Characterisation of the relaxant response to raloxifene in porcine coronary arteries

Moritz, Alkje; Radtke, Oliver A.; Gust, Ronald; Glusa, Erika; Pertz, Heinz H.

doi:10.1016/j.ejphar.2006.06.049

Cited by 12 publications

(18 citation statements)

References 36 publications

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“…The results observed indicated that both compounds 5 and 6 were the most active, as compound 5 and 6 showed a calcium channel blocking potency of 6.46±0.07 and 6.35±0.10 respectively. The observed antagonistic results for 5 and 6 are comparable with the standard calcium channel blocker verapamil which exhibited a blocking potency of 6.97±0.15 and the potency of m-nifedipine (7.48±0.05) (Moritz et al, 2006) was not achieved. On the other hand, the maximal antagonistic effect, expressed as a percentage E max value, of 106±5 observed by verapamil and of 101±1 by m-nifedipine was not achieved by all derivatives, since the highest E max results was found by 99±1, observed for both compounds 3 and 5.…”

Section: Discussionsupporting

confidence: 55%

“…The calcium channel blocking (CCBA) of 1, 4-DHP derivatives 1-6 was determined using PCASM assay (Moritz et al, 2006). The CCBA results of tested compounds are shown in Table 2.…”

Section: Pharmacological Activitymentioning

confidence: 99%

“…The presence or absence of endothelium was assessed functionally by measuring the extent of endotheliumdependent relaxation following application of substance P (10 nM) after the third KCl challenge. To inhibit vascular eicosanoid production by cyclooxygenase, experiments were performed in the continuous presence of indomethacin (6 µM) (Moritz et al, 2006).…”

Section: Synthesis Of Methyl-3-aminocrotonate Bmentioning

confidence: 99%

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Synthesis and Calcium Channel Blocking Activity of 1, 4-Dihydropyridine Derivatives Containing Ester Substitute and Phenyl Carbamoyl Group

Sadek¹

2011

American Journal of Applied Sciences

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Problem statement: Several studies on the synthesis of new nifedipine analogs have been carried out, but the literature reveled that no study on the synthesis and calcium channel blocking activity of the substituted ester with an amide (5-phenylcarbamoyl) moiety has been reported. Approach: Six new derivatives of m-nifedipine have been successfully synthesized by substituting an ester moiety with an amide (5-phenylcarbamoyl) moiety, using a modified Hantzsch reactions and tested for their pharmacological activities. The nifedipine analogs 1-6 were characterized and confirmed using elemental analysis, Infrared spectroscopy (IR), Nuclear Magnetic Resonance ( 1 H NMR) and Mass spectroscopy. The purity of the compounds was ascertained by melting point and TLC. The in vitro calcium channel blocking activities were evaluated using the high K + concentration of Porcine Coronary Artery Smooth Muscles (PCASM) assay. Results: The compounds (1-2) failed to exhibit any blocking activity (IC50 = 10 −7 to 10 −5 M range), while the compounds 3-6 relaxed precontracted porcine coronary artery smooth muscles with pEC50 values ranging between 4.37±0.10 (compound 3) and 6.46±0.07 (compound 5), indicating that compounds 3-6 exhibit comparable potencies in blocking calcium channels to reference drug varapamil (6.97±0.15) and m-nifedipine (6.48±0.05). Conclusion: The results of this study showed that some of the developed new compounds possess maximal calcium channel blocking effects comparable to m-nifedipine. The developed compounds in the present study will predicatively show an increased metabolic stability and consequently longer duration of actions compared to m-nifedipine and could be, therefore, suitable candidates for further optimization to be evaluated as a new class of antihypertensive drugs.

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Section: Discussionsupporting

confidence: 55%

“…The calcium channel blocking (CCBA) of 1, 4-DHP derivatives 1-6 was determined using PCASM assay (Moritz et al, 2006). The CCBA results of tested compounds are shown in Table 2.…”

Section: Pharmacological Activitymentioning

confidence: 99%

Section: Synthesis Of Methyl-3-aminocrotonate Bmentioning

confidence: 99%

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Synthesis and Calcium Channel Blocking Activity of 1, 4-Dihydropyridine Derivatives Containing Ester Substitute and Phenyl Carbamoyl Group

Sadek¹

2011

American Journal of Applied Sciences

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“…This may be due to inhibition of voltage gated or receptor operated calcium channels. Estrogen has also been shown to promote coronary vasodilation (28). It is possible that a low dose of estrogen induces increased coronary vasodilation, improved cardiac perfusion, and overall increased functional recovery.…”

Section: Discussionmentioning

confidence: 99%

Postischemic Infusion of 17-β-Estradiol Protects Myocardial Function and Viability

Terrell

Crisostomo

Markel

et al. 2008

Journal of Surgical Research

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Background-Females demonstrate improved cardiac recovery after ischemia-reperfusion (I/R) injury compared to males. Attenuation of myocardial dysfunction with pre-ischemic estradiol suggests that estrogen may be an important mediator of this cardioprotection. However, it remains unclear whether post injury estradiol may have clinical potential in the treatment of acute myocardial infarction. We hypothesize that post-ischemic administration of 17β-estradiol will decrease myocardial I/R injury, and improve left ventricular cardiac function.

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“…It is able to relax porcine coronary arteries in vitro due to activation of the mitogen-activated protein kinase (MAPK) pathway [13]. P38 MAPK activation has been shown to be responsible for cardioprotection during ischemic preconditioning [14].…”

Section: Selective Estrogen Receptor Modulatorsmentioning

confidence: 99%

Breast Cancer, Estrogen Receptor and Ligands

Bai

Gust²

2009

Archiv der Pharmazie

Self Cite

114

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This review emphasizes the relationship of breast cancer, estrogen receptor and ligands, especially the centrality of the estrogen receptor, which mediates on one hand the hormone-induced gene transcription and on the other hand the anti-estrogen action against breast cancer. The characterization of the estrogen receptor ligand-binding domain co-crystallized with agonists or antagonists provided a molecular basis to gain an insight into the regulation of estrogen receptor and, thereby, to describe the mechanism of the hormone therapy in treating breast cancer.

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Characterisation of the relaxant response to raloxifene in porcine coronary arteries

Cited by 12 publications

References 36 publications

Synthesis and Calcium Channel Blocking Activity of 1, 4-Dihydropyridine Derivatives Containing Ester Substitute and Phenyl Carbamoyl Group

Synthesis and Calcium Channel Blocking Activity of 1, 4-Dihydropyridine Derivatives Containing Ester Substitute and Phenyl Carbamoyl Group

Postischemic Infusion of 17-β-Estradiol Protects Myocardial Function and Viability

Breast Cancer, Estrogen Receptor and Ligands

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