Detail of "536-71-0"

Reference

Determination of diminazene in plasma by high-performance liquid chromatography

Determination of diminazene in plasma by high-performance liquid chromatography. Fouda, Hassan G. (Dep. Drug Metab., Pfizer Inc., Groton, Conn., USA). J. Chromatogr. Sci., 15(11), 537-8 (English) 1977. CODEN: JCHSBZ. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacodynamics) An anal. method is described for detg. diminazene (I) [536-71-0] levels in plasma of cattle. I is reduced to 4-aminobenzamidine which is extd. and assayed by high-performance ion pair reverse phase partition chromatog. The column was a C8 Chromegabond column and the mobile phase was an aq. soln. contg. 80 mg 1-pentane sulfonic acid in 300 mL water with 5 mL glacial acetic acid and 700 mL methanol. The internal std. was 3,4-dimethoxybenzamidine. I levels as low as 0.1 mg/mL were detected.

Chemotherapy of Trypanosoma venezuelense (T

evansi). II. Activity of metal-free organic trypanocides in mice and in vitro. Minelli, Elisa B.; Iudice, G.; Ercoli, N. (Fac. Cienc., Universidad Central de Venezuela, Caracas, Venez.). Ann. Trop. Med. Parasitol., 75(4), 383-92 (English) 1981. CODEN: ATMPA2. ISSN: 0003-4983. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacodynamics) Among the org. trypanocides, Suramin [145-63-1] is the most effective against exptl. infestation of mice with T. venezuelense (a dyskinetoplastic variant of T. evansi): its s.c. clearing does is 0.5 mg/kg and the curative dose 0.75 mg/kg. The clearing doses of Pentamidine [100-33-4], diminazene [536-71-0], and quinapyramine [3270-78-8] are of the same order, but 15-20-fold higher doses are required for cure. Intermittent administration of smaller Pentamidine doses over a 2-mo period improves its curative potential. The cure of mice treated with a single 20-mg/kg Pentamidine dose begins after a 2-wk lag period, when only traces of the drug remain, as revealed by blood and organ subinoculations. The phenanthridines ethidium, prothidium, and isometidium were ineffective, and this is attributed to their more specific action on the kinetoplast, lacking in T. venezuelense. Hydroxystilbamidine and Acriflavine caused only short and temporary clearing, even after repeated administration. Following diamidine and quinapyramine injections, the parasitemia increased during the 1st day, remained stationary on the 2nd, and was cleared on the 3rd day. The curative/clearing dose ratio varied between 1.5 and 40, with a wide scatter among different drugs and for the same drug in infections with different trypanosomes, suggesting differences in the specificity of the trypanocidal and trypanostatic drug actions. In vitro, morphol. variations and virulence diminution were dependent on drug concn. and time of exposure. Vacuolization and swelling were accompanied by inhibition or decrease of virulence, without any definite relation between morphol. and virulence. With a comparable visible deformation, hydroxystilbamidine perhaps affects the virulence less than Pentamidine, which would be in agreement with its lower in vivo activity.