FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2010028189> ?p ?o ?g. }

• W2010028189 endingPage "505" @default.
• W2010028189 startingPage "497" @default.
• W2010028189 abstract "Carvedilol, a non-selective β-adrenergic blocker, is widely used for the treatment of angina pectoris and hypertension. We examined the action of carvedilol on cloned Kv1.5 expressed in CHO cells, using the whole-cell patch clamp technique. Carvedilol reduced the peak amplitude of Kv1.5 and accelerated the inactivation rate in a concentration-dependent manner with an IC50 of 2.56 μM. Using a first-order kinetics analysis, we calculated k+1 = 19.68 μM−1 s−1 for the association rate constant, and k−1 = 44.89 s−1 for the dissociation rate constant. The apparent KD (k−1/k+1) was 2.28 μM, which is similar to the IC50 value. Other β-adrenergic blockers (alprenolol, oxprenolol and carteolol) had little or no effect on Kv1.5 currents. Carvedilol slowed the deactivation time course, resulting in a tail crossover phenomenon. Carvedilol-induced block was voltage-dependent in the voltage range for channel activation, but voltage-independent in the voltage range for full activation. The voltage dependences for both steady-state activation and inactivation were unchanged by carvedilol. Carvedilol affected Kv1.5 in a use-dependent manner. When stimulation frequencies were increased to quantify a use-dependent block, however, the block by carvedilol was slightly increased with IC50 values of 2.56 μM at 0.1 Hz, 2.38 μM at 1 Hz and 2.03 μM at 2 Hz. Carvedilol also slowed the time course of recovery from inactivation of Kv1.5. These results indicate that carvedilol blocks Kv1.5 in a reversible, concentration-, voltage-, time-, and use-dependent manner, but only at concentrations slightly higher than therapeutic plasma concentrations in humans. These effects are probably relevant to an understanding of the ionic mechanism underlying the antiarrhythmic property of carvedilol." @default.
• W2010028189 created "2016-06-24" @default.
• W2010028189 creator A5001210229 @default.
• W2010028189 creator A5025992586 @default.
• W2010028189 creator A5048979470 @default.
• W2010028189 creator A5071993326 @default.
• W2010028189 date "2012-02-01" @default.
• W2010028189 modified "2023-09-27" @default.
• W2010028189 title "Carvedilol blocks the cloned cardiac Kv1.5 channels in a β-adrenergic receptor-independent manner" @default.
• W2010028189 cites W1966611070 @default.
• W2010028189 cites W1967405524 @default.
• W2010028189 cites W1976253019 @default.
• W2010028189 cites W1982141048 @default.
• W2010028189 cites W1984114553 @default.
• W2010028189 cites W1985078738 @default.
• W2010028189 cites W1986806880 @default.
• W2010028189 cites W1989035280 @default.
• W2010028189 cites W1991514105 @default.
• W2010028189 cites W1996235743 @default.
• W2010028189 cites W1998447177 @default.
• W2010028189 cites W2002234003 @default.
• W2010028189 cites W2003940239 @default.
• W2010028189 cites W2008146005 @default.
• W2010028189 cites W2011813836 @default.
• W2010028189 cites W2017212495 @default.
• W2010028189 cites W2019045599 @default.
• W2010028189 cites W2031765503 @default.
• W2010028189 cites W2036098300 @default.
• W2010028189 cites W2049474173 @default.
• W2010028189 cites W2060366195 @default.
• W2010028189 cites W2069642958 @default.
• W2010028189 cites W2076245717 @default.
• W2010028189 cites W2077548169 @default.
• W2010028189 cites W2078761712 @default.
• W2010028189 cites W2084216237 @default.
• W2010028189 cites W2086791273 @default.
• W2010028189 cites W2088180630 @default.
• W2010028189 cites W2089123543 @default.
• W2010028189 cites W2090077875 @default.
• W2010028189 cites W2096056146 @default.
• W2010028189 cites W2112025256 @default.
• W2010028189 cites W2114594302 @default.
• W2010028189 cites W2114940281 @default.
• W2010028189 cites W2116401040 @default.
• W2010028189 cites W2117287580 @default.
• W2010028189 cites W2137150883 @default.
• W2010028189 cites W2141052628 @default.
• W2010028189 cites W2150500510 @default.
• W2010028189 cites W2151638020 @default.
• W2010028189 cites W2156378269 @default.
• W2010028189 cites W2172025889 @default.
• W2010028189 cites W2887782728 @default.
• W2010028189 cites W4255054329 @default.
• W2010028189 doi "https://doi.org/10.1016/j.bcp.2011.11.019" @default.
• W2010028189 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/22146582" @default.
• W2010028189 hasPublicationYear "2012" @default.
• W2010028189 type Work @default.
• W2010028189 sameAs 2010028189 @default.
• W2010028189 citedByCount "11" @default.
• W2010028189 countsByYear W20100281892012 @default.
• W2010028189 countsByYear W20100281892014 @default.
• W2010028189 countsByYear W20100281892015 @default.
• W2010028189 countsByYear W20100281892016 @default.
• W2010028189 countsByYear W20100281892018 @default.
• W2010028189 countsByYear W20100281892019 @default.
• W2010028189 countsByYear W20100281892022 @default.
• W2010028189 countsByYear W20100281892023 @default.
• W2010028189 crossrefType "journal-article" @default.
• W2010028189 hasAuthorship W2010028189A5001210229 @default.
• W2010028189 hasAuthorship W2010028189A5025992586 @default.
• W2010028189 hasAuthorship W2010028189A5048979470 @default.
• W2010028189 hasAuthorship W2010028189A5071993326 @default.
• W2010028189 hasConcept C12554922 @default.
• W2010028189 hasConcept C126322002 @default.
• W2010028189 hasConcept C134018914 @default.
• W2010028189 hasConcept C185592680 @default.
• W2010028189 hasConcept C2778198053 @default.
• W2010028189 hasConcept C2780591200 @default.
• W2010028189 hasConcept C71924100 @default.
• W2010028189 hasConcept C86803240 @default.
• W2010028189 hasConcept C98274493 @default.
• W2010028189 hasConceptScore W2010028189C12554922 @default.
• W2010028189 hasConceptScore W2010028189C126322002 @default.
• W2010028189 hasConceptScore W2010028189C134018914 @default.
• W2010028189 hasConceptScore W2010028189C185592680 @default.
• W2010028189 hasConceptScore W2010028189C2778198053 @default.
• W2010028189 hasConceptScore W2010028189C2780591200 @default.
• W2010028189 hasConceptScore W2010028189C71924100 @default.
• W2010028189 hasConceptScore W2010028189C86803240 @default.
• W2010028189 hasConceptScore W2010028189C98274493 @default.
• W2010028189 hasIssue "4" @default.
• W2010028189 hasLocation W20100281891 @default.
• W2010028189 hasLocation W20100281892 @default.
• W2010028189 hasOpenAccess W2010028189 @default.
• W2010028189 hasPrimaryLocation W20100281891 @default.
• W2010028189 hasRelatedWork W1966504330 @default.
• W2010028189 hasRelatedWork W1966775726 @default.
• W2010028189 hasRelatedWork W1979139803 @default.

• next