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Chemotherapy of human African trypanosomiasis.
TLDR
Four drugs have been licensed to treat human African trypanosomiasis and two of them, pentamidine and suramin, are used prior to CNS involvement, while melarsoprol is used once parasites are established in the CNS. Expand
Megazol combined with suramin: a chemotherapy regimen which reversed the CNS pathology in a model of human African trypanosomiasis in mice
TLDR
Results suggest that the megazol‐suramin combination combination treatment reversed the central nervous system pathology in this model of HAT, indicating that this chemotherapy regimen was curative. Expand
Synthesis and biological activity of nitro heterocycles analogous to megazol, a trypanocidal lead.
TLDR
Megazol was evaluated on primates infected with Trypanosoma brucei gambiense, including late-stage central nervous system infections in combination with suramin, and full recovery was observed in five monkeys in the study with no relapse of parasitemia within a 2 year follow-up. Expand
Activity of Megazol, a Trypanocidal Nitroimidazole, Is Associated with DNA Damage
TLDR
DNA damage associated with the trypanocidal activity of megazol was shown in experiments in which DNA repair-deficient RAD51−/−Trypanosoma brucei mutants were found to be hypersensitive to the drug. Expand
Sleeping sickness and the brain
TLDR
This review summarizes the current understanding of the neurological aspects of sleeping sickness, and envisages new research into blood-brain barrier models that are necessary to understand the interactions between trypanosomes and drugs active against them within the host nervous system. Expand
Effect of megazol on Trypanosoma brucei brucei acute and subacute infections in Swiss mice.
TLDR
Combined suramin and megazol treatment did prove effective and the mice were shown to have remission without further relapse from the central nervous system (CNS) and the study of threemegazol derivatives is also described here. Expand
Trypanosoma brucei brucei: a long-term model of human African trypanosomiasis in mice, meningo-encephalitis, astrocytosis, and neurological disorders.
TLDR
A chronic experimental model of HAT in mice infected with T. b. Expand
Pharmacokinetics, metabolism and excretion of megazol in a Trypanosoma brucei gambiense primate model of human African trypanosomiasis. Preliminary study.
TLDR
It is indicated that megazol crosses the blood-brain barrier after oral administration and is eliminated predominantly via the kidneys and its urinary elimination in animals with prolonged infections. Expand
Evidence for adenylyl cyclase-dependent receptors for parathyroid hormone (PTH)-related protein in rabbit kidney glomeruli.
TLDR
Findings suggest that PTHrP could affect glomerular function through changes in glomersular cAMP content by interaction with PTH receptors. Expand
Trypanocidal Activity of Methylene Blue
TLDR
In this study, methylene blue trypanocidal activity was found in vitro but it failed to cure trypanosome infection in mice when administered at 300 mg/kg p.p.o.or at 200mg/kg i.p., respectively. Expand
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