Matches in SemOpenAlex for { <https://semopenalex.org/work/W2414331310> ?p ?o ?g. }
Showing items 1 to 64 of
64
with 100 items per page.
- W2414331310 endingPage "40" @default.
- W2414331310 startingPage "534" @default.
- W2414331310 abstract "Brotizolam (2-bromo-4-(2-chlorophenyl)-9-methyl-6H-thieno[3,2-f]-1,2,4-triazolo [4,3-a]-1,4-diazepine, We 941, Lendormin) is a newly developed thienotriazolo-diazepine with distinct hypnotic effects. It was biochemically characterized by performing various receptor binding studies, uptake and release studies in vitro and determining homovanillic acid brain concentrations in vivo. Using [3H]-flunitrazepam as a radioligand, brotizolam showed an extremely high affinity for specific benzodiazepine binding sites in the rat brain, demonstrated by an IC50 value of 1.0 nmol/l. Using both [3H]-flunitrazepam and [3H]-brotizolam as radioligands, a strong correlation between the IC50 values of brotizolam and various benzodiazepines could be shown. [3H]-Flunitrazepam as well as [3H]-brotizolam bound with similar affinities to cerebellar and hippocampal synaptosomal membranes. In contrast to [3H]-flunitrazepam binding, however, [3H]-brotizolam had twice the number of specific binding sites in the hippocampus. According to the maximum binding of [3H]-flunitrazepam, the inhibition curve of brotizolam also increased in the presence of 10(-4) mol/l gamma-aminobutyric acid and decreased remarkably in the presence of 10(-4) mol/l bicuculline. Using [3H]-muscimol as a ligand, a modulating effect of brotizolam could be shown by increasing the low affinity with no change in the number of binding sites. From various further receptor binding studies, as well as from in vitro uptake and release studies of [3H]-noradrenaline, [3H]-serotonin and [3H]-dopamine, no indication was found of another biochemical effect of brotizolam. There was also no change in the homovanillic acid concentration in the rat brain striata in vivo after brotizolam treatment.(ABSTRACT TRUNCATED AT 250 WORDS)" @default.
- W2414331310 created "2016-06-24" @default.
- W2414331310 creator A5000724574 @default.
- W2414331310 creator A5035445978 @default.
- W2414331310 creator A5051347113 @default.
- W2414331310 date "1986-03-01" @default.
- W2414331310 modified "2023-09-23" @default.
- W2414331310 title "Biochemical studies with the new thienotriazolo-diazepine brotizolam." @default.
- W2414331310 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/3013211" @default.
- W2414331310 hasPublicationYear "1986" @default.
- W2414331310 type Work @default.
- W2414331310 sameAs 2414331310 @default.
- W2414331310 citedByCount "2" @default.
- W2414331310 crossrefType "journal-article" @default.
- W2414331310 hasAuthorship W2414331310A5000724574 @default.
- W2414331310 hasAuthorship W2414331310A5035445978 @default.
- W2414331310 hasAuthorship W2414331310A5051347113 @default.
- W2414331310 hasConcept C107824862 @default.
- W2414331310 hasConcept C126322002 @default.
- W2414331310 hasConcept C134018914 @default.
- W2414331310 hasConcept C170493617 @default.
- W2414331310 hasConcept C185592680 @default.
- W2414331310 hasConcept C2777810057 @default.
- W2414331310 hasConcept C2778173252 @default.
- W2414331310 hasConcept C2779738154 @default.
- W2414331310 hasConcept C2780930544 @default.
- W2414331310 hasConcept C2781442855 @default.
- W2414331310 hasConcept C55493867 @default.
- W2414331310 hasConcept C71924100 @default.
- W2414331310 hasConcept C98274493 @default.
- W2414331310 hasConceptScore W2414331310C107824862 @default.
- W2414331310 hasConceptScore W2414331310C126322002 @default.
- W2414331310 hasConceptScore W2414331310C134018914 @default.
- W2414331310 hasConceptScore W2414331310C170493617 @default.
- W2414331310 hasConceptScore W2414331310C185592680 @default.
- W2414331310 hasConceptScore W2414331310C2777810057 @default.
- W2414331310 hasConceptScore W2414331310C2778173252 @default.
- W2414331310 hasConceptScore W2414331310C2779738154 @default.
- W2414331310 hasConceptScore W2414331310C2780930544 @default.
- W2414331310 hasConceptScore W2414331310C2781442855 @default.
- W2414331310 hasConceptScore W2414331310C55493867 @default.
- W2414331310 hasConceptScore W2414331310C71924100 @default.
- W2414331310 hasConceptScore W2414331310C98274493 @default.
- W2414331310 hasIssue "3A" @default.
- W2414331310 hasLocation W24143313101 @default.
- W2414331310 hasOpenAccess W2414331310 @default.
- W2414331310 hasPrimaryLocation W24143313101 @default.
- W2414331310 hasRelatedWork W105174322 @default.
- W2414331310 hasRelatedWork W1993381432 @default.
- W2414331310 hasRelatedWork W2005704592 @default.
- W2414331310 hasRelatedWork W2019765032 @default.
- W2414331310 hasRelatedWork W2058391632 @default.
- W2414331310 hasRelatedWork W2122083355 @default.
- W2414331310 hasRelatedWork W2134141889 @default.
- W2414331310 hasRelatedWork W2135511048 @default.
- W2414331310 hasRelatedWork W2300698885 @default.
- W2414331310 hasRelatedWork W2473415771 @default.
- W2414331310 hasVolume "36" @default.
- W2414331310 isParatext "false" @default.
- W2414331310 isRetracted "false" @default.
- W2414331310 magId "2414331310" @default.
- W2414331310 workType "article" @default.