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At least 19 recordsLinked to original sources
PubMed1978

[Effect of L-tetramisol associated with rifampicin in patients with lepromatous leprosy. L-tetramisol in patients with lepromatous leprosy].

In this work are presented results obtained in the treament of thirty patients suffering of lepromatous leprosy. In a group of fifteen patients L-tetramisol was administrated in association to antimocrobian drugs. The control group received only the last medication. Immunological modifications were not observed in any case. However, in six patients treated with L-tetramisol associated to rifampicin during three months it was possible to observe a notable improvement of the clinical state. In the patients that received L-tetramisol associated to other drugs or in those that received only antimicrobian drugs the clinical improvement was very low or null.

Adolescent↗
PubMed1984

Effect of L- and D-tetramisole on 32Pi and 45Ca uptake and mineralization by matrix vesicle-enriched fractions from chicken epiphyseal cartilage.

Alkaline phosphatase has been implicated in matrix vesicle-mediated calcification. We sought to clarify its role in this process by studying the effect of L-tetramisole, a strong uncompetitive inhibitor of this enzyme, and D-tetramisole, its inactive isomer, on the uptake of 32Pi and 45Ca by matrix vesicle-enriched microsomes obtained from chicken epiphyseal cartilage. Uptake of both 32Pi and 45Ca was inhibited in a dosage-dependent manner by the L-isomer; however, 32Pi uptake was selectively inhibited at low drug concentrations and at early time periods. With increasing incubation time, inhibition of uptake of both ions was lost. Apatite crystal growth was only weakly inhibited by both the D- and L-isomers of tetramisole. The kinetics of ion uptake by the vesicles was complex. 45Ca/32Pi uptake ratios, taken with the selective inhibiton of 32Pi uptake by L-tetramisole, indicated that early phases of vesicle ion uptake might be governed by alkaline phosphatase, a known Pi-binding protein. Later stages were clearly controlled by apatite formation. Although inhibition of vesicle uptake of 32Pi and 45Ca by graded levels of L-tetramisole paralleled inhibition of alkaline phosphatase activity, surprisingly, D-tetramisole was almost as inhibitory of ion uptake as the L-isomer. This finding, coupled with the fact that alkaline phosphatase substrates were not required for vesicle ion uptake, indicates that alkaline phosphatase hydrolase activity is not directly involved in vesicle-mediated calcification under these experimental conditions.

Alkaline Phosphatase↗
PubMed1999

Comparative anthelmintic activity of strategic sustained low-level administration of albendazole in feed pellets compared to single doses of closantel and tetramisole against natural ovine parasitic gastroenteritis.

The strategic use of single therapeutic doses of closantel, tetramisole or sustained low-level administration of albendazole in feed pellets in controlling naturally acquired parasitic gastroenteritis in sheep was investigated on a farm in semi-arid Rajasthan, India. A total of 303 5- to 6-month-old sheep were divided into three groups. Two groups were dosed with single therapeutic doses of closantel and tetramisole and the third group was given a low-level medication with albendazole through feed pellets for 30 days. Faecal egg counts revealed significantly lower counts (p<0.001) in the group treated with closantel compared to the other two groups. The faecal egg counts in the group receiving sustained low-level albendazole rose after withdrawal of the medication but remained significantly lower than those in the group treated with tetramisole up to 7 weeks after treatment (p<0.05). On the other hand, in the group treated with tetramisole, the mean faecal egg count rose from 3 weeks after treatment and remained continuously higher than those in any other group up to 12 weeks after treatment. The closantel-treated group gained more body weight but the first six-monthly greasy fleece yield was greater in the group treated with medicated pellets. During the first 3 months of the experiment, three animals in the group treated with tetramisole died of parasitic gastroenteritis. Following sustained low-level administration of albendazole in feed pellets, the plasma disposition curve of both the sulphoxide and sulphone metabolites reached its plateau level by day 5 and remained almost constant thereafter. The comparative cost-effectiveness of the three treatment regimes during the first 3 months of treatment was best for the group treated with closantel followed by the group treated with medicated feed pellets.

Administration, Oral↗
PubMed1973

Stimulation of anti-Brucella vaccination in mice by tetramisole, a phenyl-imidothiazole salt.

The effect of tetramisole (hydrochloride of racemic 2, 3, 5, 6,-tetrahydro-6-phenyl-imidazo [2, 1-b] thiazole) on immunization was investigated in mice vaccinated by killed Brucella melitensis cells suspended in incomplete adjuvant. Immunity to Brucella abortus challenge was estimated by the reduction in number of B. abortus colonies per gram of spleen in those mice which escaped full immunization and also by calculation of mean infective doses for each group of mice. All tetramisole treatments significantly reduced the number of B. abortus live cells in spleen from infected mice. Tetramisole, injected twice (at the time of vaccination and 48 h later), induced a significant 3.5-fold increase of the protection brought about by Brucella vaccine alone. A single injection of 1.25 mg/kg at the time of vaccination resulted also in a significant increase of the immunity given by vaccination. No modifications of the vaccine potency were observed if tetramisole administration preceded vaccination. In such a mouse assay, tetramisole-induced stimulation was not accompanied by specific antibody increases, although measured by three serological tests.

Antibodies, Bacterial↗
PubMedDate not supplied

Effects of levamisole (NSC-177023) and tetramisole (NSC-102063) in experimental tumor systems.

Levamisole and tetramisole had no antitumor effect against the following transplantable syngeneic murine tumors: L1210 leukemia, P388 leukemia, B16 melanoma, Madison 109 lung tumor, and Lewis lung carcinoma. In the Lewis lung carcinoma system there was no effect on primary tumor growth, metastasis, or survival. Tetramisole had a variable effect on the growth of rhabdomyosarcomas and the survival of BALB/c mice following intramuscular inoculation of Moloney sarcoma virus. In two experiments treatment with tetramisole either prior to or following inoculation of Moloney sarcoma virus increased the number of mice with tumor regression as opposed to progressive tumor growth, incrneased the number of long-term survivors, and prolonged the lifespan of mice that died of tumor. In two further tests neither levamisole nor tetramisole had an effect in this system. In mice immunosuppressed with cyclophosphamide prior to virus inoculation, there was not effect of treatment with levamisole or tetramisole.

Animals↗
PubMed1980

Stereospecific inhibition of alkaline phosphatase by L-tetramisole prevents in vitro cartilage calcification.

To clarify the role of alkaline phosphatase (ALP) and ATPase in skeletal mineralization, we studied the effect of the anthelmintic drug, l-tetramisole (levamisole), a stereospecific inhibitor of ALP activity, and its inactive isomer, d-tetramisole (dexamisole), on in vitro calcification of rachitic rat cartilage. ALP activity in homogenized rachitic rat proximal tibiae was inhibited by l-tetramisole in a dose-dependent manner. Histochemical and electron microscopic cytochemical analysis of intact epiphyseal plate rachitic rat cartilage showed that 5 x 10(-2) M and greater concentrations of l-tetramisole (1) virtually abolished ALP activity, (2) moderately reduced ATPase activity, and (3) prevented in vitro cartilage calcification, while preserving the structural integrity of the matrix vesicles. Concentrations of d-tetramisole as high as 1 x 10(-1) M failed to inhibit ALP activity in tibial homogenates by more than 10 per cent and did not alter histochemical staining of enzyme activity or calcification in intact cartilage slices. Heating the cartilage slices destroyed ALP activity, prevented calcification, and disrupted matrix vesicle integrity. These data show that there is a close association between ALP activity and in vitro calcification of rachitic rat cartilage. In the absence of ALP activity, intact matrix vesicles do not promote calcification. Our data also suggest that some ATPase activity of rachitic rat cartilage may be distinct from ALP activity.

Adenosine Triphosphatases↗
PubMed1982

[Toxicity of "Farmakhim" tetramisole in laboratory and farm animals].

Tetramisole produced by ICI, England, and Tetramisole Pharmachim, Bulgaria, were comparatively studied in terms of their acute and subchronic toxicity, and the local and general tolerance and antinematode activity. No differences were found in their acute toxicity (LD50) for albino mice at oral, subcutaneous, and venous application, the index of resorption being 6.3. The same was true so far as the tolerance in calves, sheep, goats, and pigs was concerned. Orally at the rate of 45 mg/kg in sheep and over 30/kg with calves (3, resp., 2 times as high as the therapeutic dose) tetramisole produced nervous and locomotor excitement, tremor, salivation, higher respiration and pulse rate, frequent urination and defecation. Following the tenfold oral administration at intervals, of 3 days at rates of 15 and 45 mg/kg tetramisole Pharmachim did not affect unfavourably the appetite, behaviour, general status, and the clinical and biochemical composition of the blood as well as the structural pattern of the viscera in sheep. Tetramisole Pharmachim was shown to be well tolerated with regard to the conjunctivae at concentrations of up to 5 per cent, the subcutaneous tissues and muscles at conc. of up to 3 per cent, and mucous membranes of the stomach and intestines at conc. of up to 10 per cent.

Animal Diseases↗
PubMed1970

The mechanism of the paralysing action of tetramisole on Ascaris somatic muscle.

1. Tetramisole (100 mug/ml) paralysed live Ascaris in 3 min.2. Tetramisole (10 mug/ml) caused a sustained contraction of the isolated somatic muscles of the worm. This contraction was not blocked by curare nor by piperazine.3. Tetramisole reduced the resting potential of Ascaris muscle from 34+/-4 to 10+/-1 mV.4. Tetramisole caused contraction of Ascaris muscle previously depolarized with high K(+) solutions. This observation suggests that tetramisole can induce a contracture that is independent of membrane depolarization.

Acetylcholine↗
PubMed1991

Influence of L-tetramisole on the interferon production by mouse peritoneal and L929 cells.

The effect of L-tetramisole (Levamisole, Decaris) on the physiological interferon beta (INF beta) production by freshly isolated peritoneal cells of BALB/c, NZB and C3H mouse strains was studied. We have shown that these strains differ in their ability to produce physiological IFN. Peritoneal cells of individual BALB/c and NZB mice differed significantly in ability to produce the physiological IFN, but most of these animals are good producers, while the cells isolated from C3H mice are not. High concentrations of L-tetramisole (250 and 500 micrograms/ml) suppressed IFN synthesis in the cells from BALB/c and NZB mice. Lower concentration of L-tetramisole (125 micrograms/ml) inhibited the IFN production only partially and this effect was observed when the IFN production was high. When the IFN production was very low, L-tetramisole slightly increased the synthesis. L-tetramisole affected the production of the physiological IFN, but not the production of IFN induced by Newcastle disease virus (NDV) in the peritoneal cells of mice or in L929 cells.

Animals↗
PubMed1979

Synthesis and biological evaluation of tetramisole analogues as inhibitors of alkaline phosphatase of the 6-thiopurine-resistant tumor sarcoma 180/TG.

Tetramisole and its analogues are potent inhibitors of alkaline phosphatase, including isoenzymes of Sarcoma 180/TG which appear to be involved in the mechanism of resistance of this neoplastic cell line to the 6-thiopurines. To determine the requirement for the thiazole ring system of tetramisole for inhibitor potency, 2,3,5,6-tetrahydro-6-phenylimidazo[2,1-b]oxazole, 2,3-dihydro-6-phenylimidazo[2,1-b]oxazole, and 2,3,5,6-phenylimidazo[2,1-a]imidazole were synthesized and tested for inhibitory activity against alkaline phosphatase isolated from Sarcoma 180/TG. The results indicate that 2,3,5,6-tetrahydro-6-phenylimidazo[2,1-b]oxazole caused 50% inhibition at 0.21 mM, while the other synthesized compounds were inactive at a concentration of 1 mM; in contrast, tetramisole required only 0.045 mM for 50% inhibition of alkaline phosphatase activity. The findings support the concept that the thiazole ring system of the tetramisole structure is required for maximum inhibitory potency of this series against alkaline phosphatase.

Alkaline Phosphatase↗
PubMed1977

Tetramisole analogues as inhibitors of alkaline phosphatase, an enzyme involved in the resistance of neoplastic cells to 6-thiopurines.

A series of tetramisole derivatives was synthesized and tested for inhibitory activity against alkaline phosphatase which was partially purified from a murine ascitic neoplasm resistant to 6-thiopurines (Sarcoma 180/TG). These agents included derivatives substituted with halogens, CH3, or NO2 groups at either the meta or para position of the phenyl ring of tetramisole and 2,3-dehydrotetramisole. The phenyl ring of tetramisole and 2,3-dehydrotetramisole was also replaced by a naphthyl ring, and the phenyl ring of 2,3-dehydrotetramisole was substituted by a thienyl ring system. The presence of both the thiazolidine and dihydroimidazole rings of tetramisole was found to be essential for enzyme inhibitory activity. Substitution of a naphthyl for the phenyl group and dehydrogenation at the 2,3 position of the thiazolidine ring were found to significantly enhance inhibitory activity for alkaline phosphatase. Tests employing (S)-(-)-6-(4-bromophenyl)-2,3,5,6-tetrahydroimidazo[2,1-b]thiazole oxalate in combination with 6-thioguanine demonstrated that the inhibitor of alkaline phosphatase was capable of increasing the toxicity of 6-thioguanine to Sarcoma 180/TG cells in tissue culture.

Alkaline Phosphatase↗
PubMed1970

[Anthelminthic Effectiveness Of 2,3,5,6-Tetrahydro 6-Phenyl-Imidazole (2,1-B) Thiazole Hydrochloride (=tetramisole) Upon Intestinal Parasites]

A single dose of Tetramisole, 2.5 mg/kg body weight, was given to the infected cases of intestinal parasites. The number of cases were: Ascaris lumbriocides 96, hookworm 16, Trichostrongylus orientalis 10, Trichocephalus trichiurus 114 and Clonorchis sinensis 19. No dietary restriction before and after the administration of Tetramisole was required. 1. In Ascaris infection the egg negative conversion rate and the egg reduction rate were 92.7 per cent and 99.5 per cent, respectively. 2. In Trichostrongylus orientalis infections, 9 out of 10 cases were resulted egg negative after the single dose of Tetramisole, and hookworm, 12 out of 16 administered showed egg negative. However, there were no appreciable effectiveness to the cases of Trichocephalus trichiurus and Clonorchis sinensis. 3. Mild and transient side effects were noted in 75 cases (54.5%) out of 140 cases. The main symptoms were dizziness (25.5%), anorexia (25.5%), abdominal pain (18.6%), diarrhea (16.6%), headache (15.2%), nausea (14.4%) and fever (11.0%). From the above results, it is anticipated that Tetramisole is an effective anthelminthic for elimination of Ascaris, Trichostrongylus and hookworm.

Journal Article↗
PubMed1992

Determination of the partition of the tetramisole derivative (+-)-5,6-dihydro-6-phenyl-2-n-propyl-imidazo[2,1-b]thiazole into liposomal membranes by fluorescence quenching of the membrane probe 8-(2-anthryl)-octanoic acid.

Fluorescence quenching has been used to study the partition of the tetramisole derivative (+-)-5,6-dihydro-6-phenyl-2-n-propyl-imidazo[2,1-b]thiazole into liposomes, consisting of a mixture of egg L-alpha-phosphatidylcholine, egg phosphatidylethanolamine and dipalmitoylphosphatidic acid (2:1:0.06 w/w/w). The tetramisole derivative quenched the fluorescence of the intramembrane probe 8-(2-anthryl)-octanoic acid. The quenching process could be rationalized by a model for dynamic quenching in which an intermediate excited-state non-emitting complex (PQ)* between neutral quencher (Q) and excited probe (P*) is involved: [sequence: see text] where kd, k-d and ki represent the rate constants of complex formation, dissociation and deactivation, respectively. The subscripts A and L denote the aqueous and lipid phases, and the asterisk indicates the excited state. Linear Stern-Volmer plots were obtained from quenching experiments of fluorescence intensities and fluorescence life-times. The slopes of the plots were dependent on the lipid volume fraction of the liposomes. Measurement of the reciprocal of the apparent bimolecular quenching rate constant at various lipid volume fractions yielded the partition coefficient Kp and the overall quenching rate constant kq[kq = kdki/(ki+k-d)] of the tetramisole derivative. The steady-state measurements were performed at three different pH-values. Time-correlated single photon counting measurements revealed a single-exponential fluorescence decay for 8-(2-anthryl)-octanoic acid in the presence and absence of quencher. The quenching results were in accordance with the model that only the neutral form is capable of partitioning into the lipid phase. Combined average values of 318 and 6.59 x 10(8) M-1s-1 were calculated for the partition coefficient and the bimolecular quenching rate constant, respectively, from the steady-state and time-resolved quenching experiments.

Anthracenes↗
PubMed1992

Treatment of Nippostrongylus brasiliensis in normal and SPF rats using tetramisole loaded into zeolite.

Administration to rats of tetramisole loaded into zeolite was more successful in killing adults of Nippostrongylus brasiliensis than the administration of tetramisole alone. The most successful treatment occurred in SPF (Specific Pathogen Free) rats dosed with tetramisole loaded into zeolite and no worms were present in this group at autopsy eight days post-infection. It is concluded that the slow release of drug from the zeolite matrix improved its efficacy, especially in removing worms from low-grade infections.

Aluminum Silicates↗
PubMed1976

[Tetramisol, piperazine, and metrifonate treatment of experimental invasion by Ascaridia galli in chickens of differents ages].

The authors studied the anthelminthic effectiveness of a single peroral application of tetramisol (40 mg per 1 kg 1. w.), piperazine (500 mg per 1 kg 1. w.) and metriphonate (50 mg per 1 kg 1.w.) in the artificial invasion by Ascaridia galli. A set of 118 chickens of the White Leghorn breed were subjected to a single invasion by 3000 or 1500 invasive eggs at the age of 6, 36, and 48 days. The inteseffectiveness and extenseffectiveness of the treatment with the tested preparations were examined on the fifteenth day after invasion; the examination was based on the findings of ascarids in the helminthological dissection performed 48 hours on the findings of ascarids in the melminthological dissection performed 48 hours after therapy. The numbers of ascarids in the tested animals were compared with those in the controls. A histological examination was carried out to study the tissue reaction in the intestine, liver, spleen, kidneys, heart, and brain. Tetramisol showed the highest effectiveness. The intenseffectiveness of this substance reached 89-100% in young as well as older chickens. Piperazine had a good effectiveness in older chickens (61-83%); in young chickens it was entirely ineffective. The intenseffectiveness percentage of metriphonate was almost at a zero level. The extenseffectiveness of tetramisol ranged between 20 and 100% (the low values are characteristic of a severe course of invasion). Piperazine showed an extenseffectiveness ranging from 17 to 67% only in older chickens in cases of a mild invasion; otherwise it was equal to zero. Metriphonate was entirely ineffective. The reflection of ascaridiasis in the tissue reaction of the host manifested itself as granulomatous changes in intestinal mucous membrane, as multiplied histiocytic elements and plasma cells, and inflammatory lymphocytic infiltrates in the liver parenchyma.

Age Factors↗
PubMed1977

Differential effects of the isomers of tetramisole on adrenergic neurotransmission in cutaneous veins of dog.

Clinical observations indicate that dexamisole and levamisole, the isomers of tetramisole, cause mood elevation. Their effects on smooth muscle cells and adrenergic nerves were investigated in strips of dogs' saphenous veins. Dexamisole (2.5 X 10(-6) to 4 X 10(-5) M) augmented the contractile response to norepinephrine but depressed that to tyramine; cocaine inhibited the augmentation of the norepinephrine response. Levamisole (10(-5) M) did not alter the response to norepinephrine, but augmented that to tyramine. At 1.6 X 10(-4) M dexamisole, more than levamisole, depressed the responses to norepinephrine, tyramine and acetylcholine. Activation by K+ ions was not affected by the isomers. Preparations, incubated with 3H-norepinephrine, were mounted for superfusion, tension recording and determination of 3H-norepinephrine and metabolites in the superfusate. Dexamisole and levamisole augmented the 3H-norepinephrine overflow during nerve stimulation; levamisole decreased the efflux of deaminated metabolites. During tyramine-induced contractions, dexamisole depressed and levamisole augmented the efflux of 3H-norepinephrine; they reduced the appearance of metabolites. The increases in 3H-norepinephrine caused by the isomers during nerve stimulation were not seen after phenoxybenzamine. Dexamisole, more than levamisole, inhibited tissular uptake of 3H-norepinephrine. Levamisole, more than dexamisole, inhibited monoamine oxidase activity in vein homogenates. These interferences with release and disposition of norepinephrine may be related to the antidepressant properties of the tetramisole isomers.

Acetylcholine↗