Matches in SemOpenAlex for { <https://semopenalex.org/work/W2588041553> ?p ?o ?g. }
Showing items 1 to 90 of
90
with 100 items per page.
- W2588041553 abstract "Analytical pharmacology draws heavily on the concept of equilibrium of agonist and silent antagonist concentrations competing at a specific receptor site. This condition breaks down in nerve transmission when transmitter release is inhibited by prejunctional α2-adrenoceptors activated by an agonist such as clonidine. We have developed a method that allows the agonist dissociation constant KA of clonidine to be determined in a robust isolated right atrial assay of mouse, rat and guinea pig. By applying low numbers of field pulses 1-4 to prevent autoinhibitory feedback, clonidine shifted the nerve pulse stimulation-tachycardia curves to the right. These peak responses to field pulses were equated to responses to exogenous noradrenaline and the pKA determined by global fitting and display in the Clark plot. The pKA for clonidine ranged from 8.95 in the mouse, 7.8 in rat and 8.3 in guinea pig. The propranolol pKB was 8.87 in mouse and 8.91 in rat atria, reading very similarly to those values from β-adrenoceptor agonist assays under equilibrium conditions. In mesenteric resistance arteries mounted in a myograph for electrical field stimulation, clonidine again inhibited contractions to field pulses in mouse arteries with a pKA of 7.12, but was inactive in rat arteries due to competing autoinhibitory feedback from nerve-released noradrenaline. In both species, prazosin inhibited the field pulses with a pKB of 9.08 in rat and 9.03 in mouse arteries. We conclude that pKB for antagonists and pKA for the prejunctional inhibitors of nerve transmission can be determined with this novel analytical approach." @default.
- W2588041553 created "2017-02-24" @default.
- W2588041553 creator A5030737904 @default.
- W2588041553 creator A5032362251 @default.
- W2588041553 creator A5081258628 @default.
- W2588041553 date "2017-04-01" @default.
- W2588041553 modified "2023-09-26" @default.
- W2588041553 title "Novel technique to determine the p K A of clonidine at prejunctional α 2 -adrenoceptors in cardiac and vascular sympathetic transmission" @default.
- W2588041553 cites W1968721836 @default.
- W2588041553 cites W1970445852 @default.
- W2588041553 cites W1972081418 @default.
- W2588041553 cites W1981400419 @default.
- W2588041553 cites W1985001867 @default.
- W2588041553 cites W1993268995 @default.
- W2588041553 cites W1998796863 @default.
- W2588041553 cites W1998869692 @default.
- W2588041553 cites W2008632370 @default.
- W2588041553 cites W2015945758 @default.
- W2588041553 cites W2022090382 @default.
- W2588041553 cites W2037142508 @default.
- W2588041553 cites W2038853700 @default.
- W2588041553 cites W2046432572 @default.
- W2588041553 cites W2049750900 @default.
- W2588041553 cites W2050011554 @default.
- W2588041553 cites W2055189150 @default.
- W2588041553 cites W2077619217 @default.
- W2588041553 cites W2094630235 @default.
- W2588041553 cites W2097094466 @default.
- W2588041553 cites W2123841491 @default.
- W2588041553 cites W2288409654 @default.
- W2588041553 cites W2291202360 @default.
- W2588041553 cites W2331431588 @default.
- W2588041553 cites W2412970545 @default.
- W2588041553 cites W2508191581 @default.
- W2588041553 cites W2901149630 @default.
- W2588041553 cites W1968001106 @default.
- W2588041553 doi "https://doi.org/10.1016/j.ejphar.2017.02.030" @default.
- W2588041553 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/28219708" @default.
- W2588041553 hasPublicationYear "2017" @default.
- W2588041553 type Work @default.
- W2588041553 sameAs 2588041553 @default.
- W2588041553 citedByCount "0" @default.
- W2588041553 crossrefType "journal-article" @default.
- W2588041553 hasAuthorship W2588041553A5030737904 @default.
- W2588041553 hasAuthorship W2588041553A5032362251 @default.
- W2588041553 hasAuthorship W2588041553A5081258628 @default.
- W2588041553 hasConcept C126322002 @default.
- W2588041553 hasConcept C134018914 @default.
- W2588041553 hasConcept C163415756 @default.
- W2588041553 hasConcept C170493617 @default.
- W2588041553 hasConcept C185592680 @default.
- W2588041553 hasConcept C24998067 @default.
- W2588041553 hasConcept C2776885963 @default.
- W2588041553 hasConcept C2778399450 @default.
- W2588041553 hasConcept C2778938600 @default.
- W2588041553 hasConcept C2779941686 @default.
- W2588041553 hasConcept C2780648677 @default.
- W2588041553 hasConcept C71924100 @default.
- W2588041553 hasConcept C86803240 @default.
- W2588041553 hasConceptScore W2588041553C126322002 @default.
- W2588041553 hasConceptScore W2588041553C134018914 @default.
- W2588041553 hasConceptScore W2588041553C163415756 @default.
- W2588041553 hasConceptScore W2588041553C170493617 @default.
- W2588041553 hasConceptScore W2588041553C185592680 @default.
- W2588041553 hasConceptScore W2588041553C24998067 @default.
- W2588041553 hasConceptScore W2588041553C2776885963 @default.
- W2588041553 hasConceptScore W2588041553C2778399450 @default.
- W2588041553 hasConceptScore W2588041553C2778938600 @default.
- W2588041553 hasConceptScore W2588041553C2779941686 @default.
- W2588041553 hasConceptScore W2588041553C2780648677 @default.
- W2588041553 hasConceptScore W2588041553C71924100 @default.
- W2588041553 hasConceptScore W2588041553C86803240 @default.
- W2588041553 hasLocation W25880415531 @default.
- W2588041553 hasLocation W25880415532 @default.
- W2588041553 hasOpenAccess W2588041553 @default.
- W2588041553 hasPrimaryLocation W25880415531 @default.
- W2588041553 hasRelatedWork W1963904083 @default.
- W2588041553 hasRelatedWork W1974745672 @default.
- W2588041553 hasRelatedWork W2001388166 @default.
- W2588041553 hasRelatedWork W2010332437 @default.
- W2588041553 hasRelatedWork W2013457480 @default.
- W2588041553 hasRelatedWork W2016626080 @default.
- W2588041553 hasRelatedWork W2017589268 @default.
- W2588041553 hasRelatedWork W2055714395 @default.
- W2588041553 hasRelatedWork W2064416809 @default.
- W2588041553 hasRelatedWork W2588041553 @default.
- W2588041553 isParatext "false" @default.
- W2588041553 isRetracted "false" @default.
- W2588041553 magId "2588041553" @default.
- W2588041553 workType "article" @default.