| macrofilaricidal activity of metabolites of diethylcarbamazine. | the antifilarial compound diethylcarbamazine (n,n-diethyl-4-methyl-2-piperazine, dec) is known rather for its micro- than macrofilaricidal activity. but in some human filariasis i.e. loaiasis, lymphatic filariasis, the spectrum of dec activities extends to adult filaria. the potential role of the metabolites of dec in the action of the parent drug once it had been metabolized in the body of infected animals was investigated. the metabolites were evaluated in a new experimental model on which dec ... | 1989 | 2730692 |
| new antifilarial agents. 1. epoxy sulfonamides and ethynesulfonamides. | two series of 2-substituted 1,2-epoxyethanesulfonamides 2 and ethynesulfonamides 5 were synthesized and evaluated for their antifilarial activity. the trans epoxides 2t were stereospecifically prepared by a darzens reaction between aldehydes and halomethanesulfonamides. the cis isomers 2c were obtained from ethynesulfonamides 5 by semihydrogenation followed by kocl epoxidation. 2-substituted ethynesulfonamides 5 were synthesized from appropriate trans-ethenesulfonamides by a bromination/dehydrob ... | 1987 | 3681893 |
| [dipetalonema dessetae in proechimys oris. ii. evaluation of the model for pharmacologic investigations of antifilarial chemotherapy (author's transl)]. | dipetalonema dessetae in proechimys oris is a new model of rodent feafilariasis with several interesting features with respect to its utilisation in antifilarial pharmacology. 1. in the first part of these studies, it has been shown that the final host of the filaria, a rodent, was easy to breed. a prolific mosquito aedes aegypti was an effective vector, and with the selected mode of infection i.e. 200 infesting larvae subcutaneously injected, 80% of the rodents were infected. 2. from 90 to 150 ... | 1982 | 7200173 |
| study of lymphotropic targeting and macrofilaricidal activity of a melphalan prodrug on the molinema dessetae model. | this study deals with the design of a new macrofilaricidal drug derived from melphalan and having a lymphotropism to avoid the hepatic first pass effect and enhance bioavailability after oral administration. melphalan was linked to a ligand leading to a prodrug called 1,3-dp-melphalan which has structural analogy to triglycerides. the molinema dessetae/proechimys oris model was used for antiparasitic evaluation. melphalan was macrofilaricidal in vitro against molinema dessetae at 1mm, inactive i ... | 1994 | 7830099 |
| macrofilaricidal activity of albendazole-ivermectin combination: histopathological evaluation of adult molinema dessetae. | the macrofilaricidal effect of albendazole in association with ivermectin was assessed in the rodent proechimys oris, infected with molinema dessetae. the drug combination was given to five rodents 190 days after infection. a similar group was used as control. the doses administered were 10 mg per kg for albendazole and 0.04 mg per kg for ivermectin over five days. the histological examination of intra-peritoneal nodules done six weeks after therapy revealed a clear-cut macrofilaricidal effect. ... | 1994 | 7899789 |
| [use of surviving infectious larvae of dipetalonema dessetae in study and research on filaricidal substances]. | dipetalonema dessetae in proechimys oris, the natural final host is a rodent filariasis model used as an in vivo antifilarial screening test. the laboratory vector is aedes aegypti. infective larvae l3 isolated from the intermediate host develop and remain healthy for up to 30 days in a biphasic culture medium composed of a cell feeder layer (l 929) and rpmi 1640 supplemented with foetal calf serum. this culture technique has enabled us to screen antifilarial compounds on a new in vitro test. th ... | 2006 | 3795974 |
| new pudicinae (trichostrongylina, heligmosomoidea) coparasites of proechimys longicaudatus (caviomorpha) from bolivia. i--description of pudica ginsburgi n. sp. and heligmostrongylus chiarae n. sp. | two new pudicinae (trichostrongylina, heligmosomoidea, heligmonellidae) coparasites of proechimys longicaudatus (caviomorph rodent) from bolivia are described: pudica ginsburgi n. sp. is differentiated from all the other species of the genus by the great length of the spicules and of the vestibule and by a different ratio of the length of the spicules on the length of the body. heligmostrongylus chiarae n. sp. has very developed rays 4, strongly divergent from rays 5 as occurs in three other spe ... | 2001 | 11584752 |
| in vitro and in vivo antifilarial activity of ethynesulfonamides, epoxyethanesulfonamides and carboxamide analogues. | a series of 2-substituted trans-1,2-epoxyethanesulfonamides (1t), ethynesulfonamides (2), and their carboxamide analogues 3 (cis and trans) and 4 were evaluated for their antifilarial activity, first in vitro against the infective larvae of the filaria molinema dessetae, then in vivo against the same filaria in proechimys oris, its natural host. on the whole, compounds 2 displayed a high level of activity in vitro, while 4 showed a wider range and 3 were virtually inactive. the modest activity f ... | 1995 | 8595073 |
| activity of albendazole-ivermectin combination and other filaricidal drugs against infective larvae, preadult, microfilariae and adult worms of molinema dessetae in the rodent proechimys oris. | the efficacy of albendazole-ivermectin combination was tested an adult and developing stages of molinema dessetae in the rodent proechimys oris. albendazole and ivermectin, both given alone, suramin and diethylcarbamazine were used as reference compounds. the drug combination (albendazole at 10 mg/kg/ day x 5 days and ivermectin at 0.04 mg/kg/day x 5 days) was effective against infective larvae and preadult worms, and substantially reduced the number of live adult worms. the known filaricidal ag ... | 1994 | 9140472 |
| in vitro and in vivo evaluation of macrofilaricidal activity of gaba and 1,3-dipalmitoyl-2-(4-aminobutyryl)glycerol hcl: a diglyceride prodrug. | a new therapeutic target has been identified from the filaria molinema dessetae: the gabaergic system. gamma-aminobutyric acid (gaba) itself showed antifilarial effect in vitro and a macrofilaricidal action in vivo at high dose by intraperitoneal route (10(-2) m). nevertheless, no action was observed by oral route. the study we report here consists to obtain an antifilarial effect by oral route using a diglyceride prodrug. such a strategy is based on the triglycerides metabolism. a diglyceride p ... | 1992 | 1488452 |
| [a new model for studying filarial physiopathology: molinema dessetae in its definitive natural host proechimys oris]. | | 1987 | 3662335 |
| [a new model for the study of filarial physiopathology: molinema dessetae in its definitive natural host, proechimys oris. 1]. | the filarial rodent model molinema dessetae/proechimys oris, recently adapted in the laboratory allows studies on the host/parasite relationships. development of filarial worm was described elsewhere, and the model standardized. biological, parasitological data and antifilarial drug response were determined. natural models can seldom be used in laboratory; in non natural models many informations on the host-parasite relationships are lost and pathological studies can only be fragmentary and punc ... | 1987 | 3662330 |
| [experimental filariasis in proechimys oris by dipetalonema dessetae. 5. effect of parasitism on metabolism of diethylcarbamazine]. | the metabolism of diethylcarbamazine (dec) in healthy and filaria-infected proechimys oris rodents was investigated. dec and 14c labelled dec were orally administrated (100 mg/kg). the drug was quickly and intensively metabolised. about 90% of the dose administered was eliminated in the urine within 24 hours. monodeethylation was the major pathway. the major urinary metabolites were ethylcarbamazine and its n-oxide. traces of n methylpiperazine 2,5 dione and their n-oxide were also found. elimin ... | 2017 | 3816877 |
| [experimental filariasis in proechimys oris by dipetalonema dessetae: 4. effect of parasitism on protein and tissue binding of diethylcarbamazine]. | several groups of control and filaria-infected rodents were treated by radio-labelled diethylcarbamazine in order to study the effect of parasitism on the protein binding and tissue distribution of the drug. these studies were performed using equilibrium dialysis, chromatography and autoradiography. the plasmatic protein concentrations were lower in the group of infected rodents, due to a decrease of albumin. the binding rate depended on the electrophoretic fractions, but remained low and unaffe ... | 2017 | 3770013 |
| experimental filariasis of dipetalonema dessetae in proechimys oris: 3. effects of parasitism on the pharmacokinetics of diethylcarbamazine. | the pharmacokinetic parameters of diethylcarbamazine were compared in the plasma and peritoneal fluid of 5 non-infected rodents. in the filarial animals, the absorption rate constant and the elimination rate constant were significantly increased. the peak plasma concentration was twofold higher in the infested rodents than the control animals, and this may account for the rapid action of diethylcarbamazine on blood-circulating microfilariae. the area under the curve was unchanged. total clearanc ... | 2017 | 6687054 |
| [demonstration of the antifilarial activity of fosfomycin on the filaria dipetalonema dessetae, bain, in the rodent proechimys oris, thomas]. | | 1981 | 6788392 |
| [intake of microfilariae by the vector for a periodic filarioid, dipetalonema dessetae (author's transl)]. | the filariid d. dessetae in its natural host, proechimys oris, has a daily periodic microfilaraemia with a conspicuous peak during the day (blood from the ocular sinus). --if the mosquitoes engorge during the daily peak, the density of microfilariae ingested is equal or slightly superior to the density of microfilaria in the blood from the ocular sinus. however, if they engorge during the night they ingest 2,5 times the number of microfilariae than the density of microfilariae in the ocular sinu ... | 1981 | 7199270 |