Matches in SemOpenAlex for { <https://semopenalex.org/work/W2201538478> ?p ?o ?g. }
- W2201538478 endingPage "75" @default.
- W2201538478 startingPage "1264" @default.
- W2201538478 abstract "A series of novel tricyclic pyrido-phthalazine-dione derivatives was tested for antagonistic effects at the strychnine-insensitive modulatory site of the N-methyl-D-aspartate (NMDA) receptor (glycineB). All compounds displaced [3H]MDL-105,519 binding to rat cortical membranes with IC50 values of between 90 nM and 3.6 microM. In patch-clamp experiments, steady-state inward current responses of cultured hippocampal neurons to NMDA (200 microM, glycine 1 microM) were antagonized by these same compounds with IC50 values of 0.14 to 13.8 microM. The antagonism observed was typical for glycineB antagonists, i.e., they induced desensitization and their effects were not use or voltage dependent. Moreover, increasing concentrations of glycine were able to decrease their apparent potency. Much higher concentrations (>100 microM) were required to antagonize alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid-induced currents. They were potent, systemically active NMDA receptor antagonists in vivo against responses of single neurons in the rat spinal cord to microelectrophoretic application of NMDA with ID50 values in the low milligram per kilogram i.v. range. They also inhibited pentylenetetrazol-, NMDA- and maximal electroshock-induced convulsions in mice with ED50 values ranging from 8 to 100 mg/kg i.p. The duration of anticonvulsive action was rather short but was prolonged by the organic acid transport inhibitor probenecid (200 mg/kg). The agents tested represent a novel class of systemically active glycineB antagonists with greatly improved bioavailability." @default.
- W2201538478 created "2016-06-24" @default.
- W2201538478 creator A5000040258 @default.
- W2201538478 creator A5003380923 @default.
- W2201538478 creator A5013335339 @default.
- W2201538478 creator A5028197839 @default.
- W2201538478 creator A5031801089 @default.
- W2201538478 creator A5043083617 @default.
- W2201538478 creator A5045544787 @default.
- W2201538478 creator A5050366902 @default.
- W2201538478 creator A5060706996 @default.
- W2201538478 creator A5087213855 @default.
- W2201538478 creator A5088509732 @default.
- W2201538478 creator A5090757134 @default.
- W2201538478 date "1997-12-01" @default.
- W2201538478 modified "2023-10-13" @default.
- W2201538478 title "Novel systemically active antagonists of the glycine site of the N-methyl-D-aspartate receptor: electrophysiological, biochemical and behavioral characterization." @default.
- W2201538478 cites W1589136255 @default.
- W2201538478 cites W1775749144 @default.
- W2201538478 cites W1799745768 @default.
- W2201538478 cites W1925182157 @default.
- W2201538478 cites W1963718884 @default.
- W2201538478 cites W1963895697 @default.
- W2201538478 cites W1975342713 @default.
- W2201538478 cites W1978079999 @default.
- W2201538478 cites W1978446097 @default.
- W2201538478 cites W1983542896 @default.
- W2201538478 cites W1985118788 @default.
- W2201538478 cites W1987017995 @default.
- W2201538478 cites W1990149170 @default.
- W2201538478 cites W1995075936 @default.
- W2201538478 cites W1996216954 @default.
- W2201538478 cites W1996555027 @default.
- W2201538478 cites W1996555735 @default.
- W2201538478 cites W1998883371 @default.
- W2201538478 cites W2003066583 @default.
- W2201538478 cites W2011035664 @default.
- W2201538478 cites W2014281089 @default.
- W2201538478 cites W2015607927 @default.
- W2201538478 cites W2016690333 @default.
- W2201538478 cites W2017974723 @default.
- W2201538478 cites W2019072693 @default.
- W2201538478 cites W2020789218 @default.
- W2201538478 cites W2023657406 @default.
- W2201538478 cites W2023669826 @default.
- W2201538478 cites W2024173492 @default.
- W2201538478 cites W2024922880 @default.
- W2201538478 cites W2027388429 @default.
- W2201538478 cites W2028331547 @default.
- W2201538478 cites W2030463961 @default.
- W2201538478 cites W2033395644 @default.
- W2201538478 cites W2035448076 @default.
- W2201538478 cites W2037380629 @default.
- W2201538478 cites W2037465347 @default.
- W2201538478 cites W2038770898 @default.
- W2201538478 cites W2039092171 @default.
- W2201538478 cites W2039872800 @default.
- W2201538478 cites W2048152070 @default.
- W2201538478 cites W2057009745 @default.
- W2201538478 cites W2062336842 @default.
- W2201538478 cites W2069888996 @default.
- W2201538478 cites W2070275362 @default.
- W2201538478 cites W2075345533 @default.
- W2201538478 cites W2077440911 @default.
- W2201538478 cites W2077942662 @default.
- W2201538478 cites W2080997656 @default.
- W2201538478 cites W2081678712 @default.
- W2201538478 cites W2095171239 @default.
- W2201538478 cites W2095233711 @default.
- W2201538478 cites W2100368827 @default.
- W2201538478 cites W2124192107 @default.
- W2201538478 cites W2124509140 @default.
- W2201538478 cites W2149211603 @default.
- W2201538478 cites W2245679498 @default.
- W2201538478 cites W2259658508 @default.
- W2201538478 cites W2259887534 @default.
- W2201538478 cites W2267979169 @default.
- W2201538478 cites W2292111191 @default.
- W2201538478 cites W2316145923 @default.
- W2201538478 cites W2345451452 @default.
- W2201538478 cites W2444475331 @default.
- W2201538478 cites W3037165371 @default.
- W2201538478 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/9400002" @default.
- W2201538478 hasPublicationYear "1997" @default.
- W2201538478 type Work @default.
- W2201538478 sameAs 2201538478 @default.
- W2201538478 citedByCount "70" @default.
- W2201538478 countsByYear W22015384782012 @default.
- W2201538478 countsByYear W22015384782013 @default.
- W2201538478 countsByYear W22015384782014 @default.
- W2201538478 countsByYear W22015384782015 @default.
- W2201538478 countsByYear W22015384782016 @default.
- W2201538478 countsByYear W22015384782017 @default.
- W2201538478 countsByYear W22015384782018 @default.
- W2201538478 countsByYear W22015384782019 @default.
- W2201538478 countsByYear W22015384782020 @default.
- W2201538478 countsByYear W22015384782021 @default.
- W2201538478 countsByYear W22015384782022 @default.