FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2054359517> ?p ?o ?g. }

• W2054359517 endingPage "164" @default.
• W2054359517 startingPage "159" @default.
• W2054359517 abstract "DOPA has been proposed to be a neurotransmitter of the primary baroreceptor afferents terminating in the NTS and a neuromodulator in striata of rats. Pre- and post-synaptic recognition sites for DOPA itself may exist. DOPA methyl ester (DOPA ester), a potent competitive antagonist for DOPA in continuously superfused slices or within a several min when microinjected in the NIS has some limitation in in vivo use because of its unstableness as a prodrug for DOPA. We have explored to find stable and potent antagonists for DOPA. At first, we tried to clarify whether or not newly synthesized DOPA esters with bulky structure such as DOPA cyclohexyl ester (CHE), DOPA cyclopentyl ester (CPE) and DOPA cyclopentyldimethyl ester (CPDME) antagonize depressor responses to DOPA microinjected into the NTS, and to what degree these analogues 1 μM perfused via probes are converted to DOPA during striatal microdialysis in urethane-anesthetized rats. Then, we analyzed mode of antagonism of some candidate in the NTS system. During striatal microdialysis, DOPA ester 1 μM increased extracellular levels of DOPA to an 100 fold higher level at a peak of the 1st 20 min sample after the perfusion. Conversion ratio of CHE, CPE and CPDME, compared to DOPA ester, was less than 1/5 at the peak of the 3rd sample, 1/3.3 at the peak of the 2nd, and 1/2.7 at the peak of the 3rd, respectively. In the NTS, all analogues 1 μg microinjected abolished depressor responses to DOPA 60 ng. Time required to recover abase was 20 min for CHE and 10 min for DOPA ester, CPE and CPDME. At 100 ng, CHE inhibited peak depressor responses to DOPA 60 ng by 53%, CPE by 40%, and CPDME by 24%, compared to DOPA ester by 22%. Then, DOPA 10-300 ng microinjected produced dose-dependent hypotension. DOPA ester 300 ng, microinjected 1 min previously, shifted a dose-response curve for DOPA 30-300 ng to the right without reduction of the maximum response, showing a competitive mode of antagonism. CHE 30 ng competitively antagonized depressor responses to DOPA 18-300 ng without reduction of the maximum response. CHE 100 ng further shifted the dose-response curve for DOPA 18-100 ng to the right with 25% reduction of the maximum response. Antagonistic activity of CHE 100 ng was equipotent with DOPA ester 300 ng. CHE is a competitive antagonist including partially some noncompetitive components. A possible component might be related to NMDA receptors, since high concentrations of CHE displaced selective binding of [3H]-MK-801, an antagonist. In conclusion, CHE is suitable for the purpose." @default.
• W2054359517 created "2016-06-24" @default.
• W2054359517 creator A5000874955 @default.
• W2054359517 creator A5006467128 @default.
• W2054359517 creator A5030232088 @default.
• W2054359517 creator A5048426520 @default.
• W2054359517 creator A5049448328 @default.
• W2054359517 creator A5053016178 @default.
• W2054359517 creator A5057920466 @default.
• W2054359517 date "1997-01-01" @default.
• W2054359517 modified "2023-10-18" @default.
• W2054359517 title "Studies on novel, stable and potent competitive antagonists against L-DOPA" @default.
• W2054359517 cites W1550289802 @default.
• W2054359517 cites W1974171355 @default.
• W2054359517 cites W1987093122 @default.
• W2054359517 cites W1987351877 @default.
• W2054359517 cites W1989284003 @default.
• W2054359517 cites W1994705298 @default.
• W2054359517 cites W1996537104 @default.
• W2054359517 cites W2002481554 @default.
• W2054359517 cites W2007602640 @default.
• W2054359517 cites W2019833371 @default.
• W2054359517 cites W2020011596 @default.
• W2054359517 cites W2023929710 @default.
• W2054359517 cites W2033540911 @default.
• W2054359517 cites W2046583558 @default.
• W2054359517 cites W2067488590 @default.
• W2054359517 cites W2068813996 @default.
• W2054359517 cites W2097650432 @default.
• W2054359517 cites W2127886768 @default.
• W2054359517 cites W2231949118 @default.
• W2054359517 doi "https://doi.org/10.1254/fpj.110.supplement_159" @default.
• W2054359517 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/9503425" @default.
• W2054359517 hasPublicationYear "1997" @default.
• W2054359517 type Work @default.
• W2054359517 sameAs 2054359517 @default.
• W2054359517 citedByCount "0" @default.
• W2054359517 crossrefType "journal-article" @default.
• W2054359517 hasAuthorship W2054359517A5000874955 @default.
• W2054359517 hasAuthorship W2054359517A5006467128 @default.
• W2054359517 hasAuthorship W2054359517A5030232088 @default.
• W2054359517 hasAuthorship W2054359517A5048426520 @default.
• W2054359517 hasAuthorship W2054359517A5049448328 @default.
• W2054359517 hasAuthorship W2054359517A5053016178 @default.
• W2054359517 hasAuthorship W2054359517A5057920466 @default.
• W2054359517 hasBestOaLocation W20543595171 @default.
• W2054359517 hasConcept C108215921 @default.
• W2054359517 hasConcept C126322002 @default.
• W2054359517 hasConcept C134018914 @default.
• W2054359517 hasConcept C146957229 @default.
• W2054359517 hasConcept C150903083 @default.
• W2054359517 hasConcept C170493617 @default.
• W2054359517 hasConcept C185592680 @default.
• W2054359517 hasConcept C207001950 @default.
• W2054359517 hasConcept C2776219046 @default.
• W2054359517 hasConcept C2776885963 @default.
• W2054359517 hasConcept C2777440324 @default.
• W2054359517 hasConcept C28406088 @default.
• W2054359517 hasConcept C50156730 @default.
• W2054359517 hasConcept C513476851 @default.
• W2054359517 hasConcept C55493867 @default.
• W2054359517 hasConcept C71924100 @default.
• W2054359517 hasConcept C86803240 @default.
• W2054359517 hasConcept C98274493 @default.
• W2054359517 hasConceptScore W2054359517C108215921 @default.
• W2054359517 hasConceptScore W2054359517C126322002 @default.
• W2054359517 hasConceptScore W2054359517C134018914 @default.
• W2054359517 hasConceptScore W2054359517C146957229 @default.
• W2054359517 hasConceptScore W2054359517C150903083 @default.
• W2054359517 hasConceptScore W2054359517C170493617 @default.
• W2054359517 hasConceptScore W2054359517C185592680 @default.
• W2054359517 hasConceptScore W2054359517C207001950 @default.
• W2054359517 hasConceptScore W2054359517C2776219046 @default.
• W2054359517 hasConceptScore W2054359517C2776885963 @default.
• W2054359517 hasConceptScore W2054359517C2777440324 @default.
• W2054359517 hasConceptScore W2054359517C28406088 @default.
• W2054359517 hasConceptScore W2054359517C50156730 @default.
• W2054359517 hasConceptScore W2054359517C513476851 @default.
• W2054359517 hasConceptScore W2054359517C55493867 @default.
• W2054359517 hasConceptScore W2054359517C71924100 @default.
• W2054359517 hasConceptScore W2054359517C86803240 @default.
• W2054359517 hasConceptScore W2054359517C98274493 @default.
• W2054359517 hasIssue "supplement" @default.
• W2054359517 hasLocation W20543595171 @default.
• W2054359517 hasLocation W20543595172 @default.
• W2054359517 hasOpenAccess W2054359517 @default.
• W2054359517 hasPrimaryLocation W20543595171 @default.
• W2054359517 hasRelatedWork W1988430023 @default.
• W2054359517 hasRelatedWork W1990453785 @default.
• W2054359517 hasRelatedWork W2007992019 @default.
• W2054359517 hasRelatedWork W2055584145 @default.
• W2054359517 hasRelatedWork W2088135425 @default.
• W2054359517 hasRelatedWork W2088291993 @default.
• W2054359517 hasRelatedWork W2093177172 @default.
• W2054359517 hasRelatedWork W2416099545 @default.
• W2054359517 hasRelatedWork W3099760284 @default.
• W2054359517 hasRelatedWork W3199803549 @default.
• W2054359517 hasVolume "110" @default.

• next