FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W1982199478> ?p ?o ?g. }

• W1982199478 endingPage "1208" @default.
• W1982199478 startingPage "1202" @default.
• W1982199478 abstract "1 The pharmacological profile of adenosine A1 receptors in human, guinea-pig, rat and mouse brain membranes was characterized in a radioligand binding assay by use of the receptor selective antagonist, [3H]-8-cyclopentyl-1,3-dipropylxanthine ([3H]-DPCPX). 2 The affinity of [3H]-DPCPX binding sites in rat cortical and hippocampal membranes was similar. Binding site affinity was higher in rat cortical membranes than in membranes prepared from guinea-pig cortex and hippocampus, mouse cortex and human cortex. pKD values (M) were 9.55, 9.44, 8.85, 8.94, 8.67, 9.39 and 8.67, respectively. The binding site density (Bmax) was lower in rat cortical membranes than in guinea-pig or human cortical membranes. 3 The rank order of potency of seven adenosine receptor agonists was identical in each species. With the exception of 5′-N-ethylcarboxamidoadenosine (NECA), agonist affinity was 3.5–26.2 fold higher in rat cortical membranes than in human and guinea-pig brain membranes; affinity in rat and mouse brain membranes was similar. While NECA exhibited 9.3 fold higher affinity in rat compared to human cortical membranes, affinity in other species was comparable. The stable GTP analogue, Gpp(NH)p (100 μM) reduced 2-chloro-N6-cyclopentyladenosine (CCPA) affinity 7–13.9 fold, whereas the affinity of DPCPX was unaffected. 4 The affinity of six xanthine-based adenosine receptor antagonists was 2.2–15.9 fold higher in rat cortical membranes compared with human or guinea-pig membranes. The rank order of potency was species-independent. In contrast, three pyrazolopyridine derivatives, (R)-1-[(E)-3-(2-phenylpyrazolo[1,5-a]pyridin-3-yl) acryloyl]-2-piperidine ethanol (FK453), (R)-1-[(E)-3-(2-phenylpyrazolo[1,5-a]pyridin-3-yl) acryloyl]-piperidin-2-yl acetic acid (FK352) and 6-oxo-3-(2-phenylpyrazolo[1,5-a]pyridin-3-yl)-1(6H)-pyridazinebutyric acid (FK838) exhibited similar affinity in human, guinea-pig, rat and mouse brain membranes. pKi values (M) for [3H]-DPCPX binding sites in human cortical membranes were 9.31, 7.52 and 7.92, respectively. 5 Drug affinity for adenosine A2A receptors was determined in a [3H]-2-[4-(2-carboxyethyl)phenethylamino]-5′-N-ethylcarboxamidoadenosine ([3H]-CGS 21680) binding assay in rat striatal membranes. The pyrazolopyridine derivatives, FK453, FK838 and FK352 exhibited pKi values (M) of 5.90, 5.92 and 4.31, respectively, compared with pKi values of 9.31, 8.18 and 7.57 determined in the [3H]-DPCPX binding assay in rat cortical membranes. These novel pyrazolopyridine derivatives therefore represent high affinity, adenosine A1 receptor selective drugs that, in contrast to xanthine based antagonists, exhibit similar affinity for [3H]-DPCPX binding sites in human, rat, mouse and guinea-pig brain membranes. British Journal of Pharmacology (1997) 122, 1202–1208; doi:10.1038/sj.bjp.0701465" @default.
• W1982199478 created "2016-06-24" @default.
• W1982199478 creator A5004067750 @default.
• W1982199478 creator A5011188240 @default.
• W1982199478 creator A5021691019 @default.
• W1982199478 creator A5044182242 @default.
• W1982199478 creator A5055464659 @default.
• W1982199478 creator A5062356003 @default.
• W1982199478 date "1997-11-01" @default.
• W1982199478 modified "2023-10-12" @default.
• W1982199478 title "Species differences in brain adenosine A₁receptor pharmacology revealed by use of xanthine and pyrazolopyridine based antagonists" @default.
• W1982199478 cites W130778363 @default.
• W1982199478 cites W1481591305 @default.
• W1982199478 cites W1484320289 @default.
• W1982199478 cites W1511164301 @default.
• W1982199478 cites W1535611266 @default.
• W1982199478 cites W1542957393 @default.
• W1982199478 cites W1547703436 @default.
• W1982199478 cites W1674184175 @default.
• W1982199478 cites W1963827446 @default.
• W1982199478 cites W1980189014 @default.
• W1982199478 cites W1988041203 @default.
• W1982199478 cites W1989417748 @default.
• W1982199478 cites W2001110103 @default.
• W1982199478 cites W2003366915 @default.
• W1982199478 cites W2008862835 @default.
• W1982199478 cites W2009008028 @default.
• W1982199478 cites W2015172541 @default.
• W1982199478 cites W2016941264 @default.
• W1982199478 cites W2017037026 @default.
• W1982199478 cites W2031926319 @default.
• W1982199478 cites W2041366274 @default.
• W1982199478 cites W2049790354 @default.
• W1982199478 cites W2050090555 @default.
• W1982199478 cites W2080267130 @default.
• W1982199478 cites W2083957810 @default.
• W1982199478 cites W2107747076 @default.
• W1982199478 cites W2126155748 @default.
• W1982199478 cites W2159163715 @default.
• W1982199478 cites W31407392 @default.
• W1982199478 cites W4236341500 @default.
• W1982199478 cites W4293247451 @default.
• W1982199478 doi "https://doi.org/10.1038/sj.bjp.0701465" @default.
• W1982199478 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/1565029" @default.
• W1982199478 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/9401787" @default.
• W1982199478 hasPublicationYear "1997" @default.
• W1982199478 type Work @default.
• W1982199478 sameAs 1982199478 @default.
• W1982199478 citedByCount "57" @default.
• W1982199478 countsByYear W19821994782012 @default.
• W1982199478 countsByYear W19821994782013 @default.
• W1982199478 countsByYear W19821994782017 @default.
• W1982199478 countsByYear W19821994782018 @default.
• W1982199478 countsByYear W19821994782019 @default.
• W1982199478 countsByYear W19821994782020 @default.
• W1982199478 countsByYear W19821994782021 @default.
• W1982199478 countsByYear W19821994782023 @default.
• W1982199478 crossrefType "journal-article" @default.
• W1982199478 hasAuthorship W1982199478A5004067750 @default.
• W1982199478 hasAuthorship W1982199478A5011188240 @default.
• W1982199478 hasAuthorship W1982199478A5021691019 @default.
• W1982199478 hasAuthorship W1982199478A5044182242 @default.
• W1982199478 hasAuthorship W1982199478A5055464659 @default.
• W1982199478 hasAuthorship W1982199478A5062356003 @default.
• W1982199478 hasBestOaLocation W19821994782 @default.
• W1982199478 hasConcept C126322002 @default.
• W1982199478 hasConcept C134018914 @default.
• W1982199478 hasConcept C170493617 @default.
• W1982199478 hasConcept C181199279 @default.
• W1982199478 hasConcept C182683403 @default.
• W1982199478 hasConcept C185592680 @default.
• W1982199478 hasConcept C202751555 @default.
• W1982199478 hasConcept C2776991684 @default.
• W1982199478 hasConcept C2778815084 @default.
• W1982199478 hasConcept C2778938600 @default.
• W1982199478 hasConcept C2779470414 @default.
• W1982199478 hasConcept C41625074 @default.
• W1982199478 hasConcept C55493867 @default.
• W1982199478 hasConcept C57992300 @default.
• W1982199478 hasConcept C67907053 @default.
• W1982199478 hasConcept C71924100 @default.
• W1982199478 hasConcept C86803240 @default.
• W1982199478 hasConcept C98274493 @default.
• W1982199478 hasConceptScore W1982199478C126322002 @default.
• W1982199478 hasConceptScore W1982199478C134018914 @default.
• W1982199478 hasConceptScore W1982199478C170493617 @default.
• W1982199478 hasConceptScore W1982199478C181199279 @default.
• W1982199478 hasConceptScore W1982199478C182683403 @default.
• W1982199478 hasConceptScore W1982199478C185592680 @default.
• W1982199478 hasConceptScore W1982199478C202751555 @default.
• W1982199478 hasConceptScore W1982199478C2776991684 @default.
• W1982199478 hasConceptScore W1982199478C2778815084 @default.
• W1982199478 hasConceptScore W1982199478C2778938600 @default.
• W1982199478 hasConceptScore W1982199478C2779470414 @default.
• W1982199478 hasConceptScore W1982199478C41625074 @default.
• W1982199478 hasConceptScore W1982199478C55493867 @default.
• W1982199478 hasConceptScore W1982199478C57992300 @default.
• W1982199478 hasConceptScore W1982199478C67907053 @default.

• next