Benzo(B)Thiophene-2-Carboxylic acid: Calcium uptake and cyclic AMP production in isolated bone cells

  title={Benzo(B)Thiophene-2-Carboxylic acid: Calcium uptake and cyclic AMP production in isolated bone cells},
  author={J. C. Robin and M J Brown and N. Weinfeld and R. Dziak},
  journal={Calcified Tissue International},
SummaryThe purpose of the present study was to investigate the mechanism of action on bone of Benzo(B)Thiophene-2-Carboxylic Acid (BL-5583). BL-5583, at a dose range of 0.01–100 µg/ml, inhibited spontaneous as well as A23187 and PTH-induced bone resorption in tissue culture. This compound also decreased calcium uptake in both osteoclastic and osteoblastic enriched bone cell populations obtained by sequential collagenase digestion of 1–2 day newborn rat calvariae. The decrease occurred after a 5… 
Effects of thionapthene 2-carboxylic acid and related compounds on bone resorption in organ culture
TNCA had a powerful inhibitory effect when it was added to bones that had previously escaped from CT, and this suggests that TNCA will be most effective under conditions of accelerated bone resorption when an inhibiting effect is most desirable.
Crystal structure from laboratory X-ray powder diffraction data, DFT-D calculations, Hirshfeld surface analysis, and energy frameworks of a new polymorph of 1-benzothiophene-2-carboxylic acid
Several benzothiophene-based compounds, including 1-benzothiophene-2-carboxylic acid, exhibit a wide variety of pharmacological activities. They have been extensively used to treat various types of


Responses of fetal rat bone cells and bone organ cultures to the ionophore, A23187
At low concentrations, A23187 produced effects on bone similar to those of parathyroid hormone, suggesting that calcium is the primary initiator of PTH-induced bone resorption, and at the higher concentrations A23 187 may have a general inhibitory effect on cell metabolism.
Effects of vitamin D3 metabolites on bone cell calcium transport
  • R. Dziak
  • Biology
    Calcified Tissue Research
  • 2005
SummaryThe vitamin D3 metabolite, 25-hydroxycholecalciferol, at concentrations of 0.01 to 10.0 μg/ml, decreased calcium uptake by isolated bone cells. The effect occurred within 1 min after the
Calcium-mediated enhancement of the cyclic AMP response in cultured bone cells
Results indicate that Ca2+ and other cations are positive effectors of the stimulated cyclic AMP response in isolated bone cells, most consistent with enhancement of adenylate cyclase reactivity as the mode of cation action.
Calcium transport in isolated bone cells. III. Effects of parathyroid hormone and cyclic 3',5'-AMP.
It is postulated that PTH increases the permeability of bone cell membranes to calcium by magnifying the effects of parathyroid hormone at 4 C, the membrane is relatively impermeable so the PTH effect is magnified.
Biochemical characterization with parathormone and calcitonin of isolated bone cells: provisional identification of osteoclasts and osteoblasts.
Two metabolically distinct types of bone cell populations were isolated from mouse calvaria by a repetitive digestive procedure with a mixture of collagenase and trypsin, and it is postulate that the CT type of populations is enriched in osteoclasts and, possibly, osteocytes, and the PT type of population is enrichment in osteoblasts.
Calcitonin--a new hormone from the pa rathyroid which lowers blood calcium.
  • D. Copp
  • Medicine, Biology
    Oral surgery, oral medicine, and oral pathology
  • 1963
2-Thiophenecarboxylic Acid: Inhibitor of Bone Resorption in Tissue Culture
In tissue culture 2-thiophenecarboxylic acid inhibited both spontaneous resorption of bone and that induced by parathyroid hormone. Its action was to inhibit calcium transfer out of bone.
Divalent cation ionophores stimulate resorption and inhibit DNA synthesis in cultured fetal rat bone.
Two divalent cation ionophores, A23187 and Ionomycin, which are selective for calcium, stimulated the resorption of fetal rat long bones in organ culture at 0.1 to 1 micromolar but not at higher concentrations, implying that cell replication is not required for osteoclast formation in fetalRat long bone cultures.
Calcium transport in isolated bone cells II. Calcium transport studies
Calcium transport was studied in bone cells isolated from fetal rat calvaria and uptake experiments revealed an active component of calcium exchange that appeared to be dependent on medium phosphate concentration.