.
- W4319338553 title "Improvement of the Metabolic Stability of GPR88 Agonist RTI-13951-33: Design, Synthesis, and Biological Evaluation" @default.
- W4319338553 cites W1973091091 @default.
- W4319338553 cites W1975616682 @default.
- W4319338553 cites W1986552985 @default.
- W4319338553 cites W2013818660 @default.
- W4319338553 cites W2043239339 @default.
- W4319338553 cites W2044801980 @default.
- W4319338553 cites W2049535760 @default.
- W4319338553 cites W2097194698 @default.
- W4319338553 cites W2112893277 @default.
- W4319338553 cites W2155014655 @default.
- W4319338553 cites W2160397887 @default.
- W4319338553 cites W2170426869 @default.
- W4319338553 cites W2171098630 @default.
- W4319338553 cites W2481416678 @default.
- W4319338553 cites W2492142443 @default.
- W4319338553 cites W2558811538 @default.
- W4319338553 cites W2602297337 @default.
- W4319338553 cites W2604729881 @default.
- W4319338553 cites W2793301337 @default.
- W4319338553 cites W2884874610 @default.
- W4319338553 cites W2905480784 @default.
- W4319338553 cites W2964358699 @default.
- W4319338553 cites W3105946202 @default.
- W4319338553 cites W3192786658 @default.
- W4319338553 cites W4225278923 @default.
- W4319338553 cites W4293223886 @default.
- W4319338553 cites W647659435 @default.
- W4319338553 doi "https://doi.org/10.1021/acs.jmedchem.2c01983" @default.
- W4319338553 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/36749855" @default.
- W4319338553 hasPublicationYear "2023" @default.
- W4319338553 type Work @default.
- W4319338553 citedByCount "0" @default.
- W4319338553 crossrefType "journal-article" @default.
- W4319338553 hasAuthorship W4319338553A5006323154 @default.
- W4319338553 hasAuthorship W4319338553A5018268684 @default.
- W4319338553 hasAuthorship W4319338553A5026978522 @default.
- W4319338553 hasAuthorship W4319338553A5031112700 @default.
- W4319338553 hasAuthorship W4319338553A5036778176 @default.
- W4319338553 hasAuthorship W4319338553A5049083915 @default.
- W4319338553 hasAuthorship W4319338553A5065409960 @default.
- W4319338553 hasAuthorship W4319338553A5068613321 @default.
- W4319338553 hasAuthorship W4319338553A5083021000 @default.
- W4319338553 hasConcept C112705442 @default.
- W4319338553 hasConcept C170493617 @default.
- W4319338553 hasConcept C185592680 @default.
- W4319338553 hasConcept C202751555 @default.
- W4319338553 hasConcept C2778938600 @default.
- W4319338553 hasConcept C2991874392 @default.
- W4319338553 hasConcept C55493867 @default.
- W4319338553 hasConcept C71924100 @default.
- W4319338553 hasConcept C98274493 @default.
- W4319338553 hasConceptScore W4319338553C112705442 @default.
- W4319338553 hasConceptScore W4319338553C170493617 @default.
- W4319338553 hasConceptScore W4319338553C185592680 @default.
- W4319338553 hasConceptScore W4319338553C202751555 @default.
- W4319338553 hasConceptScore W4319338553C2778938600 @default.
- W4319338553 hasConceptScore W4319338553C2991874392 @default.
- W4319338553 hasConceptScore W4319338553C55493867 @default.
- W4319338553 hasConceptScore W4319338553C71924100 @default.
- W4319338553 hasConceptScore W4319338553C98274493 @default.
- W4319338553 hasFunder F4320337330 @default.
- W4319338553 hasIssue "4" @default.
- W4319338553 hasLocation W43193385531 @default.
- W4319338553 hasLocation W43193385532 @default.
- W4319338553 hasLocation W43193385533 @default.
- W4319338553 hasOpenAccess W4319338553 @default.
- W4319338553 hasPrimaryLocation W43193385531 @default.
- W4319338553 hasRelatedWork W1982282930 @default.
- W4319338553 hasRelatedWork W2042405111 @default.
- W4319338553 hasRelatedWork W2141289501 @default.
- W4319338553 hasRelatedWork W2594910449 @default.
- W4319338553 hasRelatedWork W2606334551 @default.
- W4319338553 hasRelatedWork W2960553615 @default.
- W4319338553 hasRelatedWork W2991030316 @default.
- W4319338553 hasRelatedWork W3043458966 @default.
- W4319338553 hasRelatedWork W3134698206 @default.
- W4319338553 hasRelatedWork W4364376666 @default.
- W4319338553 hasVolume "66" @default.
- W4319338553 isParatext "false" @default.
- W4319338553 isRetracted "false" @default.
- W4319338553 workType "article" @default.