Inhibition of rabbit platelet phosphodiesterase activity and aggregation by calcium channel blockers

Moore, John B.; Fuller, Barbara L.; Falotico, Robert; Tolman, E.L.

doi:10.1016/0049-3848(85)90275-0

Cited by 34 publications

(12 citation statements)

References 14 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…This has been reported on phosphodiesterase prepared from bovine heart [32,33] as well as on rabbit platelets [34], These latter authors found for N if and approximate IC50 value of 800 pmol/l for in vitro rabbit ADP-induced platelet aggrega tion. This could certainly be explained by methodological differences.…”

Section: Discussionmentioning

confidence: 69%

“…Therefore, beside their specific effects, these agents might have multiple nonspecific effects such as those re ported herein. Other properties have also been described such as potentiation of the antiaggregatory activity of PGD2 [34] or com petitive antagonism of platelet-aggregating 257 factor [40] and of thromboxane At receptors [41]. These multiple effects might explain the reported effect of DHP to have beneficial effects in the treatment of a number of cardio vascular and circulatory disorders and in ex perimental atherosclerosis [42].…”

Section: Discussionmentioning

confidence: 95%

See 1 more Smart Citation

Comparative Inhibitory Effects of Dihydropyridines on Platelet Aggregation, Calcium Uptake and Cyclic AMP Concentration

Blache

Ojeda

1992

Pharmacology

View full text Add to dashboard Cite

We studied the in vitro effects of several calcium channel blockers from the dihydropyridine (DHP) family on platelet aggregation and endogenous serotonin secretion, calcium uptake and cyclic AMP (cAMP) concentration using washed rat platelets. We found that, after 1 min incubation, nifedipine (Nil), nitrendipine (Nit) and nisoldipine (Nis) inhibited the thrombin-induced platelet aggregation and serotonin secretion with IC50 of about 140, 5 and 2 μmol/l, respectively. Nis and Nit are thus much more active than Nif. We also found that the thrombin-induced Ca²⁺ uptake amounted to 2,600 ± 326 pmol Ca²⁺/10⁹ platelets in control conditions. In the presence of 10 μmol/l of the DHP, this uptake was decreased by 19, 49 or 77 %, with Nif, Nit or Nis, respectively. Compound BAY K 8644 (BK) with known agonistic properties on the calcium channel had inhibitory effects on the studied parameters. These compounds were in the order of Nif < BK < Nit < Nis. When added to previously aggregated platelets, Nit caused them to deaggregate. These results seem to be similar to those obtained with cAMP analogues or adenylate cyclase activators. The platelet resting cAMP concentration was therefore measured in the presence of the DHP. A nonsignificant increase was found with 20 μmol/l Nif whereas significant increases of 20 and 68 % as compared with controls were obtained with 20 μmol/l Nit and Nis, respectively. Partition studies between platelets and plasma lipoproteins indicated that the effects might be related to the lipophilicity of the compounds. These data suggest that these agents work on platelet activity by multiple effects located intracellularly or at the membrane level. We propose that these effects could work in combination to explain the in vivo potency of these agents in the treatment of cardiovascular disorders.

show abstract

Section: Discussionmentioning

confidence: 69%

Section: Discussionmentioning

confidence: 95%

Comparative Inhibitory Effects of Dihydropyridines on Platelet Aggregation, Calcium Uptake and Cyclic AMP Concentration

Blache

Ojeda

1992

Pharmacology

View full text Add to dashboard Cite

show abstract

“…Sustained Ca 2+ increase generates reactive oxygen species (ROS) and the formation of ROS causes the disruption of Ca 2+ homeostasis and cell death (Manzl et al, 2004). Nifedipine, by its actions on monoamine transporters (Padmanabhan et al, 2008) and phosphodiesterase (Moore et al, 1985) enhances cAMP-CREB-BDNF signaling (Sasaki et al, 2007), an important factor in neuroplasticity.…”

Section: Introductionmentioning

confidence: 99%

Effect of nifedipine, imipramine and sertraline on the antidepressant-like actions of furosemide in forced swim (FST) and tail suspension (TST) tests models of depression in mice

S.¹,

E.²

2012

Afr. J. Biotechnol.

View full text Add to dashboard Cite

“…Determination of cGMP-specffic phosphodiesterase activity The supernatant fraction of AIO VSMC lysate was used for cGMP-specific phosphodiesterase determination [25,26]. The crude cytosolic enzyme (8.4 mg/ml) was incubated with cGMP (1O ,tM, containing 0.1 ,uCi of [3H]cGMP) and compound in a final volume of 0.4 ml (buffer was 50 mM Tris/HCl, 5 mM MgCl2, pH 7.4).…”

Section: Introductionmentioning

confidence: 99%

Mechanism of anti-proliferation caused by YC-1, an indazole derivative, in cultured rat A10 vascular smooth-muscle cells

YU¹,

CHENG²,

GUH³

et al. 1997

Biochemical Journal

View full text Add to dashboard Cite

An indazole derivative, YC-1, was identified in this study to be capable of reversibly and effectively inhibiting proliferation of rat AIO vascular smooth-muscle cells (VSMCs) in vitro. YC-1 (1-100 1uM) dose-dependently inhibited [3H]thymidine incorporation into DNA in rat AlO VSMCs that were synchronized by serum depletion and then restimulated by addition of 10 % foetal calf serum (FCS), whereas FCS-induced [3H]thymidine incorporation into rat synchronized endothelial cells was unaffected by this agent. The dose of YC-1 required to cause inhibition of FCS-induced proliferation was similar to that necessary for the formation of cellular cyclic GMP (cGMP). Guanylate cyclase activity in soluble fractions of VSMCs was activated by (1-100 ,uM), whereas cGMP-specific phosphodiesterase activity was unaffected by this compound. The anti-proliferative effect of YC-1 was mimicked by 8-bromo-cGMP, a membrane-permeable cGMP analogue, and was antagonized by KT 5823 (0.2,M), a selective inhibitor of protein kinase G. The anti-proliferative

show abstract

Inhibition of rabbit platelet phosphodiesterase activity and aggregation by calcium channel blockers

Cited by 34 publications

References 14 publications

Comparative Inhibitory Effects of Dihydropyridines on Platelet Aggregation, Calcium Uptake and Cyclic AMP Concentration

Comparative Inhibitory Effects of Dihydropyridines on Platelet Aggregation, Calcium Uptake and Cyclic AMP Concentration

Effect of nifedipine, imipramine and sertraline on the antidepressant-like actions of furosemide in forced swim (FST) and tail suspension (TST) tests models of depression in mice

Mechanism of anti-proliferation caused by YC-1, an indazole derivative, in cultured rat A10 vascular smooth-muscle cells

Contact Info

Product

Resources

About