Matches in SemOpenAlex for { <https://semopenalex.org/work/W2154866319> ?p ?o ?g. }
Showing items 1 to 85 of
85
with 100 items per page.
- W2154866319 endingPage "99" @default.
- W2154866319 startingPage "91" @default.
- W2154866319 abstract "Guanabenz (E-2,6-dichlorobenzylideneaminoguanidine acetate, Wy-8678) and its identified metabolites were tested for their ability to displace [3H]clonidine from the cerebral α2-receptors of rat and dog. The Kj's for inhibition of [3H]clonidine binding to rat membranes were 1.97, 0.96, 14.0, and 108 nM for clonidine, guanabenz, p-hydroxyguanabenz, and the Z-isomer of guanabenz, respectively. The other metabolites at concentrations of 10,000 nM did not displace [3H]clonidine. Scatchard analysis indicated single populations of binding sites with KD' s of 2.37 and 2.39 nM and Bmax's of 5.39 and 5.12 pmol/g for rat and dog preparations, respectively. Hill analysis yielded coefficients approximating unity, indicating a lack of cooperativity in binding. The high affinity of guanabenz relative to that of its metabolites for the α2-receptor provided the basis for the development of an assay capable of discriminating guanabenz from its weakly hypotensive (p-hydroxyguanabenz and the Z-isomer of guanabenz) and pharmacologically inactive (2–6, dichlorobenzyl alcohol,2,6-dichlorobenzaldehyde, 2,6-dichlorobenzaldehyde azine, 2,6-dichlorobenzaldehyde semicarbizone, creatinine adduct of 2,6-dichlorobenzaldehyde, and an isomer of the creatinine adduct) metabolites. Antihypertensive agents with different mechanisms of action such as indoramin, prazosin, debrisoquine, and bethanidine bound little, if at all, and thus will not interfere with the assay of guanabenz." @default.
- W2154866319 created "2016-06-24" @default.
- W2154866319 creator A5006521742 @default.
- W2154866319 creator A5049064009 @default.
- W2154866319 creator A5068601126 @default.
- W2154866319 creator A5090485785 @default.
- W2154866319 date "1983-01-01" @default.
- W2154866319 modified "2023-09-27" @default.
- W2154866319 title "Differential binding of guanabenz and its metabolites to cerebral ?2-receptors: The basis for a radioligand assay specific for the drug" @default.
- W2154866319 cites W1968656936 @default.
- W2154866319 cites W1977715056 @default.
- W2154866319 cites W1998845488 @default.
- W2154866319 cites W2049922557 @default.
- W2154866319 cites W2055573624 @default.
- W2154866319 cites W2074631079 @default.
- W2154866319 cites W2076380276 @default.
- W2154866319 cites W2081992620 @default.
- W2154866319 cites W2085111713 @default.
- W2154866319 cites W2162516461 @default.
- W2154866319 cites W2184350871 @default.
- W2154866319 cites W2395206925 @default.
- W2154866319 cites W2414674564 @default.
- W2154866319 doi "https://doi.org/10.1002/ddr.430030111" @default.
- W2154866319 hasPublicationYear "1983" @default.
- W2154866319 type Work @default.
- W2154866319 sameAs 2154866319 @default.
- W2154866319 citedByCount "10" @default.
- W2154866319 countsByYear W21548663192021 @default.
- W2154866319 countsByYear W21548663192023 @default.
- W2154866319 crossrefType "journal-article" @default.
- W2154866319 hasAuthorship W2154866319A5006521742 @default.
- W2154866319 hasAuthorship W2154866319A5049064009 @default.
- W2154866319 hasAuthorship W2154866319A5068601126 @default.
- W2154866319 hasAuthorship W2154866319A5090485785 @default.
- W2154866319 hasConcept C126322002 @default.
- W2154866319 hasConcept C134018914 @default.
- W2154866319 hasConcept C170493617 @default.
- W2154866319 hasConcept C185592680 @default.
- W2154866319 hasConcept C2776885963 @default.
- W2154866319 hasConcept C2778399450 @default.
- W2154866319 hasConcept C2778680573 @default.
- W2154866319 hasConcept C2778938600 @default.
- W2154866319 hasConcept C2780648677 @default.
- W2154866319 hasConcept C55493867 @default.
- W2154866319 hasConcept C67847695 @default.
- W2154866319 hasConcept C71240020 @default.
- W2154866319 hasConcept C71924100 @default.
- W2154866319 hasConcept C86803240 @default.
- W2154866319 hasConcept C98274493 @default.
- W2154866319 hasConceptScore W2154866319C126322002 @default.
- W2154866319 hasConceptScore W2154866319C134018914 @default.
- W2154866319 hasConceptScore W2154866319C170493617 @default.
- W2154866319 hasConceptScore W2154866319C185592680 @default.
- W2154866319 hasConceptScore W2154866319C2776885963 @default.
- W2154866319 hasConceptScore W2154866319C2778399450 @default.
- W2154866319 hasConceptScore W2154866319C2778680573 @default.
- W2154866319 hasConceptScore W2154866319C2778938600 @default.
- W2154866319 hasConceptScore W2154866319C2780648677 @default.
- W2154866319 hasConceptScore W2154866319C55493867 @default.
- W2154866319 hasConceptScore W2154866319C67847695 @default.
- W2154866319 hasConceptScore W2154866319C71240020 @default.
- W2154866319 hasConceptScore W2154866319C71924100 @default.
- W2154866319 hasConceptScore W2154866319C86803240 @default.
- W2154866319 hasConceptScore W2154866319C98274493 @default.
- W2154866319 hasIssue "1" @default.
- W2154866319 hasLocation W21548663191 @default.
- W2154866319 hasOpenAccess W2154866319 @default.
- W2154866319 hasPrimaryLocation W21548663191 @default.
- W2154866319 hasRelatedWork W1974745672 @default.
- W2154866319 hasRelatedWork W1980606392 @default.
- W2154866319 hasRelatedWork W1980753781 @default.
- W2154866319 hasRelatedWork W2001569974 @default.
- W2154866319 hasRelatedWork W2007942013 @default.
- W2154866319 hasRelatedWork W2037108296 @default.
- W2154866319 hasRelatedWork W2055714395 @default.
- W2154866319 hasRelatedWork W2067473655 @default.
- W2154866319 hasRelatedWork W2409055232 @default.
- W2154866319 hasRelatedWork W4242194979 @default.
- W2154866319 hasVolume "3" @default.
- W2154866319 isParatext "false" @default.
- W2154866319 isRetracted "false" @default.
- W2154866319 magId "2154866319" @default.
- W2154866319 workType "article" @default.