FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2037697488> ?p ?o ?g. }

• W2037697488 endingPage "1076" @default.
• W2037697488 startingPage "1071" @default.
• W2037697488 abstract "1 α1-Adrenoceptor subtypes in rabbit thoracic aorta have been examined in binding and functional experiments. 2 [3H]-prazosin bound to two distinct populations of α1-adrenoceptors (pKD,high = 9.94, Rhigh = 79.2 fmol mg−1 protein; pKD,low = 8.59, Rlow = 215 fmol mg−1 protein). Pretreatment with chloroethylclonidine (CEC, 10 μm) almost inactivated the prazosin-high affinity sites and reduced the number of the low affinity sites without changing the pKD value. 3 In the displacement experiments with CEC-untreated membranes, unlabelled prazosin, WB4101 and HV723 displaced the binding of 200 pm [3H]-prazosin monophasically; the affinities for WB4101 (pK1 = 8.88) and HV723 (8.49) were about 10 times lower than that for prazosin (9.99). In the CEC-pretreated membranes also, the antagonists inhibited the binding of 1000 pm [3H]-prazosin monophasically; the pK1 values for prazosin, WB4101 and HV723 were 9.09, 8.97 and 8.17, respectively. These results suggest that the prazosin-high and low affinity sites can be independently appraised in the former and latter experimental conditions. Noradrenaline, but not methoxamine, showed slightly higher affinity for the prazosin-high affinity site than for the low affinity site. 4 In the functional experiments, noradrenaline (0.001–100 μm) and methoxamine (0.1–100 μm) produced concentration-dependent contractions. Pretreatment with CEC inhibited the contractions induced by low concentrations of noradrenaline but without effect on the responses to methoxamine. Prazosin inhibited the concentration-response curves for noradrenaline in the CEC-untreated aorta in a manner which was not consistent with competitive antagonism at a single site, and two distinct affinity constants (pKB = 9.71 and 8.74) were obtained. However, after CEC-pretreatment, Schild plots for prazosin were not significantly different from unity (pKB = 8.50). WB4101 and HV723 competitively inhibited the noradrenaline-induced contraction with low pKB values (approximately 8.30), irrespective of CEC-pretreatment. Methoxamine-induced contractions were competitively inhibited by prazosin, WB4101 and HV723 with low pKB values similar to those obtained when noradrenaline was used as the agonist. These were not affected by CEC-pretreatment. 5 The affinity constant for noradrenaline (pKA = 6.40) in CEC-untreated aorta was slightly greater than that obtained in CEC-pretreated aorta (5.78). On the other hand, methoxamine showed a similar affinity in CEC-untreated and pretreated aortae (pKA = approximately 4.5). 6 Nifedipine (1 μm) slightly attenuated the contractile responses to noradrenaline and methoxamine in CEC-untreated and pretreated aortae, suggesting that nifedipine cannot discriminate between α1-adrenoceptors involved in CEC-sensitive and -resistant contractions. 7 From these results it is suggested that in the rabbit thoracic aorta there are two distinct α1-adrenoceptor subtypes (presumably α1B and α1L subtypes according to recently proposed subclassification), both of which are involved in noradrenaline-induced contraction. The α1L subtype predominantly mediates the contraction induced by methoxamine." @default.
• W2037697488 created "2016-06-24" @default.
• W2037697488 creator A5017801785 @default.
• W2037697488 creator A5055301993 @default.
• W2037697488 creator A5062876325 @default.
• W2037697488 date "1993-04-01" @default.
• W2037697488 modified "2023-10-03" @default.
• W2037697488 title "Pharmacological characterization of two distinct α1-adrenoceptor subtypes in rabbit thoracic aorta" @default.
• W2037697488 cites W159198934 @default.
• W2037697488 cites W1794062514 @default.
• W2037697488 cites W1823527954 @default.
• W2037697488 cites W1841809633 @default.
• W2037697488 cites W1865252654 @default.
• W2037697488 cites W1971251151 @default.
• W2037697488 cites W1996897799 @default.
• W2037697488 cites W2000360015 @default.
• W2037697488 cites W2014884270 @default.
• W2037697488 cites W2020404323 @default.
• W2037697488 cites W2024741560 @default.
• W2037697488 cites W2026619533 @default.
• W2037697488 cites W2043200348 @default.
• W2037697488 cites W2043813981 @default.
• W2037697488 cites W2048373362 @default.
• W2037697488 cites W2057971042 @default.
• W2037697488 cites W2062592957 @default.
• W2037697488 cites W2065852536 @default.
• W2037697488 cites W2074631079 @default.
• W2037697488 cites W2092028537 @default.
• W2037697488 cites W2128635872 @default.
• W2037697488 cites W2141432073 @default.
• W2037697488 cites W2294563906 @default.
• W2037697488 cites W2418498003 @default.
• W2037697488 cites W2419241215 @default.
• W2037697488 cites W4293247451 @default.
• W2037697488 doi "https://doi.org/10.1111/j.1476-5381.1993.tb13507.x" @default.
• W2037697488 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/1908151" @default.
• W2037697488 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/8097950" @default.
• W2037697488 hasPublicationYear "1993" @default.
• W2037697488 type Work @default.
• W2037697488 sameAs 2037697488 @default.
• W2037697488 citedByCount "69" @default.
• W2037697488 countsByYear W20376974882012 @default.
• W2037697488 countsByYear W20376974882014 @default.
• W2037697488 countsByYear W20376974882015 @default.
• W2037697488 countsByYear W20376974882016 @default.
• W2037697488 crossrefType "journal-article" @default.
• W2037697488 hasAuthorship W2037697488A5017801785 @default.
• W2037697488 hasAuthorship W2037697488A5055301993 @default.
• W2037697488 hasAuthorship W2037697488A5062876325 @default.
• W2037697488 hasBestOaLocation W20376974881 @default.
• W2037697488 hasConcept C126322002 @default.
• W2037697488 hasConcept C134018914 @default.
• W2037697488 hasConcept C170493617 @default.
• W2037697488 hasConcept C185592680 @default.
• W2037697488 hasConcept C2776885963 @default.
• W2037697488 hasConcept C2778938600 @default.
• W2037697488 hasConcept C2779980429 @default.
• W2037697488 hasConcept C2780648677 @default.
• W2037697488 hasConcept C2780745239 @default.
• W2037697488 hasConcept C55493867 @default.
• W2037697488 hasConcept C71924100 @default.
• W2037697488 hasConcept C86803240 @default.
• W2037697488 hasConcept C98274493 @default.
• W2037697488 hasConceptScore W2037697488C126322002 @default.
• W2037697488 hasConceptScore W2037697488C134018914 @default.
• W2037697488 hasConceptScore W2037697488C170493617 @default.
• W2037697488 hasConceptScore W2037697488C185592680 @default.
• W2037697488 hasConceptScore W2037697488C2776885963 @default.
• W2037697488 hasConceptScore W2037697488C2778938600 @default.
• W2037697488 hasConceptScore W2037697488C2779980429 @default.
• W2037697488 hasConceptScore W2037697488C2780648677 @default.
• W2037697488 hasConceptScore W2037697488C2780745239 @default.
• W2037697488 hasConceptScore W2037697488C55493867 @default.
• W2037697488 hasConceptScore W2037697488C71924100 @default.
• W2037697488 hasConceptScore W2037697488C86803240 @default.
• W2037697488 hasConceptScore W2037697488C98274493 @default.
• W2037697488 hasIssue "4" @default.
• W2037697488 hasLocation W20376974881 @default.
• W2037697488 hasLocation W20376974882 @default.
• W2037697488 hasLocation W20376974883 @default.
• W2037697488 hasLocation W20376974884 @default.
• W2037697488 hasOpenAccess W2037697488 @default.
• W2037697488 hasPrimaryLocation W20376974881 @default.
• W2037697488 hasRelatedWork W1965781866 @default.
• W2037697488 hasRelatedWork W1966357256 @default.
• W2037697488 hasRelatedWork W1992842231 @default.
• W2037697488 hasRelatedWork W2082001899 @default.
• W2037697488 hasRelatedWork W2083539015 @default.
• W2037697488 hasRelatedWork W2127219007 @default.
• W2037697488 hasRelatedWork W2163966674 @default.
• W2037697488 hasRelatedWork W2165958118 @default.
• W2037697488 hasRelatedWork W2398697207 @default.
• W2037697488 hasRelatedWork W4251709836 @default.
• W2037697488 hasVolume "108" @default.
• W2037697488 isParatext "false" @default.
• W2037697488 isRetracted "false" @default.
• W2037697488 magId "2037697488" @default.
• W2037697488 workType "article" @default.