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Chemical Compound Review

Diacarb     N-(5-sulfamoyl-1,3,4- thiadiazol-2...

Synonyms: Diuramide, Glauconox, Glaupax, Acetazolam, Diamox, ...
 
 
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Disease relevance of Diacarb

 

Psychiatry related information on Diacarb

 

High impact information on Diacarb

 

Chemical compound and disease context of Diacarb

 

Biological context of Diacarb

 

Anatomical context of Diacarb

  • Acetazolamide, in a dose sufficient to inhibit the erythrocyte carbonic anhydrase (EC 4.2.1.1), thus induced a rapid and marked increase in CBF, leaving CMRO2 unchanged [23].
  • This effect of acetazolamide on CBF is probably explained by a decrease in brain pH rather than by brain tissue hypoxia due to inhibition of oxygen unloading in the brain capillaries [23].
  • Absolute reabsorption of bicarbonate was also significantly higher in superficial than in juxtamedullary nephrons after administration of acetazolamide (727 +/- 82 vs. 346 +/- 126 pmol/min; P less than 0.05) [24].
  • Bicarbonate reabsorption that was insensitive to acetazolamide occurred in the superficial and deep loop of Henle and between the distal tubule and base collecting duct [25].
  • Blocking the carbonic anhydrase with acetazolamide (100 mg/kg) completely prevented the protective effect of a 1 M HCO3- infusion, and 6 out of 8 stomachs ulcerated [26].
 

Associations of Diacarb with other chemical compounds

  • Thus, acetazolamide caused either inhibition or stimulation of Na+ uptake depending on the conditions with respect to pH and HCO3- gradients [27].
  • Furthermore, an outwardly directed bicarbonate concentration gradient from the deep loop of Henle to vasa recta was demonstrated during acetazolamide (delta tCO2 = 20.9 +/- 3.3 mM), but was abolished during combined mannitol and acetazolamide administration (delta tCO2 = 3.5 +/- 0.9 mM) [25].
  • In addition, acetazolamide may potentiate the phosphaturic effect of parathyroid hormone by promoting accumulation of cyclic AMP in tissue [28].
  • Addition of forskolin stimulated an increase in short-circuit current that was likely a result of bicarbonate secretion because it was inhibited by a HCO3(-)-free solution, by addition of the carbonic anhydrase inhibitor, acetazolamide, or by mucosal addition of the anion channel blocker, diphenylamine 2-carboxylate [29].
  • The reaction depends upon the trapping of OH ions produced during gastric stimulation and is blocked by the benzimidazole, Hassle 149/94, which inhibits the K+ + H+-ATPase and by acetazolamide, an inhibitor of carbonic anhydrase activity [30].
 

Gene context of Diacarb

  • Some remarkable clinical features were observed in a large hypoPP family carrying an SCN4A mutation: a complete penetrance in men and women, an early age at onset, postcritic myalgias and an increased number and severity of attacks induced by acetazolamide [31].
  • Similar to CA VA, CA VB is a "low activity" enzyme with a sensitivity to acetazolamide [32].
  • The valproyl derivative of acetazolamide (5-valproylamido-1,3,4-thiadiazole-2-sulfonamide, 6M) was one of the best hCA I and hCA II inhibitor in the series and exhibited very strong anticonvulsant properties in an MES test in mice [33].
  • The isoenzyme CA III, which is resistant to inhibition by sulfonamides, did not appear to be present in these ocular tissues, since the histochemical staining of enzyme activity was completely abolished by 10(-6) M acetazolamide [34].
  • Cerebral perfusion reserve was obtained from 6 patients (3 MELAS, 1 MERRF, 1 KSS, 1 CCOD) for a comparative analysis using the split-dose 123I-IMP SPECT method before and after the injection of acetazolamide [35].
 

Analytical, diagnostic and therapeutic context of Diacarb

References

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  2. Letter: Anticonvulsants, acetazolamide and osteomalacia. Mallette, L.E. N. Engl. J. Med. (1975) [Pubmed]
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  19. Mapping the gene for acetazolamide responsive hereditary paryoxysmal cerebellar ataxia to chromosome 19p. von Brederlow, B., Hahn, A.F., Koopman, W.J., Ebers, G.C., Bulman, D.E. Hum. Mol. Genet. (1995) [Pubmed]
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  23. Effect of acetazolamide on cerebral blood flow and cerebral metabolic rate for oxygen. Vorstrup, S., Henriksen, L., Paulson, O.B. J. Clin. Invest. (1984) [Pubmed]
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  32. Human mitochondrial carbonic anhydrase VB. cDNA cloning, mRNA expression, subcellular localization, and mapping to chromosome x. Fujikawa-Adachi, K., Nishimori, I., Taguchi, T., Onishi, S. J. Biol. Chem. (1999) [Pubmed]
  33. Carbonic anhydrase inhibitors: anticonvulsant sulfonamides incorporating valproyl and other lipophilic moieties. Masereel, B., Rolin, S., Abbate, F., Scozzafava, A., Supuran, C.T. J. Med. Chem. (2002) [Pubmed]
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  35. SPECT findings in mitochondrial encephalomyopathy. Watanabe, Y., Hashikawa, K., Moriwaki, H., Oku, N., Seike, Y., Kodaka, R., Ono, J., Uehara, T., Kusuoka, H., Nishimura, T. J. Nucl. Med. (1998) [Pubmed]
  36. Distal tubule bicarbonate accumulation in vivo. Effect of flow and transtubular bicarbonate gradients. Iacovitti, M., Nash, L., Peterson, L.N., Rochon, J., Levine, D.Z. J. Clin. Invest. (1986) [Pubmed]
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