FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W44171809> ?p ?o ?g. }

• W44171809 endingPage "24" @default.
• W44171809 startingPage "15" @default.
• W44171809 abstract "The present studies were undertaken to examine the in vitro calcium antagonistic properties of lercanidipine (CAS 132866-11-6, Rec 15/2375) in vascular and non-vascular tissues, as well as its binding profile and in particular its affinity to the calcium channel binding sites. Lercanidipine proved to be endowed with high affinity for the dihydropyridine subunit of the L-type calcium channel, where it was much more potent than on the other receptors tested. The nature of the interaction of lercanidipine with the calcium channel appears competitive, as evidenced by a progressive increase in the apparent Kd of the ligand with no change in Bmax. The performed functional in vitro studies in isolated vascular and cardiac tissues demonstrated that lercanidipine has a slower onset and offset of calcium antagonistic activity compared with other calcium antagonists. The time-course of inhibition of vascular smooth muscle contraction showed substantial differences after addition of lercanidipine with regard to the other calcium antagonists tested (nitrendipine and amlodipine). On repeated washing of rat aorta to remove the drugs from the preparation, the effects of nitrendipine disappeared rapidly. After amlodipine incubation, contractility of the tissue was still impaired after 6 h washout with the highest concentrations tested, but completely recovered in 1-3 h after washout of the lowest concentration. On the contrary, the preparations incubated with lercanidipine showed a decrease in contractility that reached the maximum 1 to 3 h after the removal of the compound from the bath at all the active concentrations tested. The functional calcium antagonistic activity of lercanidipine was also evaluated as relaxing potency against the tonic contractions induced by preincubation of rat aorta, bladder and colon with 80 mmol/l K+. In rat aorta, lercanidipine proved more potent than nitrendipine. Comparing the IC50 values evaluated after 3 h of contact time, lercanidipine resulted more active on the vascular tissue with potency ratios of 177 and 8.5 for aorta vs bladder and aorta vs colon, respectively. In contrast, nitrendipine showed about the same activity in the three tested tissues, and potency ratios of 2.0 and 0.8 for aorta vs bladder and aorta vs colon were calculated. In rat aortic strips maintained during the incubation with lercanidipine at different degrees of depolarization, the functional calcium antagonistic activity markedly increased by raising the tissue depolarization and the potency ratio between the IC50 values evaluated at 5 and 100 mmol/l K+ resulted 138. Nitrendipine provided very similar results, whereas nifedipine activity did not seem to be affected by raising the tissue depolarization. The negative inotropic effects of lercanidipine on normally and partially depolarized rabbit ventricular strips, as well as in guinea-pig atria, were negligible in comparison to its effects on vasculature. On the whole these characteristics suggest a slow onset of action and long duration of effects also after in vivo administration. In addition, the unique vascular selectivity of lercanidipine implies that the therapeutically desirable vasodilator activity is not or scarcely associated with a decrease in cardiac contractile force." @default.
• W44171809 created "2016-06-24" @default.
• W44171809 creator A5001488752 @default.
• W44171809 creator A5005729738 @default.
• W44171809 creator A5022249344 @default.
• W44171809 creator A5033342794 @default.
• W44171809 creator A5037492112 @default.
• W44171809 creator A5052071936 @default.
• W44171809 creator A5054132162 @default.
• W44171809 date "1996-01-01" @default.
• W44171809 modified "2023-10-06" @default.
• W44171809 title "Pharmacological in vitro studies of the new 1,4-dihydropyridine calcium antagonist lercanidipine." @default.
• W44171809 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/8821512" @default.
• W44171809 hasPublicationYear "1996" @default.
• W44171809 type Work @default.
• W44171809 sameAs 44171809 @default.
• W44171809 citedByCount "12" @default.
• W44171809 countsByYear W441718092014 @default.
• W44171809 countsByYear W441718092017 @default.
• W44171809 countsByYear W441718092018 @default.
• W44171809 crossrefType "journal-article" @default.
• W44171809 hasAuthorship W44171809A5001488752 @default.
• W44171809 hasAuthorship W44171809A5005729738 @default.
• W44171809 hasAuthorship W44171809A5022249344 @default.
• W44171809 hasAuthorship W44171809A5033342794 @default.
• W44171809 hasAuthorship W44171809A5037492112 @default.
• W44171809 hasAuthorship W44171809A5052071936 @default.
• W44171809 hasAuthorship W44171809A5054132162 @default.
• W44171809 hasConcept C126322002 @default.
• W44171809 hasConcept C170493617 @default.
• W44171809 hasConcept C178790620 @default.
• W44171809 hasConcept C185592680 @default.
• W44171809 hasConcept C18699975 @default.
• W44171809 hasConcept C2776885963 @default.
• W44171809 hasConcept C2779283177 @default.
• W44171809 hasConcept C2779395532 @default.
• W44171809 hasConcept C2779572014 @default.
• W44171809 hasConcept C2779646130 @default.
• W44171809 hasConcept C2780548744 @default.
• W44171809 hasConcept C2781212610 @default.
• W44171809 hasConcept C2992686903 @default.
• W44171809 hasConcept C39133596 @default.
• W44171809 hasConcept C519063684 @default.
• W44171809 hasConcept C55493867 @default.
• W44171809 hasConcept C71924100 @default.
• W44171809 hasConcept C84393581 @default.
• W44171809 hasConcept C85520022 @default.
• W44171809 hasConcept C86803240 @default.
• W44171809 hasConcept C98274493 @default.
• W44171809 hasConceptScore W44171809C126322002 @default.
• W44171809 hasConceptScore W44171809C170493617 @default.
• W44171809 hasConceptScore W44171809C178790620 @default.
• W44171809 hasConceptScore W44171809C185592680 @default.
• W44171809 hasConceptScore W44171809C18699975 @default.
• W44171809 hasConceptScore W44171809C2776885963 @default.
• W44171809 hasConceptScore W44171809C2779283177 @default.
• W44171809 hasConceptScore W44171809C2779395532 @default.
• W44171809 hasConceptScore W44171809C2779572014 @default.
• W44171809 hasConceptScore W44171809C2779646130 @default.
• W44171809 hasConceptScore W44171809C2780548744 @default.
• W44171809 hasConceptScore W44171809C2781212610 @default.
• W44171809 hasConceptScore W44171809C2992686903 @default.
• W44171809 hasConceptScore W44171809C39133596 @default.
• W44171809 hasConceptScore W44171809C519063684 @default.
• W44171809 hasConceptScore W44171809C55493867 @default.
• W44171809 hasConceptScore W44171809C71924100 @default.
• W44171809 hasConceptScore W44171809C84393581 @default.
• W44171809 hasConceptScore W44171809C85520022 @default.
• W44171809 hasConceptScore W44171809C86803240 @default.
• W44171809 hasConceptScore W44171809C98274493 @default.
• W44171809 hasIssue "1" @default.
• W44171809 hasLocation W441718091 @default.
• W44171809 hasOpenAccess W44171809 @default.
• W44171809 hasPrimaryLocation W441718091 @default.
• W44171809 hasRelatedWork W1983370340 @default.
• W44171809 hasRelatedWork W2012187456 @default.
• W44171809 hasRelatedWork W2015116661 @default.
• W44171809 hasRelatedWork W2019501849 @default.
• W44171809 hasRelatedWork W2103616575 @default.
• W44171809 hasRelatedWork W2170203080 @default.
• W44171809 hasRelatedWork W2991195926 @default.
• W44171809 hasRelatedWork W44171809 @default.
• W44171809 hasRelatedWork W4911587 @default.
• W44171809 hasRelatedWork W1926820969 @default.
• W44171809 hasVolume "46" @default.
• W44171809 isParatext "false" @default.
• W44171809 isRetracted "false" @default.
• W44171809 magId "44171809" @default.
• W44171809 workType "article" @default.