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Chemical Compound Review

Amocarzina     4-methyl-N-[4-[(4- nitrophenyl)amino]phenyl...

Synonyms: Amocarzine, Amocarzinum, AC1NUYYE, CHEMBL469328, Cgp-6140, ...
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Disease relevance of Phenthiourezine

  • An open clinical trial of amocarzine was carried out in onchocerciasis patients in Ecuador and Guatemala [1].
  • Twenty-eight patients who had skin snips positive for microfilariae (Mf) were studied 120 days after receiving amocarzine, when each was negative for Mf: 16 (57%) were positive for O. volvulus DNA in the PCR-based assay [2].
  • The clinical investigations with three types of a three days regimen of amocarzine permitted to adjust the fixed dosing to the body weight related dosing and subsequently the administration of amocarzine from fasting state to drug intake after food [3].

High impact information on Phenthiourezine


Chemical compound and disease context of Phenthiourezine


Biological context of Phenthiourezine


Anatomical context of Phenthiourezine

  • In addition, the glandular esophagus demonstrated degenerative alterations of the cytoplasm and loosening of the cuticular lining after exposure to CGP 6140 [7].

Associations of Phenthiourezine with other chemical compounds


Gene context of Phenthiourezine

  • At 20-28 h after the application of amocarzine, mf were degenerated or dead and a marked eosinophil-parasite adherence (EPA) reaction was seen, with intense staining for intra- and extracellular eosinophil granule proteins such as eosinophil cationic protein (ECP) surrounding the mf [6].

Analytical, diagnostic and therapeutic context of Phenthiourezine

  • Fully automated analytical system using liquid-solid extraction and liquid chromatography for the determination of CGP 6140 in plasma [13].
  • CGP 6140 is currently undergoing clinical trials in patients suffering from onchocercosis [12].
  • Ultrasonography of onchocercal skin nodules detected changes within the nodules following amocarzine therapy [3].
  • Since amocarzine and its major N-oxide metabolite are coloured agents, urine colorimetry was used to assess the urinary excretion of the N-oxide qualitatively [14].
  • The present results indicate that an ophthalmologic real time linear scanner can be used in the bidimensional mode as a non-invasive method to assess sequentially the events in superficial onchocercal nodules following chemotherapy with amocarzine [15].


  1. Onchocercacidal effects of amocarzine (CGP 6140) in Latin America. Poltera, A.A., Zea-Flores, G., Guderian, R., Beltranena, F., Proana, R., Moran, M., Zak, F., Striebel, H.P. Lancet (1991) [Pubmed]
  2. Polymerase chain reaction-based assessment after macrofilaricidal therapy in Onchocerca volvulus infection. Nutman, T.B., Parredes, W., Kubofcik, J., Guderian, R.H. J. Infect. Dis. (1996) [Pubmed]
  3. Amocarzine investigated as oral onchocercacidal drug in 272 adult male patients from Guatemala. Results from three dose regimens spread over three days. Zea-Flores, G., Beltranena, F., Poltera, A.A., Lopez, M., Moran, M., Zea-Flores, C.E., de Ramirez, I., Lecaillon, J.B., Zak, F., Palomo, M. Trop. Med. Parasitol. (1991) [Pubmed]
  4. The influence of food on the pharmacokinetics of CGP 6140 (amocarzine) after oral administration of a 1200 mg single dose to patients with onchocerciasis. Lecaillon, J.B., Dubois, J.P., Soula, G., Pichard, E., Poltera, A.A., Ginger, C.D. British journal of clinical pharmacology. (1990) [Pubmed]
  5. Pharmacokinetics of CGP 6140 (amocarzine) after oral administration of single 100-1600 mg doses to patients with onchocerciasis. Lecaillon, J.B., Dubois, J.P., Awadzi, K., Poltera, A.A., Ginger, C.D. British journal of clinical pharmacology. (1990) [Pubmed]
  6. Immunoelectron microscopic evidence for release of eosinophil granule matrix protein onto microfilariae of Onchocerca volvulus in the skin after exposure to amocarzine. Gutiérrez-Peña, E.J., Knab, J., Büttner, D.W. Parasitol. Res. (1998) [Pubmed]
  7. Electron microscopic studies on the effects of CGP 6140 and CGP 20376 on microfilariae and third stage larvae of Onchocerca volvulus. Strote, G. Trop. Med. Parasitol. (1989) [Pubmed]
  8. In vivo effect of benzothiazole and amoscanate derivatives on the fine structure of adult Brugia spp. and Litomosoides carinii. Franz, M., Zahner, H., Mehlhorn, H., Striebel, H.P. Parasitol. Res. (1990) [Pubmed]
  9. Modulatory effects of antifilarial drugs ivermectin, CGP 6140 and CGP 20376 on the oxidative burst of eosinophilic granulocytes. Tischendorf, F.W., Brattig, N.W., Hoyer, A., Medina-De la Garza, C.E., Geisinger, F. Acta Trop. (1993) [Pubmed]
  10. Influence of food related to dose on the pharmacokinetics of amocarzine and of its N-oxide metabolite, CGP 13 231, after oral administration to 20 onchocerciasis male patients from Guatemala. Lecaillon, J.B., Poltera, A.A., Zea-Flores, G., de Ramirez, I., Nowell de Arevalo, A. Trop. Med. Parasitol. (1991) [Pubmed]
  11. Studies on the activity of the Ciba Geigy compounds CGP 6140, 20376, 20309 and 21833 against third and fourth stage larvae of Onchocerca volvulus. Strote, G. Trop. Med. Parasitol. (1989) [Pubmed]
  12. Activity, mechanism of action and pharmacokinetics of 2-tert-butylbenzothiazole and CGP 6140 (amocarzine) antifilarial drugs. Köhler, P., Davies, K.P., Zahner, H. Acta Trop. (1992) [Pubmed]
  13. Fully automated analytical system using liquid-solid extraction and liquid chromatography for the determination of CGP 6140 in plasma. Rouan, M.C., Campestrini, J., Lecaillon, J.B., Dubois, J.P., Lamontagne, M., Pichon, B. J. Chromatogr. (1988) [Pubmed]
  14. Onchocercacidal effect of three drug regimens of amocarzine in 148 patients of two races and both sexes from Esmeraldas, Ecuador. Guderian, R.H., Anselmi, M., Proaño, R., Naranjo, A., Poltera, A.A., Moran, M., Lecaillon, J.B., Zak, F., Cascante, S. Trop. Med. Parasitol. (1991) [Pubmed]
  15. Use of an ophthalmologic ultrasoundscanner in human onchocercal skin nodules for non-invasive sequential assessment during a macrofilaricidal trial with amocarzine in Guatemala. The first experiences. Poltera, A.A., Reyna, O., Zea-Flores, G., Beltranena, F., Nowell de Arevalo, A., Zak, F. Trop. Med. Parasitol. (1991) [Pubmed]
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