The Chemotherapeutic Action of Phenanthridine Compounds

Ethidium bromide: pharmacokinetics and efficacy against trypanosme infections in rabbits and calves

“…That the bile should be a major route of ethidium excretion is in accordance with the findings of Schanker & Soloman (1963), Schanker (1968) and Nayak & Schanker (1969) who presented evidence for the active transport of tertiary and quarternary ammonium compounds into the bile of rats. Biliary excretion of phenanthridines has also been reported by other workers (Goodwin, Goss & Lock, 1950;Taylor, 1960a;MacGregor & Clarkson, 1971. In rabbits with cannulated bile ducts, no drug was found in the faeces and the rate of appearance of radioactivity in the bile over the first 12 h following treatment was approximately the same as was found in the faeces of uncannulated ethidium-treated rabbits.…”

The Chemotherapeutic Action of Phenanthridine Compounds

“…The first of these drugs has been shown to be active Goodwin, Goss, Lock, and Walls, 1950) when given during the incubation period, but not against an established infection, whereas 3C47 is active under both conditions. It seems probable from this evidence that although 6C46 is toxic to the blood forms of the parasite, it is either inactive against the intracellular forms, or does not penetrate readily enough to produce a concentration lethal to the enclosed parasites.…”

“…The effects of drugs upon T. cruzi in tissue culture The method of maintaining T. cruzi in tissue culture was similar to that described by Hawking (1946), with a modification in the method of infection. Explants from the hearts of embryo rats were placed in a thick suspension of T. cruzi in serum-Tyrode mixture.…”

“…The trypanosomes were examined for motility. Estimations of drug were made by the method described in Part III of this work (Goodwin, Goss, and Lock, 1950).…”

Trypanocidal Action of Phenanthridine Compounds: Further 2:7‐diamino Phenanthridinium Compounds

“…2: 7-Dicarbethoxyamino Phenanthridinium Compounds (Table V).-It has been reported previously that interference with the primary amino groups in the 2: 7-positions greatly reduces trypanocidal activity against African species of trypanosomes, though such compounds may possess activity against the South American T. cruzi (Goodwin et al, 1950). I have prepared and tested a number of such compounds.…”