Matches in SemOpenAlex for { <https://semopenalex.org/work/W2000938898> ?p ?o ?g. }
Showing items 1 to 82 of
82
with 100 items per page.
- W2000938898 endingPage "1491" @default.
- W2000938898 startingPage "1485" @default.
- W2000938898 abstract "Using the Merrifield solid-phase method, we have synthesized 18 new 2-O-alkyltyrosine-substituted analogues (where alkyl = methyl and ethyl) of the arginine-vasopressin (AVP) vasopressor antagonists [1-deaminopenicillamine]-arginine-vasopressin (dPAVP), [1-(beta-mercapto-beta,beta-diethylpropionic acid)]arginine-vasopressin (dEt2AVP), and [1-(beta-mercapto-beta,beta-cyclopentamethylenepropionic acid)]arginine-vasopressin (d(CH2)5AVP) and of their 8-D-arginine (d(R2)DAVP) analogues, their 4-valine (dR2VAVP) analogues, and their 4-valine,8-D-arginine (d(R2)VDAVP) analogues [where R = CH3 or C2H5 and 2R = (CH2)5]. These analogues were tested for agonistic and antagonistic activities in in vivo rat vasopressor and rat antidiuretic and in vitro rat uterus assay systems. Although many exhibit very low antidiuretic activities, none of the new analogues antagonize antidiuretic responses to AVP. They exhibit no evident pressor activities and are in fact all highly effective antagonists of the vasopressor responses to AVP. They are also potent antagonists of the in vitro oxytocic responses to oxytocin, both in the absence and in the presence of Mg2+. These analogues together with their corresponding antivasopressor pA2 values are as follows: 1. dPTyr(Et)AVP, 8.40 +/- 0.08; 2. dEt2Tyr(Me)AVP, 8.53 +/- 0.06; 3. dEt2Tyr(Et)AVP, 8.46 +/- 0.08; 4. d(CH2)5Tyr(Et)AVP, 8.47 +/- 0.04; 5. dPTyr(Me)DAVP, 8.31 +/- 0.08; 6. dPTyr(Et)DAVP, 8.27 +/- 0.06; 7. dEt2Tyr(Me)DAVP, 8.57 +/- 0.03; 8. dEt2Tyr(Et)DAVP, 8.33 +/- 0.06; 9. d(CH2)5Tyr(Me)DAVP, 8.41 +/- 0.05; 10. d(CH2)5Tyr(Et)DAVP, 8.45 +/- 0.05; 11. dPTyr(Me)VAVP, 8.36 +/- 0.07; 12. dPTyr(Et)VAVP, 8.07 +/- 0.13; 13. dEt2Tyr(Me)VAVP, 8.29 +/- 0.08; 14. dEt2Tyr(Et)VAVP, 8.42 +/- 0.06; 15. dPTyr(Me)VDAVP, 7.84 +/- 0.06; 16. dPTyr(Et)VDAVP, 8.46 +/- 0.03; 17. dET2Tyr(Me)VDAVP, 8.35 +/- 0.10; 18. dEt2Tyr (Et)VDAVP, 8.19 +/- 0.07. Seven of these analogues are clearly more potent vasopressor antagonists than their respective unalkylated tyrosine-containing parents. In the remaining 11, antagonistic potency was not changed significantly. In no instance did 2-O-alkyltyrosine substitution decrease antagonistic potency. With pA2 values equal to or greater than 8.40, nine of these antagonists (numbers 1-4, 7, 9, 10, 14, and 16) are among the most potent vasopressor antagonists reported to date. They could thus serve as additional valuable pharmacological tools in studies on the roles of AVP in the control of blood pressure in normal and in pathophysiological conditions. These findings may also provide useful clues to the design of more potent and selective antagonists of AVP." @default.
- W2000938898 created "2016-06-24" @default.
- W2000938898 creator A5019752727 @default.
- W2000938898 creator A5022185589 @default.
- W2000938898 creator A5079883467 @default.
- W2000938898 creator A5086458513 @default.
- W2000938898 creator A5090391240 @default.
- W2000938898 date "1985-10-01" @default.
- W2000938898 modified "2023-09-23" @default.
- W2000938898 title "Synthesis and some pharmacological properties of 18 potent O-alkyltyrosine-substituted antagonists of the vasopressor responses to arginine-vasopressin" @default.
- W2000938898 doi "https://doi.org/10.1021/jm00148a019" @default.
- W2000938898 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/4045923" @default.
- W2000938898 hasPublicationYear "1985" @default.
- W2000938898 type Work @default.
- W2000938898 sameAs 2000938898 @default.
- W2000938898 citedByCount "17" @default.
- W2000938898 countsByYear W20009388982012 @default.
- W2000938898 countsByYear W20009388982016 @default.
- W2000938898 crossrefType "journal-article" @default.
- W2000938898 hasAuthorship W2000938898A5019752727 @default.
- W2000938898 hasAuthorship W2000938898A5022185589 @default.
- W2000938898 hasAuthorship W2000938898A5079883467 @default.
- W2000938898 hasAuthorship W2000938898A5086458513 @default.
- W2000938898 hasAuthorship W2000938898A5090391240 @default.
- W2000938898 hasConcept C126322002 @default.
- W2000938898 hasConcept C134018914 @default.
- W2000938898 hasConcept C150903083 @default.
- W2000938898 hasConcept C170493617 @default.
- W2000938898 hasConcept C185592680 @default.
- W2000938898 hasConcept C207001950 @default.
- W2000938898 hasConcept C2776176026 @default.
- W2000938898 hasConcept C2776370428 @default.
- W2000938898 hasConcept C2776885963 @default.
- W2000938898 hasConcept C2777468819 @default.
- W2000938898 hasConcept C2777573094 @default.
- W2000938898 hasConcept C2779420931 @default.
- W2000938898 hasConcept C2779881253 @default.
- W2000938898 hasConcept C515207424 @default.
- W2000938898 hasConcept C55493867 @default.
- W2000938898 hasConcept C71924100 @default.
- W2000938898 hasConcept C86803240 @default.
- W2000938898 hasConcept C90474776 @default.
- W2000938898 hasConceptScore W2000938898C126322002 @default.
- W2000938898 hasConceptScore W2000938898C134018914 @default.
- W2000938898 hasConceptScore W2000938898C150903083 @default.
- W2000938898 hasConceptScore W2000938898C170493617 @default.
- W2000938898 hasConceptScore W2000938898C185592680 @default.
- W2000938898 hasConceptScore W2000938898C207001950 @default.
- W2000938898 hasConceptScore W2000938898C2776176026 @default.
- W2000938898 hasConceptScore W2000938898C2776370428 @default.
- W2000938898 hasConceptScore W2000938898C2776885963 @default.
- W2000938898 hasConceptScore W2000938898C2777468819 @default.
- W2000938898 hasConceptScore W2000938898C2777573094 @default.
- W2000938898 hasConceptScore W2000938898C2779420931 @default.
- W2000938898 hasConceptScore W2000938898C2779881253 @default.
- W2000938898 hasConceptScore W2000938898C515207424 @default.
- W2000938898 hasConceptScore W2000938898C55493867 @default.
- W2000938898 hasConceptScore W2000938898C71924100 @default.
- W2000938898 hasConceptScore W2000938898C86803240 @default.
- W2000938898 hasConceptScore W2000938898C90474776 @default.
- W2000938898 hasIssue "10" @default.
- W2000938898 hasLocation W20009388981 @default.
- W2000938898 hasLocation W20009388982 @default.
- W2000938898 hasOpenAccess W2000938898 @default.
- W2000938898 hasPrimaryLocation W20009388981 @default.
- W2000938898 hasRelatedWork W105014381 @default.
- W2000938898 hasRelatedWork W1964596246 @default.
- W2000938898 hasRelatedWork W1984470734 @default.
- W2000938898 hasRelatedWork W1988627537 @default.
- W2000938898 hasRelatedWork W2006017029 @default.
- W2000938898 hasRelatedWork W2029964435 @default.
- W2000938898 hasRelatedWork W2041552780 @default.
- W2000938898 hasRelatedWork W2069292195 @default.
- W2000938898 hasRelatedWork W2088618831 @default.
- W2000938898 hasRelatedWork W2407537258 @default.
- W2000938898 hasVolume "28" @default.
- W2000938898 isParatext "false" @default.
- W2000938898 isRetracted "false" @default.
- W2000938898 magId "2000938898" @default.
- W2000938898 workType "article" @default.