The Antithrombogenic In Vivo Effects of Calcium Channel Blockers in Experimental Thrombosis in Mice

1987 ◽  
Vol 57 (03) ◽  
pp. 283-285 ◽  
Author(s):  
M P Ortega ◽  
C Sunkel ◽  
J G Priego ◽  
P R Statkow
Keyword(s):  
Protective Effect ◽  
Calcium Channel ◽  
Calcium Channel Blockers ◽  
The Other ◽  
Channel Blockers ◽  
Male Mice ◽  
New Model ◽  
Experimental Thrombosis ◽  
In Vivo Effects

SummaryA new model of thrombotic challenge, well suited for screening agents and which acts primarily against platelet thromboembolism, has been used to test the in vivo anti-platelet effects of four calcium channel blockers (CCB). An i. v. injection of a mixture of collagen plus epinephrine (15 μg and 1.8 μg/mouse, respectively) was given to male mice. 94% control mice died or remained paralyzed for more than 15 minutes. The dihydropyridine agents, CRE-223 and Nifedipine, were highly protective against experimental thrombosis, whereas Verapamil had a weaker and much shorter effect and, on the other hand, Diltiazem had no protective effect over a range of doses. The activity on both dihydropyridines lasted for seven hours or even longer.

Praziquantel and the benzodiazepine Ro 11-3128 do not compete for the same binding sites in schistosomes

Parasitology ◽  
2007 ◽  
Vol 135 (1) ◽  
pp. 47-54 ◽  
Author(s):  
L. PICA-MATTOCCIA ◽  
A. RUPPEL ◽  
C. M. XIA ◽  
D. CIOLI
Keyword(s):  
Calcium Channel ◽  
Binding Sites ◽  
Calcium Influx ◽  
Cytochalasin D ◽  
The Other ◽  
Channel Blockers ◽  
Spastic Paralysis ◽  
Receptor Sites

SUMMARYThe benzodiazepine Ro 11-3128 (methyl-clonazepam) presents several similarities with praziquantel with regard to its anti-schistosomal mode of action, since both drugs cause spastic paralysis, calcium influx and tegumental disruption in the parasites. In order to know whether the two compounds share the same binding sites in the schistosomes, we performed in vivo and in vitro competition experiments. We took advantage of the fact that Ro 11-3128 is active against immature Schistosoma mansoni (whereas praziquantel is inactive), and praziquantel is active against S. japonicum (which is insensitive to Ro 11-3128). An excess of praziquantel did not inhibit the activity of Ro 11-3128 against immature S. mansoni and an excess of Ro 11-3128 did not inhibit the activity of praziquantel against S. japonicum, suggesting that the schistosome binding sites of the two drugs are different. On the other hand, cytochalasin D, an agent known to perturb – among other things – calcium channel function, was capable of inhibiting the schistosomicidal activity of both praziquantel and Ro 11-3128, thus adding another element of similarity between the two anti-schistosomal agents. A similar, albeit partial, inhibition of the schistosomicidal activity of the two drugs was exerted by some of the classical calcium channel blockers. Taken together, these results suggest that praziquantel and Ro 11-3128, although binding to different schistosome receptor sites, may use the same basic anti-schistosomal effector mechanisms.

scholarly journals Investigation of Calcium Channel Blockers as Antiprotozoal Agents and Their Interference in the Metabolism ofLeishmania (L.) infantum

2016 ◽  
Vol 2016 ◽  
pp. 1-9 ◽  
Author(s):  
Juliana Quero Reimão ◽  
Juliana Tonini Mesquita ◽  
Daiane Dias Ferreira ◽  
Andre Gustavo Tempone
Keyword(s):  
Calcium Channel ◽  
Chagas Disease ◽  
Calcium Channel Blockers ◽  
Channel Blockers ◽  
Antiprotozoal Activity ◽  
Additive Interaction ◽  
Therapeutic Class ◽  
Species Production

Leishmaniasis and Chagas disease are neglected parasitic diseases endemic in developing countries; efforts to find new therapies remain a priority. Calcium channel blockers (CCBs) are drugs in clinical use for hypertension and other heart pathologies. Based on previous reports about the antileishmanial activity of dihydropyridine-CCBs, this work aimed to investigate whether thein vitroanti-Leishmania infantumand anti-Trypanosoma cruziactivities of this therapeutic class would be shared by other non-dihydropyridine-CCBs. Except for amrinone, our results demonstrated antiprotozoal activity for fendiline, mibefradil, and lidoflazine, with IC50values in a range between 2 and 16 μM and Selectivity Index between 4 and 10. Fendiline demonstrated depolarization of mitochondrial membrane potential, with increased reactive oxygen species production in amlodipine and fendiline treatedLeishmania, but without plasma membrane disruption. Finally,in vitrocombinations of amphotericin B, miltefosine, and pentamidine againstL. infantumshowed in isobolograms an additive interaction when these drugs were combined with fendiline, resulting in overall mean sum of fractional inhibitory concentrations between 0.99 and 1.10. These data demonstrated that non-dihydropyridine-CCBs present antiprotozoal activity and could be useful candidates for futurein vivoefficacy studies against Leishmaniasis and Chagas’ disease.

scholarly journals The angiotensin II type 1 receptor blocker azilsartan can overwhelm the sympathetic nerve activation stimulated by coadministration of calcium channel blockers

2019 ◽  
Vol 20 (1) ◽  
pp. 147032031983952 ◽  
Author(s):  
Michio Fukuda ◽  
Yukako Isobe-Sasaki ◽  
Ryo Sato ◽  
Toshiyuki Miura ◽  
Masashi Mizuno ◽  
...  
Keyword(s):  
Angiotensin Ii ◽  
Calcium Channel ◽  
Calcium Channel Blockers ◽  
Sympathetic Nerve ◽  
Sympathetic Nerve Activity ◽  
The Other ◽  
Channel Blockers ◽  
Nerve Activity ◽  
The Relationship

Objective: In our recent study, non-Gaussianity of heart rate variability (λ25s), an indicator of sympathetic nerve activity, did not change during two-day treatment with the angiotensin II type 1 receptor blocker (ARB) azilsartan. Coadministration of calcium channel blockers (CCBs) might affect the study results. Methods: In this subanalysis, 20 patients with chronic kidney disease (14 men; age 61±15 years) were divided into three groups: patients with coadministration of L-type CCB, patients without coadministration of CCB, and patients with coadministration of sympathoinhibitory (L/T- or L/T/N-type) CCB. λ25s was calculated separately in daytime and nighttime. Results: Daytime λ25s at baseline was higher in patients with L-type CCB coadministration (0.62±0.18, n = 5) compared with those without CCB (0.49±0.13, n = 11) and those with sympathoinhibitory CCB (0.46±0.06, n = 4). The relationship between the changes in daytime λ25s and systolic blood pressure was positive in patients with L-type CCB coadministration, whereas the relationship was inverse in the other two groups. A larger decrease in daytime λ25s was shown in patients with L-type CCB coadministration compared with those in the other two groups. Conclusions: CCBs, as well as diuretics, are recommended as second-line antihypertensive agents. Our results suggested that ARBs can overwhelm the activation of sympathetic nerve activity stimulated by coadministration of L-type CCBs.

scholarly journals In Vivo and Ex Vivo Evaluation of L-Type Calcium Channel Blockers on Acid β-Glucosidase in Gaucher Disease Mouse Models

PLoS ONE ◽  
2009 ◽  
Vol 4 (10) ◽  
pp. e7320 ◽  
Author(s):  
Ying Sun ◽  
Benjamin Liou ◽  
Brian Quinn ◽  
Huimin Ran ◽  
You-Hai Xu ◽  
...  
Keyword(s):  
Calcium Channel ◽  
Mouse Models ◽  
Calcium Channel Blockers ◽  
Gaucher Disease ◽  
Ex Vivo ◽  
Channel Blockers

Study of the protective effect of calcium channel blockers against neuronal damage induced by glutamate in cultured hippocampal neurons

2013 ◽  
Vol 65 (3) ◽  
pp. 730-736 ◽  
Author(s):  
Krzysztof Sendrowski ◽  
Małgorzata Rusak ◽  
Piotr Sobaniec ◽  
Elżbieta Iłendo ◽  
Milena Dąbrowska ◽  
...  
Keyword(s):  
Protective Effect ◽  
Calcium Channel ◽  
Calcium Channel Blockers ◽  
Hippocampal Neurons ◽  
Neuronal Damage ◽  
Channel Blockers ◽  
Cultured Hippocampal Neurons
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