ArticlePharmaceutical research1998
Bisphosphonates and tetracycline: experimental models for their evaluation in calcium-related disorders.
Article in Pharmaceutical research, 1998. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 8 papers.
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Who cites it
8 citing papers in PubMed, 32 citations in OpenAlex.
- Synthesis of a Series of Heterocyclic N-Substituted Derivatives of Alendronic Acid and Their Preliminary Biological Evaluation.Chemistry & biodiversity · 2026Article
- Calcinosis in dermatomyositis: Origins and possible therapeutic avenues.Best practice & research. Clinical rheumatology · 2022Review
- Clinical Treatment Options in Scleroderma: Recommendations and Comprehensive Review.Clinical reviews in allergy & immunology · 2022Review
- Familial tumoral calcinosis and the role of O-glycosylation in the maintenance of phosphate homeostasis.Biochimica et biophysica acta · 2009Review
- GALNT3, a gene associated with hyperphosphatemic familial tumoral calcinosis, is transcriptionally regulated by extracellular phosphate and modulates matrix metalloproteinase activity.Biochimica et biophysica acta · 2009Article
- Bone-specific drug delivery systems: approaches via chemical modification of bone-seeking agents.Clinical pharmacokinetics · 2003Review
- Inhibition of nanobacteria by antimicrobial drugs as measured by a modified microdilution method.Antimicrobial agents and chemotherapy · 2002Article
- Synthesis and preclinical pharmacology of 2-(2-aminopyrimidinio) ethylidene-1,1-bisphosphonic acid betaine (ISA-13-1)-a novel bisphosphonate.Pharmaceutical research · 1999Article
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Authors and funding
9 authors at 3 institutions in 3 countries.
Funding
Abstract
purposeThis work was aimed at synthesizing novel bisphosphonates (BPs) and examining them in comparison to clinically used BPs such as pamidronate and alendronate, and to tetracycline, in order to evaluate their potential as anticalcification and antiresorption agents. The correlation between the various models was examined in order to establish facile experimental models for pre-screening of potential compounds.
methodsNitrogen-containing heterocyclic, novel BPs such as 2-(3-methylimidazolio) ethylidene-1,1-bisphosphonic acid betaine (VS-5b), 2-(2-dimethylamino-4-pyrazinio)ethylidene-1,1-bisphosphonic acid betaine (VS-6b), and 2-(2-alpha-pyridylethylthio) ethylidene-1,1-bisphosphonic acid (ISA-225), were synthesized and evaluated in comparison to clinically used BPs, in various experimental models of resorption and calcification.
resultsThe physicochemical properties of the novel compounds are slightly different than the BPs in clinical use: the pKa values are lower, the affinity for hydroxyapatite is lower and the solubilities of the calcium salts are higher. The anticalcification potencies of the novel compounds were high and ranked as follows: alendronate = pamidronate > VS-6b = VS-5b = ISA-225 > tetracycline. The in vivo antiresorption activity of VS-5b and VS-6b in comparison to that of the clinically employed, pamidronate, was shown to be similar and higher, respectively.
conclusionsThe anticalcification activity of the novel compounds as well as that of tetracycline was lower than that of alendronate. The antiresorption activity of VS-6b was similar to that of pamidronate. A good correlation between the different models was found, enabling the facile screening of novel compounds. The activities of tetracycline and EDTA highlight the distinct behavior of BPs as "crystal poison." In addition, tetracycline was found to be a potent anticalcification agent in the ectopic calcification model.
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