Matches in SemOpenAlex for { <https://semopenalex.org/work/W1989151505> ?p ?o ?g. }
- W1989151505 endingPage "1454" @default.
- W1989151505 startingPage "1444" @default.
- W1989151505 abstract "Several derivatives and analogues of the general anaesthetic 2,6-diisopropylphenol (propofol) have been recently synthesised with the aim of exploring the structure-activity relationships. In the present study, the effects of one such compound, 4-iodo-2,6-diisopropylphenol (4-I-Pro), on γ-aminobutyric acid type A (GABAA) receptors in vitro were compared with its in vivo effects in rodents. Human GABAA receptors were expressed in Xenopus oocytes, and the actions of 4-I-Pro on receptor function were compared with those of propofol by two-electrode voltage-clamp recording. Similar to propofol, 4-I-Pro directly activated Cl− currents in the absence of GABA at all combinations of receptor subunits tested. However, the efficacy of 4-I-Pro in inducing direct activation of α1β2γ2S receptors was markedly less than that of propofol. Similarly to propofol, 4-I-Pro potentiated in a concentration-dependent manner GABA-evoked Cl− currents measured at different GABAA receptor constructs. As expected, intraperitoneal injection of propofol induced sedation, ataxia, and loss of the righting reflex in rats. In contrast, administration of 4-I-Pro failed to produce any of these behavioural effects. Administration of 4-I-Pro to rats reduced in a dose-dependent manner the incidence of tonic-clonic seizures induced by pentylenetetrazol and induced an anticonflict effect as measured in the Vogel test. Microdialysis revealed that, like propofol, administration of 4-I-Pro reduced acetylcholine release in the hippocampus of freely moving rats. These results demonstrate that para-substitution of the phenol ring of propofol with iodine yields a compound that exhibits anticonvulsant and anticonflict effects, but is devoid of sedative-hypnotic and anaesthetic properties. Thus, 4-I-Pro possesses pharmacological characteristics more similar to anxiolytic and anticonvulsant drugs than to general anaesthetics. British Journal of Pharmacology (1999) 126, 1444–1454; doi:10.1038/sj.bjp.0702449" @default.
- W1989151505 created "2016-06-24" @default.
- W1989151505 creator A5028115615 @default.
- W1989151505 creator A5033665710 @default.
- W1989151505 creator A5036328704 @default.
- W1989151505 creator A5065508661 @default.
- W1989151505 creator A5066081782 @default.
- W1989151505 creator A5080033292 @default.
- W1989151505 creator A5080871062 @default.
- W1989151505 creator A5083331235 @default.
- W1989151505 creator A5090509427 @default.
- W1989151505 creator A5090548570 @default.
- W1989151505 date "1999-03-01" @default.
- W1989151505 modified "2023-10-10" @default.
- W1989151505 title "Characterization of the electrophysiological and pharmacological effects of 4-iodo-2,6-diisopropylphenol, a propofol analogue devoid of sedative-anaesthetic properties" @default.
- W1989151505 cites W1001819427 @default.
- W1989151505 cites W1668093331 @default.
- W1989151505 cites W1750985838 @default.
- W1989151505 cites W1757874161 @default.
- W1989151505 cites W1911099943 @default.
- W1989151505 cites W1954401748 @default.
- W1989151505 cites W1963046602 @default.
- W1989151505 cites W1963517504 @default.
- W1989151505 cites W1968452865 @default.
- W1989151505 cites W1968875887 @default.
- W1989151505 cites W1978013837 @default.
- W1989151505 cites W1995800815 @default.
- W1989151505 cites W1999394080 @default.
- W1989151505 cites W2009159885 @default.
- W1989151505 cites W2034230488 @default.
- W1989151505 cites W2036297239 @default.
- W1989151505 cites W2036887677 @default.
- W1989151505 cites W2045995579 @default.
- W1989151505 cites W2047080686 @default.
- W1989151505 cites W2051919399 @default.
- W1989151505 cites W2053592987 @default.
- W1989151505 cites W2053659412 @default.
- W1989151505 cites W2056855842 @default.
- W1989151505 cites W2065750640 @default.
- W1989151505 cites W2081025398 @default.
- W1989151505 cites W2090050109 @default.
- W1989151505 cites W2092273976 @default.
- W1989151505 cites W2106001183 @default.
- W1989151505 cites W2161846844 @default.
- W1989151505 cites W2168205523 @default.
- W1989151505 cites W2172077992 @default.
- W1989151505 cites W2266582081 @default.
- W1989151505 cites W2289222529 @default.
- W1989151505 cites W2337845188 @default.
- W1989151505 cites W2405577466 @default.
- W1989151505 cites W2419447906 @default.
- W1989151505 cites W4291746756 @default.
- W1989151505 doi "https://doi.org/10.1038/sj.bjp.0702449" @default.
- W1989151505 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/1565920" @default.
- W1989151505 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/10217539" @default.
- W1989151505 hasPublicationYear "1999" @default.
- W1989151505 type Work @default.
- W1989151505 sameAs 1989151505 @default.
- W1989151505 citedByCount "31" @default.
- W1989151505 countsByYear W19891515052013 @default.
- W1989151505 countsByYear W19891515052014 @default.
- W1989151505 countsByYear W19891515052015 @default.
- W1989151505 countsByYear W19891515052017 @default.
- W1989151505 countsByYear W19891515052020 @default.
- W1989151505 countsByYear W19891515052021 @default.
- W1989151505 crossrefType "journal-article" @default.
- W1989151505 hasAuthorship W1989151505A5028115615 @default.
- W1989151505 hasAuthorship W1989151505A5033665710 @default.
- W1989151505 hasAuthorship W1989151505A5036328704 @default.
- W1989151505 hasAuthorship W1989151505A5065508661 @default.
- W1989151505 hasAuthorship W1989151505A5066081782 @default.
- W1989151505 hasAuthorship W1989151505A5080033292 @default.
- W1989151505 hasAuthorship W1989151505A5080871062 @default.
- W1989151505 hasAuthorship W1989151505A5083331235 @default.
- W1989151505 hasAuthorship W1989151505A5090509427 @default.
- W1989151505 hasAuthorship W1989151505A5090548570 @default.
- W1989151505 hasBestOaLocation W19891515052 @default.
- W1989151505 hasConcept C126322002 @default.
- W1989151505 hasConcept C168258287 @default.
- W1989151505 hasConcept C169760540 @default.
- W1989151505 hasConcept C170493617 @default.
- W1989151505 hasConcept C185263204 @default.
- W1989151505 hasConcept C185592680 @default.
- W1989151505 hasConcept C2775858608 @default.
- W1989151505 hasConcept C2776277131 @default.
- W1989151505 hasConcept C2778186239 @default.
- W1989151505 hasConcept C42219234 @default.
- W1989151505 hasConcept C55493867 @default.
- W1989151505 hasConcept C71924100 @default.
- W1989151505 hasConcept C86803240 @default.
- W1989151505 hasConcept C98274493 @default.
- W1989151505 hasConceptScore W1989151505C126322002 @default.
- W1989151505 hasConceptScore W1989151505C168258287 @default.
- W1989151505 hasConceptScore W1989151505C169760540 @default.
- W1989151505 hasConceptScore W1989151505C170493617 @default.
- W1989151505 hasConceptScore W1989151505C185263204 @default.
- W1989151505 hasConceptScore W1989151505C185592680 @default.
- W1989151505 hasConceptScore W1989151505C2775858608 @default.