Matches in SemOpenAlex for { <https://semopenalex.org/work/W2120780012> ?p ?o ?g. }
Showing items 1 to 92 of
92
with 100 items per page.
- W2120780012 endingPage "457" @default.
- W2120780012 startingPage "450" @default.
- W2120780012 abstract "The previously described cyclic delta opioid receptor-selective tetrapeptide H-Tyr-d-Cys-Phe-d-Pen-OH (JOM-13) was modified at residue 3 by incorporation of both natural and unnatural amino acids with varying steric, electronic, and lipophilic properties. Effects on mu and delta opioid receptor binding affinities were evaluated by testing the compounds for displacement of radiolabeled receptor-selective ligands in a guinea pig brain receptor binding assay. Results obtained with the bulky aromatic 1-Nal3 and 2-Nal3 substitutions suggest that the shape of the receptor subsite with which the side chain of the internal aromatic residue interacts differs for delta and mu receptors. This subsite of either receptor can accommodate the transverse steric bulk of the 1-Nal3 side chain but only the delta receptor can readily accept the more elongated 2-Nal3 side chain. Several analogs with pi-excessive heteroaromatic side chains in residue 3 were examined. In general, these analogs display diminished binding to mu and delta receptors, consistent with previous findings for analogs with residue 3 substitutions of modified electronic character. Several analogs with alkyl side chains in residue 3 were also examined. While delta receptor binding affinity is severely diminished with Val3, Ile3, and Leu3 substitutions, Cha3 substitution is very well tolerated, indicating that, contrary to the widely held belief, an aromatic side chain in this portion of the ligand is not required for delta receptor binding. Where possible, comparison of results in this delta-selective tetrapeptide series with those reported for analogous modification in the cyclic delta-selective pentapeptide [d-Pen2, d-Pen5]enkephalin (DPDPE) and linear pentapeptide enkephalins reveals similar trends." @default.
- W2120780012 created "2016-06-24" @default.
- W2120780012 creator A5056293361 @default.
- W2120780012 creator A5079002496 @default.
- W2120780012 date "2009-01-12" @default.
- W2120780012 modified "2023-10-03" @default.
- W2120780012 title "Modification of the Phe3 aromatic moiety in delta receptor-selective dermorphin/deltorphin-related tetrapeptides Effects on opioid receptor binding" @default.
- W2120780012 cites W1970042656 @default.
- W2120780012 cites W1977221227 @default.
- W2120780012 cites W1984748059 @default.
- W2120780012 cites W1991440046 @default.
- W2120780012 cites W2003286976 @default.
- W2120780012 cites W2006370393 @default.
- W2120780012 cites W2016275972 @default.
- W2120780012 cites W2043813981 @default.
- W2120780012 cites W2054890348 @default.
- W2120780012 cites W2066367002 @default.
- W2120780012 cites W2070762066 @default.
- W2120780012 cites W2089320192 @default.
- W2120780012 cites W2092781319 @default.
- W2120780012 cites W2138947171 @default.
- W2120780012 doi "https://doi.org/10.1111/j.1399-3011.1992.tb01449.x" @default.
- W2120780012 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/1330964" @default.
- W2120780012 hasPublicationYear "2009" @default.
- W2120780012 type Work @default.
- W2120780012 sameAs 2120780012 @default.
- W2120780012 citedByCount "20" @default.
- W2120780012 countsByYear W21207800122019 @default.
- W2120780012 countsByYear W21207800122021 @default.
- W2120780012 crossrefType "journal-article" @default.
- W2120780012 hasAuthorship W2120780012A5056293361 @default.
- W2120780012 hasAuthorship W2120780012A5079002496 @default.
- W2120780012 hasBestOaLocation W21207800122 @default.
- W2120780012 hasConcept C116569031 @default.
- W2120780012 hasConcept C141087196 @default.
- W2120780012 hasConcept C14397066 @default.
- W2120780012 hasConcept C170493617 @default.
- W2120780012 hasConcept C178790620 @default.
- W2120780012 hasConcept C185592680 @default.
- W2120780012 hasConcept C201194858 @default.
- W2120780012 hasConcept C204921945 @default.
- W2120780012 hasConcept C2778938600 @default.
- W2120780012 hasConcept C2778981110 @default.
- W2120780012 hasConcept C2779281246 @default.
- W2120780012 hasConcept C2779564779 @default.
- W2120780012 hasConcept C2781063702 @default.
- W2120780012 hasConcept C2781338088 @default.
- W2120780012 hasConcept C521977710 @default.
- W2120780012 hasConcept C55493867 @default.
- W2120780012 hasConcept C71240020 @default.
- W2120780012 hasConcept C88016717 @default.
- W2120780012 hasConceptScore W2120780012C116569031 @default.
- W2120780012 hasConceptScore W2120780012C141087196 @default.
- W2120780012 hasConceptScore W2120780012C14397066 @default.
- W2120780012 hasConceptScore W2120780012C170493617 @default.
- W2120780012 hasConceptScore W2120780012C178790620 @default.
- W2120780012 hasConceptScore W2120780012C185592680 @default.
- W2120780012 hasConceptScore W2120780012C201194858 @default.
- W2120780012 hasConceptScore W2120780012C204921945 @default.
- W2120780012 hasConceptScore W2120780012C2778938600 @default.
- W2120780012 hasConceptScore W2120780012C2778981110 @default.
- W2120780012 hasConceptScore W2120780012C2779281246 @default.
- W2120780012 hasConceptScore W2120780012C2779564779 @default.
- W2120780012 hasConceptScore W2120780012C2781063702 @default.
- W2120780012 hasConceptScore W2120780012C2781338088 @default.
- W2120780012 hasConceptScore W2120780012C521977710 @default.
- W2120780012 hasConceptScore W2120780012C55493867 @default.
- W2120780012 hasConceptScore W2120780012C71240020 @default.
- W2120780012 hasConceptScore W2120780012C88016717 @default.
- W2120780012 hasIssue "5" @default.
- W2120780012 hasLocation W21207800121 @default.
- W2120780012 hasLocation W21207800122 @default.
- W2120780012 hasLocation W21207800123 @default.
- W2120780012 hasOpenAccess W2120780012 @default.
- W2120780012 hasPrimaryLocation W21207800121 @default.
- W2120780012 hasRelatedWork W1971724091 @default.
- W2120780012 hasRelatedWork W1980921288 @default.
- W2120780012 hasRelatedWork W1993401992 @default.
- W2120780012 hasRelatedWork W2000231299 @default.
- W2120780012 hasRelatedWork W2045059440 @default.
- W2120780012 hasRelatedWork W2077781430 @default.
- W2120780012 hasRelatedWork W2078109202 @default.
- W2120780012 hasRelatedWork W2111128814 @default.
- W2120780012 hasRelatedWork W2120780012 @default.
- W2120780012 hasRelatedWork W2400264347 @default.
- W2120780012 hasVolume "39" @default.
- W2120780012 isParatext "false" @default.
- W2120780012 isRetracted "false" @default.
- W2120780012 magId "2120780012" @default.
- W2120780012 workType "article" @default.