Matches in SemOpenAlex for { <https://semopenalex.org/work/W2909968317> ?p ?o ?g. }
- W2909968317 endingPage "717" @default.
- W2909968317 startingPage "708" @default.
- W2909968317 abstract "The α1 -adrenoceptor (α1 -AR) antagonists are potential candidates for the treatment of blood pressure. Higenamine (HG) is a novel α1 -AR antagonist. In this study, we investigated the effects of HG in HEK293A cells transfected with α1A -, α1B -, and α1D -AR in vitro, rat mesenteric artery ex vivo, Wistar-Kyoto rats and spontaneously hypertensive rats in vivo. The radioligand binding assay showed that HG competitively inhibited the binding of [3 H]-prazosin to α1 -AR in a concentration-dependent manner. The affinities (pKi) of HG for the cloned α1A -, α1B -, and α1D -AR were 6.57, 6.48, and 6.35, respectively, indicating that HG displayed no selectivity for the three α1 -AR subtypes. In in vitro studies, HG was able to blunt inositol monophosphate production. It also displayed an inhibitory effect on the influx and entry of calcium ions and phosphorylation of extracellular signal-regulated kinase 1 and 2 induced by phenylephrine (PE). In ex vivo studies, PE caused a dose-dependent inotropic response curve, and the pA2 value for HG was 6.86 ± 0.29. In addition, the in vivo results showed that HG could decrease the blood pressure in normotension, spontaneous hypertension, and PE-induced hypertension models. These results indicate that HG can directly bind to α1 -AR and it appears to be a novel antagonist for α1 -AR, which may contribute to its hypotensive effect." @default.
- W2909968317 created "2019-01-25" @default.
- W2909968317 creator A5008097382 @default.
- W2909968317 creator A5019257182 @default.
- W2909968317 creator A5055517335 @default.
- W2909968317 creator A5055769104 @default.
- W2909968317 creator A5061406271 @default.
- W2909968317 creator A5069286054 @default.
- W2909968317 creator A5072454821 @default.
- W2909968317 creator A5075714559 @default.
- W2909968317 creator A5076062530 @default.
- W2909968317 date "2019-01-15" @default.
- W2909968317 modified "2023-10-18" @default.
- W2909968317 title "Identification of higenamine as a novel α<sub>1</sub>-adrenergic receptor antagonist" @default.
- W2909968317 cites W1520433389 @default.
- W2909968317 cites W1531133799 @default.
- W2909968317 cites W1978344211 @default.
- W2909968317 cites W1984857320 @default.
- W2909968317 cites W2006793476 @default.
- W2909968317 cites W2011893778 @default.
- W2909968317 cites W2021476621 @default.
- W2909968317 cites W2049407111 @default.
- W2909968317 cites W2050002341 @default.
- W2909968317 cites W2069380892 @default.
- W2909968317 cites W2072486491 @default.
- W2909968317 cites W2075569362 @default.
- W2909968317 cites W2081733999 @default.
- W2909968317 cites W2089519104 @default.
- W2909968317 cites W2089571568 @default.
- W2909968317 cites W2105549969 @default.
- W2909968317 cites W2121819992 @default.
- W2909968317 cites W2281522791 @default.
- W2909968317 cites W2616768283 @default.
- W2909968317 cites W2786245560 @default.
- W2909968317 cites W2800175679 @default.
- W2909968317 cites W2804346358 @default.
- W2909968317 cites W2810932569 @default.
- W2909968317 cites W4233171306 @default.
- W2909968317 cites W4296224641 @default.
- W2909968317 cites W1493144990 @default.
- W2909968317 doi "https://doi.org/10.1002/ptr.6261" @default.
- W2909968317 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/30648306" @default.
- W2909968317 hasPublicationYear "2019" @default.
- W2909968317 type Work @default.
- W2909968317 sameAs 2909968317 @default.
- W2909968317 citedByCount "11" @default.
- W2909968317 countsByYear W29099683172019 @default.
- W2909968317 countsByYear W29099683172020 @default.
- W2909968317 countsByYear W29099683172021 @default.
- W2909968317 countsByYear W29099683172022 @default.
- W2909968317 countsByYear W29099683172023 @default.
- W2909968317 crossrefType "journal-article" @default.
- W2909968317 hasAuthorship W2909968317A5008097382 @default.
- W2909968317 hasAuthorship W2909968317A5019257182 @default.
- W2909968317 hasAuthorship W2909968317A5055517335 @default.
- W2909968317 hasAuthorship W2909968317A5055769104 @default.
- W2909968317 hasAuthorship W2909968317A5061406271 @default.
- W2909968317 hasAuthorship W2909968317A5069286054 @default.
- W2909968317 hasAuthorship W2909968317A5072454821 @default.
- W2909968317 hasAuthorship W2909968317A5075714559 @default.
- W2909968317 hasAuthorship W2909968317A5076062530 @default.
- W2909968317 hasConcept C126322002 @default.
- W2909968317 hasConcept C134018914 @default.
- W2909968317 hasConcept C150903083 @default.
- W2909968317 hasConcept C170493617 @default.
- W2909968317 hasConcept C185592680 @default.
- W2909968317 hasConcept C202751555 @default.
- W2909968317 hasConcept C207001950 @default.
- W2909968317 hasConcept C26291073 @default.
- W2909968317 hasConcept C2776885963 @default.
- W2909968317 hasConcept C2777952589 @default.
- W2909968317 hasConcept C2780648677 @default.
- W2909968317 hasConcept C55493867 @default.
- W2909968317 hasConcept C71924100 @default.
- W2909968317 hasConcept C84393581 @default.
- W2909968317 hasConcept C86803240 @default.
- W2909968317 hasConcept C98274493 @default.
- W2909968317 hasConceptScore W2909968317C126322002 @default.
- W2909968317 hasConceptScore W2909968317C134018914 @default.
- W2909968317 hasConceptScore W2909968317C150903083 @default.
- W2909968317 hasConceptScore W2909968317C170493617 @default.
- W2909968317 hasConceptScore W2909968317C185592680 @default.
- W2909968317 hasConceptScore W2909968317C202751555 @default.
- W2909968317 hasConceptScore W2909968317C207001950 @default.
- W2909968317 hasConceptScore W2909968317C26291073 @default.
- W2909968317 hasConceptScore W2909968317C2776885963 @default.
- W2909968317 hasConceptScore W2909968317C2777952589 @default.
- W2909968317 hasConceptScore W2909968317C2780648677 @default.
- W2909968317 hasConceptScore W2909968317C55493867 @default.
- W2909968317 hasConceptScore W2909968317C71924100 @default.
- W2909968317 hasConceptScore W2909968317C84393581 @default.
- W2909968317 hasConceptScore W2909968317C86803240 @default.
- W2909968317 hasConceptScore W2909968317C98274493 @default.
- W2909968317 hasFunder F4320321001 @default.
- W2909968317 hasFunder F4320322919 @default.
- W2909968317 hasIssue "3" @default.
- W2909968317 hasLocation W29099683171 @default.
- W2909968317 hasLocation W29099683172 @default.