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Biomedical subjects

P Coudert

Publications and source records attributed to P Coudert.

At least 37 records · Page 2Linked to original sources
PubMed1997

Vaccination against Eimeria magna coccidiosis using spray dispersion of precocious line oocysts in the nest box.

Coccidiosis mostly affects young rabbits just after weaning (5- to 6-week-old animals). Prevention of this disease must therefore be initiated before weaning. 'Precocious lines', derived from field species display good immunogenicity, though not pathogenic when administered at the right dose. In the present work, we tested the vaccination method of the whole litter at 25 days of age by spray dispersion of oocysts of a precocious line of Eimeria magna in the nest box. Three doses were tested, d1 = 4 x 10(2) oocysts, d2 = 4 x 10(3) oocysts, d3 = 4 x 10(4) oocysts. The animals were challenged individually with 10(4) oocysts of a wild strain of E. magna at 35 days of age, 5 days after weaning. The oocyst output and weight gain were recorded after vaccination and after challenge. The vaccinated animals did not display any vaccine reaction. The dose d3 was totally effective on oocyst output and on weight gain under our experimental conditions. As our challenge conditions were severe, we think that a lower vaccine dose could be used. This method proved to be efficient, and quick and easy to use because it did not require animal manipulation.

Animals↗
PubMed1997

Pharmacophore requirements in new series of pyridazinyl alkanoic acids, N-[(pyridazin-2-yl) alkyl] succinyl and glutaryl amides, inhibitors of thromboxane A2 biosynthesis.

New series of 5-benzyl-6-methyl-4-oxo pyridazin-2-yl alkanoic acids, N-[(pyridazin-2-yl)alkyl] succinyl and glutaryl amides have been synthesized and evaluated in vitro as TXA2 biosynthesis inhibitors. The experiments were carried out using arachidonic acid (32.8 microM) as a substrate and horse platelet microsomes as sources of TXA2 synthase. The presence of TXB2, a stable metabolite of TXA2, was determined by RIA. The potency of active compounds (1.10(-4) < IC 50 < 1.10(-6) M) greatly depends on the length of the chain at the N-2 position on the pyridazine ring. Furthermore, enzyme inhibition in vitro is increased with the presence of a halogen atom on the aromatic moiety of the benzyl group at C-5. Compound 4f having a pentanoic side chain and a 4-fluoro benzyl moiety was the most active derivative with an IC50 value of 6.69 x 10(-6) M. Molecular modelling studies were done on all the synthesized pyridazinones and on prostaglandin H2 (PGH2) suggesting spatial features and volumes of TXA2 synthase pharmacophore mode in these series of derivatives.

Amides↗
PubMed1997

Synthesis and analgesic effects of 3-substituted 4,6-diarylpyridazine derivatives of the arylpiperazine class.

A new series of 4,6-diaryl pyridazines substituted in the 3-position by arylpiperazinyl moieties was synthesized and evaluated for analgesic activity. Five out of the nine tested compounds possessed significant antinociceptive effects in the phenylbenzoquinone-induced writhing test (PBQ test) with ED50 values ranging from 26.0 to 37.7 mg/kg ip. The most active derivatives 2a, 2d and 2h had a low toxicity (LD50 > 800 mg/kg ip) but showed some sedative and neurotoxic effects from the dose of 50 mg/kg ip. The three selected pyridazines were devoid of activity in the hot-plate test. However, analgesic activity of 2d and 2h was significantly reversed by naloxone in the PBQ test. Administered at the low dose of 5 mg/kg ip, 2h greatly potentiated the antinociceptive response induced by morphine (0.15 mg/kg sc). In addition, analgesic effects of 2h (2.5 mg/kg ip) were also potentiated by 5-hydroxytryptophan combined with carbidopa. These results suggest that pyridazine 2h induces analgesia, which is mediated via both opioid and serotonergic mechanisms.

Acetaminophen↗
PubMed1997

In utero transmission of Pneumocystis carinii sp. f. oryctolagi.

Although vertical transmission of Pneumocystis in human or animal hosts has often been suspected, no evidence demonstrating this infection route has been furnished until now. This widespread parasite is constantly found in the lungs of rabbits, which spontaneously develop a benign pneumocystosis at weaning. However, the infection source, the method of entry of Pneumocystis organisms into the rabbit and when this mammal is infected, remain to be known. As a few parasites have been microscopically observed and detected by PCR in the lungs of rabbits at birth, in utero Pneumocystis infection has been hypothesized. The presence of Pneumocystis was therefore carefully assessed in 16 pregnant does, their embryos and fetuses by using several detection methods. Pneumocystis was detected by PCR in maternal blood, embryos, amniotic fluid and fetuses. The parasite was also revealed histologically and by immunofluorescence in fetal and maternal lungs and in placentas. The results suggest that vertical transmission of P. carinii sp. f. oryctolagi occurs as early as at the 10th day of pregnancy.

Amniotic Fluid↗
PubMed1997

Effects of two N-arylpiperazinylmethylpyrazolo [1,5-d][1,2,4]triazine derivatives in pain and antidepressant tests in mice.

The antinociceptive and antidepressant effects of two pyrazolotriazine derivatives, 2-phenyl-3,3a-dihydro-4-oxo-5-(4-phenylpiperazin-1-yl) methyl-pyrazolo[1,5-d][1,2,4]-triazine (SM1) and 2-phenyl-3,3a-dihydro-4-oxo-5-[4-(4-fluorophenyl)piperazin-1-yl] methylpyrazolo[1,5-d][1,2,4] triazine (SM3) have been investigated in mice using classical pharmacological tests. The intraperitoneal LD50 values of SM1 and SM3 were 253.4 and 218.8 mg kg-1 respectively. SM1 and SM3 showed analgesic properties in the phenylbenzoquinone-induced abdominal constriction test (ED50 approximately 10-15 mg kg-1, i.p.) and in the hot-plate test. The antinociceptive effects of the triazines were significantly reduced by administration of naloxone (1 and 3.2 mg kg-1, s.c.) and yohimbine (1 mg kg-1, p.o.). Acute intraperitoneal administration of both compounds (1 mg kg-1 SM1 or 1.5 mg kg-1 SM3) potentiated morphine (0.15 mg kg-1, s.c.) analgesia in the phenylbenzoquinone test. Although this synergistic activity was not reversed by methysergide (0.5 mg kg-1, i.p.), the analgesic activity of both compounds was enhanced by administration of 5-hydroxytryptophan (50 mg kg-1, i.p.) in conjunction with carbidopa (25 mg kg-1, i.p.). Furthermore, neither compound (at 100 mg kg-1, i.p.) significantly reduced the duration of immobility of mice in the forced swimming test, and both (at 75 mg kg-1, i.p.) were ineffective at enhancing the toxic effects of yohimbine (30 mg kg-1, s.c.). Only SM3 (ED50 = 74.5 mg kg-1, i.p.) significantly antagonized reserpine (2.5 mg kg-1, i.p.)-induced ptosis. Thus, the results suggest that SM1 and SM3 have antinociceptive properties related to co-involvement of opioidergic and alpha 2-adrenoceptor mechanism without associated antidepressant properties.

Adrenergic alpha-Antagonists↗
PubMed1997

Natural transmission of Pneumocystis carinii in nonimmunosuppressed animals: early contagiousness of experimentally infected rabbits (Oryctolagus cuniculus).

Airborne transmission of Pneumocystis carinii has been established, but the infective form and the sources of infection remain unknown. Animal models for studies of P. carinii have previously been limited to immunosuppressed rodents; however, this study was performed with nonimmunodepressed P. carinii-free rabbits. This study was aimed at determining (i) the delay between inoculation of animals (day zero [D0]) and the onset of contagiousness and (ii) the end of contagiousness of these animals (donors). Five-week-old rabbits were used as contact animals and were housed with the donors. The cohabitation periods were for 4 or 5 days from D0 to D4, D4 to D8, D8 to D13, D13 to D18, and D18 to D22. The highest parasite burdens were observed in contact animals housed with donors from D8 to D13 or D13 to D18. This period (8th to 18th day following the day of inoculation of donors) might correspond to the highest phase of contagiousness of donors.

Animals↗
PubMed1997

Synthesis and pharmacological evaluation in mice of new non-classical antinociceptive agents, 5-(4-arylpiperazin-1-yl)-4-benzyl-1,2-oxazin-6-ones.

Several 5-(4-arylpiperazin-1-yl)-4-benzyl-1,2-oxazin-6-ones have been synthesized and tested for analgesic activity in a visceral pain model (phenylbenzoquinone-induced writhing test = PBQ test). A good correlation has been found between the antinociceptive effects of drugs and both their lipophilic and steric properties. The most active derivatives 5c and 5f, with intraperitoneal ED50 values of 10.5 and 10.3 mg kg-1 respectively, were more extensively investigated by evaluating their analgesic activity in a somatosensory pain model (hot plate test), as well as their sedative properties. Furthermore, naloxone suppressed the effect of 5c and 5f in the PBQ test, though these derivatives were ineffective to potentiate morphine analgesia. Pretreatment with yohimbine did not significantly attenuate the analgesic effects of 5c and 5f. In addition, pretreatment with 5-hydroxytryptophan associated with carbidopa also failed to potentiate the antinociceptive effects of 5c and 5f. So, a part of the analgesic activity of 5c and 5f seems to be related to an opioidergic mechanisms, especially at the mu receptor level. Molecular modeling studies performed on the opiate drug morphine and on the most stable conformer of 5f showed structural similarities between these two molecules.

Analgesics↗
PubMed1996

Eimeria magna Pérard, 1925: study of the endogenous development of parental and precocious strains.

The endogenous development of a parental strain of E. magna and its deriving precocious line was studied after inoculation of coccidia-free rabbits with oocysts or sporocysts directly into the duodenum and using electron microscopy. Four meront generations could be observed mainly in the jejunum and ileum for the parent strain. The first merogony began 24 h post-inoculation (h p.i.). and meronts were matured about 48 h p.i. The second and the third generation were complete at 66 and 84 h p.i. respectively. Thus, each generation needs approximately 16-20 h for maturation. The fourth generation appeared 102 h p.i. and the young gamonts were present 120 h p.i. As in the other rabbit Eimeria, two types of meronts were described: A and B. The morphology of all endogenous stages of the precocious line was similar but refractile bodies were absent in the first generation merozoites and the fourth generation meront was lacking.

Animals↗
PubMed1996

Eimeria coecicola Cheissin 1947: endogenous development in gut-associated lymphoid tissue.

Coccidia-free rabbits were inoculated with different doses of a pure strain of Eimeria coecicola and samples of gut were taken at 80, 96, 112, 128, 144, and 160 h postinoculation. The use of a very low infective dose (2-20 oocysts) was sufficient to study the last merogony. The number of merozoites in meronts increased when the infective dose decreased. Only the first merogony of this coccidium in lymphocytes or M-cells of gut-associated lymphoid tissue (GALT) has previously been described. Three other generations of meronts are described herein. All these endogenous stages were observed in the epithelium of the vermiform appendix, sacculus rotundus, and Peyer's patches, especially at the bases of the domes. However, in heavily infected tissues the gamonts were seen throughout the epithelium of the GALT. The third- and fourth-generation meronts were of two types. As in other eimerian species of the rabbit, type A meronts produced thick polynucleated merozoites, whereas type B meronts gave rise to large numbers of thin merozoites with one nucleus. Microgamonts were polynucleated and less numerous than macrogamonts. Type A meronts were also polynucleated and less numerous at the end of the merogony. Therefore, types A and B could correspond to a sexual phenotype differentiation occuring during the two asexual phases of multiplication.

Animals↗
PubMed1996

Validation of random amplified polymorphic DNA assays by ribotyping as tools for epidemiological surveys of Pasteurella from animals.

Two collections of strains of Pasteurella were studied for epidemiological purposes by ribotyping and random amplified polymorphic DNA (RAPD) assays. These strains were isolated through two different structures of animal productions: cattle and rabbit. Forty strains of P. haemolytica from cattle reared in independent breeding-herds belonged to only 3 ribotypes after digestion with HindIII and PvuII. No further discrimination of these strains was obtained by RAPD assays. All these 40 strains showed more than 90% of similarity. This result was consistent with the hypothesis of a clonal dissemination of these strains in bovine herds, possible favoured by the large use of antibiotics. Forty-one strains of P. multocida were isolated in rabbits flocks belonging to 16 breeders. Six of these were linked by commercial relationships. Twenty-eight out of the 29 strains isolated through this commercial network belonged to only three ribotypes whereas the 12 strains from independant breeders belonged to 9 ribotypes. Results of RAPD assays were in accordance with those of ribotyping and validate the use of RAPD assays for epidemiological studies of Pasteurella strains.

Animals↗
PubMed1996

Effect on free radical processes of some ascorbic acid analogues.

Ascorbic acid, present in plasma from humans at concentrations of 50 to 200 mumol/l, has multiple antioxidant properties. Structural modification of this vitamin by the introduction of lipophilic moieties has allowed to the development of ascorbate esters and ethers active as free radical quenchers. Thus, a new series of ascorbic acid analogues possessing one or two aromatic rings was prepared in an attempt to synthesize potent antioxidants with lipophilic properties. Substituted 3-hydroxy furan-2 (5H)-ones and in some cases, dihydrofuro[3,4-b]pyrones were prepared. The synthesized compounds were evaluated for their antioxidant activity in vitro. So, 4-(4-methoxybenzoyl)-3-hydroxy-5-phenylfuran-2(5H)-one 3e (IC50 = 3.06 x 10(-4) M) was found to be the most effective in scavenging the superoxide anion, whereas 4-benzoyl-3-hydroxy-5-(3,4-dimethoxyphenyl)furan- 2(5H)-one 3d (IC50 = 1.38 x 10(-4) M) was the most active in inhibiting, lipid peroxidation.

Animals↗
PubMed1996

Synthesis and trazodone-like analgesic activity of 4-phenyl-6-aryl-2-[3-(4-arylpiperazin-1-yl)propyl]pyridazin -3-ones.

A series of 4,6-diaryl pyridazinones, chemically related to trazodone, ws synthesized and evaluated for analgesic activity. With ED50 values ranging from 8.4 to 46.7 mg kg(-1) i.p. in the phenylbenzoquinone-induced writhing test (PBQ test), most compounds were several times more potent than acetaminophen (ED50 = 231.3 mg kg(-1) i.p.) and noramidopyrine (ED50 = 68.5 mg kg(-1) i.p.). A multiple linear regression analysis demonstrated a correlation between antinociceptive activity and lipophilicity, as well as electronic and steric factors. The most active pyridazinones 2c and 2j exhibited minimal sedative and neurotoxic effects at the dose of 25 mg kg(-1) i.p. They were devoid of activity in the hot plate test and their analgesic activity was not significantly reversed by naloxone in the PBQ test. The antinociceptive response induced by morphine (0.15 mg kg(-1) s.c.) in the PBQ test was greatly potentiated by 2c and 2j administered at the low doses of 1 and 2.5 mg kg(-1) i.p., respectively. On the other hand, their analgesic effects were enhanced synergistically by 5-hydroxytryptophan combined with carbidopa. All these data imply that a significant part of the antinociceptive effect induced by 2c and 2j may involve both opioid and serotonergic pathways. In addition, these two pyridazinones did not exhibit any antidepressant properties in the forced swimming test, nor did they potentiate yohimbine-induced toxicity.

5-Hydroxytryptophan↗
PubMed1996

Eimeria media Kessel 1929: comparative study of endogenous development between precocious and parental strains.

Endogenous development of a pure strain of Eimeria media and of a precocious line derived from this strain was studied in specific pathogen-free (SPF) rabbits. Endogenous development of the parental strain comprised three generations and the gamogony began 76 h post-inoculation (pi). Two types of meronts were observed in each generation. The type A meronts gave rise to large, polynucleated merozoites present in low numbers. Multiplication was carried out by endomerogony. Within type B meronts, merozoites arose from ectomerogony. These were slender and more numerous than those of type A. The sporozoite refractile body was divided and distributed into the first and second generation merozoites but not into the third. The endogenous development of the precocious line was similar to that of the parental strain except that no refractile body was observed and the last merogony was absent. Gamogony appeared 60 h pi.

Animals↗
PubMed1996

Synthesis of peripherally acting analgesic 3-arylpiperazinyl-5-benzyl-pyridazines.

A series of 3-arylpiperazinyl-5-benzyl-pyridazines was synthesized and evaluated for analgesic activity. The structures of these new pyridazine derivatives were confirmed by IR, 1H-NMR spectra and by elementary analysis. With ED50 values ranging from 6.0 to 71.5 mg/kg i.p. most of the compounds were several times more potent than acetaminophen (ED50 = 228.6 mg/kg i.p.) and noramidopyrine ((ED50 = 68.8 mg/kg i.p.) in the phenylbenzoquinone-induced writhing test (PBQ-test). Quantitative structure-activity relationships were accomplished by a Hansch analysis. The most active pyridazines 2h-j exhibited sedative properties from the dose of 25 mg/kg i.p. Their lack of activity in the hot plate test was in favour of peripherally acting agents. In the PBQ test, analgesic activity of 2h-j was antagonized by naloxone. However, their antinociceptive effect added up to those of 5-hydroxytryptophan when given in association with carbidopa. These results demonstrated that analgesic properties of pyridazine derivatives might involve a serotonergic pathway without interaction with opiodergic systems.

5-Hydroxytryptophan↗
PubMed1995

Eimeria magna: pathogenicity, immunogenicity and selection of a precocious line.

A precocious line (PrEmag) of Eimeria magna in rabbits was obtained by selecting for early development of oocysts. The prepatent period was shortened by 46 h. The pathogenicity of PrEmag was substantially reduced and its reproductive potential was much lower (500 times) than that of the parent strain. Rabbits given 2500 oocysts of PrEmag were almost totally protected against a challenge with the parent strain. As in other precocious lines of coccidia from the rabbit, PrEmag showed morphological anomalies of the sporulated oocysts. Each sporocyst harboured one large refractile body instead of the two smaller ones in the parent strain.

Animals↗
PubMed1995

Behavioural profile of two potential antidepressant pyridazine derivatives including arylpiperazinyl moieties in their structure, in mice.

The potential antidepressant effects of two pyridazine derivatives, 5-benzyl 6-methyl 2-[4-(3-trifluoro-methyl phenyl) piperazin-1-yl] methylpyridazin-3-one (PC4) and 5-benzyl 6-methyl 2-[4-(3-chlorophenyl) piperazin-1-yl] methylpyridazin-3-one (PC13), were evaluated using classical psychopharmacological tests in mice. The intraperitoneal LD50 values of PC4 and PC13 were respectively 1125.8 and 429.6 mg kg-1. Only at intraperitoneal doses of 100 mg kg-1 did PC4 or PC13 significantly decrease locomotor activity. Both compounds (5-20 mg kg-1, i.p.) reduced the duration of immobility of mice in the forces swimming test, antagonized reserpine (2.5 mg kg-1, i.p.)-induced ptosis, and potentiated reserpine (2.5 mg kg-1, i.p.)-induced hypothermia. PC4 and PC13 (20 mg kg-1, i.p.) partly reversed hypothermia induced by low dose apomorphine (5 mg kg-1, s.c.) but were less effective for higher doses of apomorphine (16 mg kg-1, s.c.). At 200 mg kg-1, intraperitoneal PC13 enhanced the toxic effects of yohimbine (30 mg kg-1, s.c.), while PC4 was inactive. Head twitches produced either by L-5-hydroxytryptophan (4 mg kg-1, i.p.) in mice pretreated with pargyline (100 mg kg-1, i.p.) or by 1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane (3 mg kg-1, i.p.) were antagonized by both pyridazine derivatives (20 mg kg-1, i.p.). PC4 and PC13 showed analgesic properties in the phenylbenzoquinone-induced abdominal constriction test (5.0 < ED50 < 5.5 mg kg-1, i.p.) and in the hot-plate test (10 to 37% of analgesia at 10 mg kg-1, i.p.).(ABSTRACT TRUNCATED AT 250 WORDS)

5-Hydroxytryptophan↗
PubMed1995

Synthesis of new serotonergic 2-substituted 4,6-diaryl pyridazin-3-ones.

A series of 4,6-diaryl pyridazin-3-ones substituted in the 2-position by [4-(4-aryl piperazin-1-yl]-but-2-ynyl moieties was synthesized and evaluated for antidepressant activity. The structures of these new pyridazine derivatives were confirmed by IR, 1H-NMR spectra and by elementary analysis. At 150 mg/kg i.p., they induced little or no reduction of the duration of immobility of mice in the forced swimming test. Head twitches produced by L-5-hydroxytryptophan in mice pretreated with pargyline were significantly potentiated by most of the tested compounds. In addition, pyridazine derivatives did not antagonize reserpine-induced palpebral ptosis or enhance the toxic effects of yohimbine and were almost devoid of anticholinergic properties in mice.

5-Hydroxytryptophan↗