FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W1990738023> ?p ?o ?g. }

• W1990738023 endingPage "391" @default.
• W1990738023 startingPage "382" @default.
• W1990738023 abstract "We describe the synthesis and some pharmacological properties of 16 new in vivo antagonists of oxytocin. These are based on modifications of three peptides: A, B, and C. A is our previously reported potent and selective antagonist of the vasopressor (V1 receptor) responses to arginine-vasopressin (AVP)/weak oxytocin antagonist, [1-(beta-mercapto-beta,beta-pentamethylenepropionic acid), 2-O-methyltyrosine]arginine-vasopressin (d(CH2)5[Tyr(Me)2]AVP. B reported here, the Ile3 analogue of A, is d(CH2)5[Tyr(Me)2]AVT (5 below) and C is our previously reported potent nonselective oxytocin antagonist/AVP V1 antagonist, [1-(beta-mercapto-beta,beta-pentamethylenepropionic acid),2-O- methyltyrosine,8-ornithine]vasotocin (d(CH2)5[Tyr(Me)2]OVT). The following substitutions and deletions, alone or in combination, were employed in A, B, and C: 1-deaminopenicillamine (dP); D-Tyr(Alk)2 (where Alk = Me or Et), D-Phe2; Val4, Thr4; delta 3-Pro7; Lys8, Cit8; desGly9, desGly-NH2(9), Ala-NH2(9); Leu-NH2(9); Arg-NH2(9). The 16 new analogues are (1) d(CH2)5[D-Tyr(Me)2]AVP, (2) d(CH2)5[D-Tyr(Me)2, Val4,delta 3-Pro7]AVP, (3) d(CH2)5[D-Tyr-(Et)2, Val4,Lys8]VP, (4) d(CH2)5[D-Tyr(Et)2,Val4,Cit8]VP, (5) d(CH2)5[Tyr(Me)2]AVT, (6) d(CH2)5[Tyr(Me)2,Lys8]VT, (7) dP[Tyr(Me)2]AVT, (8) dP[Tyr(Me)2,Val4]AVT, (9) d(CH2)5[D-Tyr(Me)2, Val4]AVT, (10) d(CH2)5[D-Phe2,Val4]AVT, (11) d(CH2)5[Tyr(Me)2,Thr4]OVT, (12) d(CH2)5[Tyr(Me)2,Thr4,Ala-NH2(9)]OVT, (13) d(CH2)5[Tyr(Me)2,Thr4,Leu-NH2(9)]OVT, (14) d(CH2)5[Tyr(Me)2,Thr4,Arg-NH2(9)]OVT, (15) desGly-NH2(9),d(CH2)5[Tyr(Me)2,Thr4]OVT, (16) desGly9,d(CH2)5[Tyr(Me)2,Thr4]OVT. 1-4 are analogues of A, 5-10 are analogues of B, and 11-16 are analogues of C. Their protected precursors were synthesized either entirely by the solid-phase method or by a combination of solid-phase and solution methods (1 + 8 or 8 + 1 couplings). All analogues were tested in rats for agonistic and antagonistic activities in oxytocic (in vitro, without and with Mg2+, and in vivo) assays as well as by antidiuretic and vasopressor assays. All analogues exhibit potent oxytocic antagonism in vitro and in vivo. With an in vitro pA2 (in the absence of Mg2+) = 9.12 +/- 0.09, dP[Tyr(Me)2]AVT is (7) one of the most potent in vitro oxytocin antagonists reported to date. Fifteen of these analogues (all but 6) appear as potent or more potent in vivo oxytocin antagonists than C (pA2 = 7.37 +/- 0.17). Analogues 1-9 and 14 are potent AVP V1 antagonists. Their anti-V1 pA2 values range from 7.92 to 8.45. They are thus nonselective oxytocin antagonists.(ABSTRACT TRUNCATED AT 400 WORDS)" @default.
• W1990738023 created "2016-06-24" @default.
• W1990738023 creator A5002268768 @default.
• W1990738023 creator A5004687937 @default.
• W1990738023 creator A5019752727 @default.
• W1990738023 creator A5022185589 @default.
• W1990738023 creator A5052093356 @default.
• W1990738023 creator A5070707400 @default.
• W1990738023 creator A5079883467 @default.
• W1990738023 creator A5082031784 @default.
• W1990738023 creator A5086458513 @default.
• W1990738023 creator A5090391240 @default.
• W1990738023 date "1989-02-01" @default.
• W1990738023 modified "2023-10-16" @default.
• W1990738023 title "Solid-phase synthesis of 16 potent (selective and nonselective) in vivo antagonists of oxytocin" @default.
• W1990738023 doi "https://doi.org/10.1021/jm00122a016" @default.
• W1990738023 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/2913298" @default.
• W1990738023 hasPublicationYear "1989" @default.
• W1990738023 type Work @default.
• W1990738023 sameAs 1990738023 @default.
• W1990738023 citedByCount "103" @default.
• W1990738023 countsByYear W19907380232012 @default.
• W1990738023 countsByYear W19907380232013 @default.
• W1990738023 countsByYear W19907380232014 @default.
• W1990738023 countsByYear W19907380232015 @default.
• W1990738023 countsByYear W19907380232016 @default.
• W1990738023 countsByYear W19907380232018 @default.
• W1990738023 countsByYear W19907380232019 @default.
• W1990738023 countsByYear W19907380232021 @default.
• W1990738023 countsByYear W19907380232022 @default.
• W1990738023 crossrefType "journal-article" @default.
• W1990738023 hasAuthorship W1990738023A5002268768 @default.
• W1990738023 hasAuthorship W1990738023A5004687937 @default.
• W1990738023 hasAuthorship W1990738023A5019752727 @default.
• W1990738023 hasAuthorship W1990738023A5022185589 @default.
• W1990738023 hasAuthorship W1990738023A5052093356 @default.
• W1990738023 hasAuthorship W1990738023A5070707400 @default.
• W1990738023 hasAuthorship W1990738023A5079883467 @default.
• W1990738023 hasAuthorship W1990738023A5082031784 @default.
• W1990738023 hasAuthorship W1990738023A5086458513 @default.
• W1990738023 hasAuthorship W1990738023A5090391240 @default.
• W1990738023 hasConcept C118303440 @default.
• W1990738023 hasConcept C126322002 @default.
• W1990738023 hasConcept C134018914 @default.
• W1990738023 hasConcept C150903083 @default.
• W1990738023 hasConcept C170493617 @default.
• W1990738023 hasConcept C185592680 @default.
• W1990738023 hasConcept C207001950 @default.
• W1990738023 hasConcept C2776176026 @default.
• W1990738023 hasConcept C2776370428 @default.
• W1990738023 hasConcept C2776885963 @default.
• W1990738023 hasConcept C2777468819 @default.
• W1990738023 hasConcept C2779135415 @default.
• W1990738023 hasConcept C515207424 @default.
• W1990738023 hasConcept C55493867 @default.
• W1990738023 hasConcept C71240020 @default.
• W1990738023 hasConcept C71924100 @default.
• W1990738023 hasConcept C86803240 @default.
• W1990738023 hasConceptScore W1990738023C118303440 @default.
• W1990738023 hasConceptScore W1990738023C126322002 @default.
• W1990738023 hasConceptScore W1990738023C134018914 @default.
• W1990738023 hasConceptScore W1990738023C150903083 @default.
• W1990738023 hasConceptScore W1990738023C170493617 @default.
• W1990738023 hasConceptScore W1990738023C185592680 @default.
• W1990738023 hasConceptScore W1990738023C207001950 @default.
• W1990738023 hasConceptScore W1990738023C2776176026 @default.
• W1990738023 hasConceptScore W1990738023C2776370428 @default.
• W1990738023 hasConceptScore W1990738023C2776885963 @default.
• W1990738023 hasConceptScore W1990738023C2777468819 @default.
• W1990738023 hasConceptScore W1990738023C2779135415 @default.
• W1990738023 hasConceptScore W1990738023C515207424 @default.
• W1990738023 hasConceptScore W1990738023C55493867 @default.
• W1990738023 hasConceptScore W1990738023C71240020 @default.
• W1990738023 hasConceptScore W1990738023C71924100 @default.
• W1990738023 hasConceptScore W1990738023C86803240 @default.
• W1990738023 hasIssue "2" @default.
• W1990738023 hasLocation W19907380231 @default.
• W1990738023 hasLocation W19907380232 @default.
• W1990738023 hasOpenAccess W1990738023 @default.
• W1990738023 hasPrimaryLocation W19907380231 @default.
• W1990738023 hasRelatedWork W1980066808 @default.
• W1990738023 hasRelatedWork W1984470734 @default.
• W1990738023 hasRelatedWork W1988627537 @default.
• W1990738023 hasRelatedWork W2006017029 @default.
• W1990738023 hasRelatedWork W2009418740 @default.
• W1990738023 hasRelatedWork W2021472254 @default.
• W1990738023 hasRelatedWork W2069292195 @default.
• W1990738023 hasRelatedWork W2088618831 @default.
• W1990738023 hasRelatedWork W3035096519 @default.
• W1990738023 hasRelatedWork W2407537258 @default.
• W1990738023 hasVolume "32" @default.
• W1990738023 isParatext "false" @default.
• W1990738023 isRetracted "false" @default.
• W1990738023 magId "1990738023" @default.
• W1990738023 workType "article" @default.