Matches in SemOpenAlex for { <https://semopenalex.org/work/W2019464657> ?p ?o ?g. }
- W2019464657 endingPage "207" @default.
- W2019464657 startingPage "199" @default.
- W2019464657 abstract "In search for effective antagonist structures for the nociceptin (NOP) receptor, a number of N-acylated oligopeptides, including N-acyl tetra- and pentapeptides selective for the κ-opioid receptor, as well as N-acyl hexapeptides bearing the Ac-Arg-Tyr-Tyr-Arg-Ile-Lys (Ac-RYYRIK) core sequence originally isolated from combinatorial chemical libraries, were synthesized and studied in radioreceptor binding assays, [35S]GTPγS functional tests and in mouse vas deferens (MVD) bioassays. The properties of the novel antagonist candidates were compared to known antagonists. A new antagonist structure with a reduced, primer alcohol C-terminus, Ac-Arg-Tyr-Tyr-Arg-Ile-lysinol (Ac-RYYRIK-ol) was described in the mouse vas deferens tests, showing an equilibrium inhibitory constant value (Ke) of 2.44 nM, and no agonist effect at 10 μM ligand concentration. Schild-analysis indicated a clearly competitive interaction at the NOP receptor, whereas the peptide did not affect the action of the δ-opioid receptor agonist [d-Ala2,d-Leu5]enkephalin. Ac-RYYRIK-ol also exhibited a high affinity in [3H]nociceptin-NH2 binding competition assays using rat brain membranes. Agonist-induced G-protein activation via NOP receptors was studied in [35S]GTPγS binding stimulation assays by the use of both native brain tissue preparations and membranes from cultured CHO cells expressing recombinant nociceptin receptors. Ac-RYYRIK-ol displayed only weak intrinsic agonist activity, whereas it effectively inhibited the stimulation generated by nociceptin. The results support the high potency and antagonist nature of Ac-RYYRIK-ol and reveal important roles for both the N- and the C-terminal region of the molecule." @default.
- W2019464657 created "2016-06-24" @default.
- W2019464657 creator A5002878894 @default.
- W2019464657 creator A5011139745 @default.
- W2019464657 creator A5023678610 @default.
- W2019464657 creator A5025961417 @default.
- W2019464657 creator A5027880067 @default.
- W2019464657 creator A5044486787 @default.
- W2019464657 creator A5045100034 @default.
- W2019464657 creator A5061978169 @default.
- W2019464657 creator A5063615617 @default.
- W2019464657 creator A5066954927 @default.
- W2019464657 creator A5070023471 @default.
- W2019464657 creator A5073876245 @default.
- W2019464657 date "2004-11-01" @default.
- W2019464657 modified "2023-10-11" @default.
- W2019464657 title "Nociceptin antagonism: probing the receptor by N-acetyl oligopeptides" @default.
- W2019464657 cites W1598044684 @default.
- W2019464657 cites W191719900 @default.
- W2019464657 cites W1968344910 @default.
- W2019464657 cites W1973370124 @default.
- W2019464657 cites W1975668170 @default.
- W2019464657 cites W1976946888 @default.
- W2019464657 cites W1979692501 @default.
- W2019464657 cites W1983702349 @default.
- W2019464657 cites W1986077790 @default.
- W2019464657 cites W1988335071 @default.
- W2019464657 cites W1988402607 @default.
- W2019464657 cites W1990402206 @default.
- W2019464657 cites W1992718637 @default.
- W2019464657 cites W1993514196 @default.
- W2019464657 cites W2000762521 @default.
- W2019464657 cites W2002799969 @default.
- W2019464657 cites W2009006906 @default.
- W2019464657 cites W2014237020 @default.
- W2019464657 cites W2015766640 @default.
- W2019464657 cites W2016562510 @default.
- W2019464657 cites W2019237794 @default.
- W2019464657 cites W2020874927 @default.
- W2019464657 cites W2021928628 @default.
- W2019464657 cites W2022948613 @default.
- W2019464657 cites W2023012408 @default.
- W2019464657 cites W2024378142 @default.
- W2019464657 cites W2025068387 @default.
- W2019464657 cites W2030506713 @default.
- W2019464657 cites W2033715015 @default.
- W2019464657 cites W2035041777 @default.
- W2019464657 cites W2039648325 @default.
- W2019464657 cites W2049571174 @default.
- W2019464657 cites W2050728278 @default.
- W2019464657 cites W2051889741 @default.
- W2019464657 cites W2052394143 @default.
- W2019464657 cites W2053284320 @default.
- W2019464657 cites W2053427358 @default.
- W2019464657 cites W2066624199 @default.
- W2019464657 cites W2071846673 @default.
- W2019464657 cites W2072158907 @default.
- W2019464657 cites W2075963772 @default.
- W2019464657 cites W2076527193 @default.
- W2019464657 cites W2079172002 @default.
- W2019464657 cites W2081085830 @default.
- W2019464657 cites W2083433463 @default.
- W2019464657 cites W2086165260 @default.
- W2019464657 cites W2089467147 @default.
- W2019464657 cites W2313401199 @default.
- W2019464657 doi "https://doi.org/10.1016/j.regpep.2004.06.019" @default.
- W2019464657 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/15491792" @default.
- W2019464657 hasPublicationYear "2004" @default.
- W2019464657 type Work @default.
- W2019464657 sameAs 2019464657 @default.
- W2019464657 citedByCount "20" @default.
- W2019464657 countsByYear W20194646572013 @default.
- W2019464657 countsByYear W20194646572015 @default.
- W2019464657 countsByYear W20194646572018 @default.
- W2019464657 crossrefType "journal-article" @default.
- W2019464657 hasAuthorship W2019464657A5002878894 @default.
- W2019464657 hasAuthorship W2019464657A5011139745 @default.
- W2019464657 hasAuthorship W2019464657A5023678610 @default.
- W2019464657 hasAuthorship W2019464657A5025961417 @default.
- W2019464657 hasAuthorship W2019464657A5027880067 @default.
- W2019464657 hasAuthorship W2019464657A5044486787 @default.
- W2019464657 hasAuthorship W2019464657A5045100034 @default.
- W2019464657 hasAuthorship W2019464657A5061978169 @default.
- W2019464657 hasAuthorship W2019464657A5063615617 @default.
- W2019464657 hasAuthorship W2019464657A5066954927 @default.
- W2019464657 hasAuthorship W2019464657A5070023471 @default.
- W2019464657 hasAuthorship W2019464657A5073876245 @default.
- W2019464657 hasConcept C125439840 @default.
- W2019464657 hasConcept C159023312 @default.
- W2019464657 hasConcept C170493617 @default.
- W2019464657 hasConcept C185592680 @default.
- W2019464657 hasConcept C2776885963 @default.
- W2019464657 hasConcept C2777803847 @default.
- W2019464657 hasConcept C2778684643 @default.
- W2019464657 hasConcept C2778938600 @default.
- W2019464657 hasConcept C2779886867 @default.
- W2019464657 hasConcept C2781063702 @default.
- W2019464657 hasConcept C55493867 @default.