Analogs or derivatives of bephenium (N,N-dimethyl-N-(2-phenoxyethyl)benzenemethanaminium).
An antihelminthic drug that has been tried experimentally in rheumatic disorders where it apparently restores the immune response by increasing macrophage chemotaxis and T-lymphocyte function. Paradoxically, this immune enhancement appears to be beneficial in rheumatoid arthritis where dermatitis, leukopenia, and thrombocytopenia, and nausea and vomiting have been reported as side effects. (From Smith and Reynard, Textbook of Pharmacology, 1991, p435-6)

Methyridine (2-[2-methoxyethyl]-pyridine]) and levamisole activate different ACh receptor subtypes in nematode parasites: a new lead for levamisole-resistance. (1/6)

1. The development of resistance to all chemotherapeutic agents increases and needs to be addressed. We are interested in resistance in parasitic nematodes to the anthelmintic levamisole. During studies on methyridine, we found that it gave us a new insight into pharmacological changes associated with levamisole resistance. Initially, electrophysiological investigation using a two-micropipette current-clamp recording technique revealed that methyridine acts as a cholinergic agonist on nematode muscle receptors (Ascaris suum). Methyridine (>30 microm) produced reversible concentration-dependent depolarizations and increases in input conductance. Mecamylamine (30 microm) and paraherquamide (0.3 microm) produced reversible antagonism of the depolarization and conductance responses to methyridine. These observations suggest that methyridine, like acetylcholine and levamisole, gates ion channels on the muscle of parasitic nematodes. 2. The antagonistic effects of dihydro-beta-erythroidine and paraherquamide on methyridine-induced contractions of A. suum muscle flaps were then examined to determine if methyridine showed subtype selectivity for N-subtype (nicotine-sensitive) or L-subtype (levamisole-sensitive) acetylcholine receptors. Dihydro-beta-erythroidine weakly antagonized the effects of methyridine (but had no effect on levamisole responses). The antagonism of methyridine (pA2, 5.9) and nicotine (pA2, 6.1) by paraherquamide was similar, but was less than the antagonism of levamisole (pA2, 7.0). The antagonist profiles suggested that methyridine has a selective action on the N-subtype rather than on the L-subtype. 3. A novel use for a larval inhibition migration assay was made using L3 larvae of Oesophagostomum dentatum. Inhibitory effects of nicotine, levamisole, pyrantel and methyridine on the migration of larvae of levamisole-sensitive (SENS) and levamisole-resistant (LEV-R) isolates were tested at different concentrations. Levamisole and pyrantel (putative L-subtype-selective agonists) concentration-response plots were displaced to the right in LEV-R isolates. Nicotine (an N-subtype-selective agonist) and methyridine produced little shift in concentration-response plots in the LEV-R isolates. Resistance dose ratios were used to calculate the relative selectivity, rhoL, for the L-type receptor (levamisole rhoL=1.0; pyrantel rhoL=0.93; methyridine rhoL=0.17; nicotine rhoL=0.06). These observations reveal an N-subtype-selective action of methyridine and suggest that levamisole resistance may be associated with a loss of the L-subtype, but not the N-subtype receptors. The pharmacology of methyridine suggests an approach for the treatment of levamisole-resistant parasites.  (+info)

Pharmacology of N-, L-, and B-subtypes of nematode nAChR resolved at the single-channel level in Ascaris suum. (2/6)

Pharmacological experiments on Ascaris suum have demonstrated the presence of three (N-, L-, and B-) subtypes of cholinergic receptor mediating contraction of body wall muscle in parasitic nematodes. In the present study, these ionotropic acetylcholine (ACh) receptors (nAChRs) were activated by levamisole and bephenium under patch-clamp conditions and competitively antagonized by paraherquamide and 2-desoxoparaherquamide. A number of recordings exhibited three separate current amplitude levels, indicating the presence of small, intermediate, and large conductance subtypes of receptor. The mean conductance of the small conductance subtype, G25, was 22 +/- 1 pS; the intermediate conductance channel, G35, was 33 +/- 1 pS; and the large conductance channel, G45, was 45 +/- 1 pS. The small channel was not antagonized significantly by paraherquamide and was identified as the N-subtype. The intermediate channel was preferentially activated by levamisole rather than bephenium and antagonized by paraherquamide: the intermediate channel was identified as the L-subtype. The large conductance channel was preferentially activated by bephenium, antagonized more by 2-desoxoparaherquamde than by paraherquamide and was identified as the B-subtype. These observations reveal that the three channel subtypes have different selectivity for cholinergic anthelmintics. The different selectivity of these compounds should be considered when dealing with drug resistant infections.  (+info)

Phenotypic characterization of two Ancylostoma caninum isolates with different susceptibilities to the anthelmintic pyrantel. (3/6)

 (+info)

Selective effect of the anthelmintic bephenium on Haemonchus contortus levamisole-sensitive acetylcholine receptors. (4/6)

 (+info)

Use of common salt fortified with iron in the control and prevention of anemia--a collaborative study. Report of the Working Group on Fortification of Salt with Iron. (5/6)

The efficacy of salt fortified with iron (FePO4 and NaHSO4) to control anemia was investigated by large scale field trials in three rural areas and one urban area located in different parts of India, each covering a total population of 4000 to 6000. Hb levels were determined before the introduction of the fortified salt and at six monthly intervals thereafter. Iron-fortified salt was acceptable to the population and its consumption for a period of 12 to 18 months was without any untoward effects. At the end of 12 to 18 months of consumption of iron-fortified salt, a significant improvement in the Hb-levels and a significant reduction in the incidence of anemia was observed in all the test areas. In one of the rural areas tested, there was a high incidence of hookworm infestation and iron-fortified salt showed a significant impact on Hb levels even in this area. Deworming concomitant with distribution of iron-fortified salt was shown to have only a marginal additional benefit.  (+info)

The interaction between anthelmintic drugs and histamine in Ascaris suum. (6/6)

1 Piperazine reduced the histamine content of Ascaris suum, yet it greatly increased the uptake of histamine from the surrounding medium, the neuromuscular structures of the nematode preferentially increasing in amount. 2 Bephenium reduced the histamine content of Ascaris and the uptake of histamine from the surrounding medium. However, the relative amount in the neuromuscular structures increased. 3 The flaccid paralysing action of piperazine may thus involve increased histamine absorption whereas the spastic paralysing action of bephenium may be independent of histamine.  (+info)

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Abstract Pyrantel pamoate was administered orally as a single dose in a suspension or chewable tablet to 379 patients with helminth infections. Single doses of oral suspension were administered for 3 consecutive days to 89 patients. A modified Stoll technique and Richie's concentration method were performed twice before treatment and at 10 and 30 days after treatment. In a single dose of about 5 mg per pound of body weight (base activity) the cure rate for ascariasis was 96.7%; the reduction of the egg count in one case not completely cured was 98%. Significant activity was also observed against Necator americanus; however, at the dosages employed, it was not superior to other agents currently in use. No significant activity was noted against Trichuris trichiura. Clinical observation showed that both formulations were well tolerated by the patients. No significant changes attributable to therapy were observed in determinations of hematopoetic, liver, or renal function.
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Pyrantel pamoate, along with all other kinds of de-worming medications, can flush the worms out of the intestines, and the worms exit the body during defecation. It works by making the worm relax its grip on the intestinal wall, allowing it to pass with the stool. It is important to note that Pyrantel only affects worms in the intestine, and does nothing to remove worms encysted in other parts of the cats body, so multiple treatments with Pyrantel are necessary to give the encysted worms time to migrate back to the intestine to be removed. Follow-up de-worming treatments should be given approximately two weeks after the initial treatment. Roundworms are a disgusting and uncomfortable parasite that, while not usually fatally dangerous in cats, can cause serious problems in kittens. Make sure not to forget follow-up treatments, because an infection can spring back very easily from encysted larvae. ...
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Our results demonstrate that the mechanism of action of tribendimidine against nematodes is the same as levamisole and pyrantel, namely, tribendimidine is an L-subtype nAChR agonist. Thus, tribendimidine may not be a viable anthelmintic where resistance to levamisole or pyrantel already exists but c …
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1960). "The Comparative Efficacy of Bephenium Hydroxynaphthoate and Tetrachloroethylene against Hookworm and other Parasites of ... "Compound Summary: Tetrachloroethylene". PubChem. Retrieved 9 September 2020. M. Rossberg et al. "Chlorinated Hydrocarbons" in ...
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  • The cation in this salt is called benzylammonium and is a moiety found in pharmaceuticals such as the anthelmintic agent bephenium hydroxynaphthoate, used in treating ascariasis. (wikipedia.org)
  • Tetrachlorethylene, introduced in for the treatment of hookworms of man and anthelmintic drugs for, is still used for the so-called American hookworm Necator americanus of man but was superseded by bephenium hydroxynaphthoate for the treatment of the European hookworm Ancylostoma duodenale of man and by disophenol for the treatment of canine hookworm Ancylostoma caninum. (wwwladys.ro)
  • Bephenium hydroxynaphthoate at 25 mg/kg and Disophenol at 3 mg/kg were found to be effective only in 79.1 to 92.2 %, 88.1 to 100%, 84.6 to 95.3 %, 85.9 to 100% and 68.3 to 84 % cases respectively. (elephantcare.org)
  • Analogs or derivatives of bephenium (N,N-dimethyl-N-(2-phenoxyethyl)benzenemethanaminium). (bvsalud.org)
  • Benzylamine is an organic chemical compound with the condensed structural formula C6H5CH2NH2 (sometimes abbreviated as PhCH2NH2 or BnNH2). (wikipedia.org)
  • DEC is a synthetic organic compound which is highly specific for several parasites and does not contain any toxic metallic elements. (meddic.jp)
  • It is the organic compound 1-adamantylamine or 1-aminoadamantane , meaning it consists of an adamantane backbone that has an amino group substituted at one of the four methyne positions. (hitchhikersgui.de)
  • Apart from medical uses, this compound is useful as a building block in organic synthesis, allowing the insertion of an adamantyl group . (hitchhikersgui.de)
  • It is a potent metabolite of bupropion , the compound in GlaxoSmithKline's Wellbutrin . (rug.nl)
  • Nitazoxanide (NTZ) is a main compound of a class of broad-spectrum anti-parasitic compounds named thiazolides. (readtiger.com)
  • Chemical Name: Enalapril maleate Molecular Formula: C24H32N2O9 Formula Weight: 492.52 CAS No.: 76095-16-4 2-Chloro-N,N-dimethylethylamine hydrochloride (DMC) is used as intermediate for the synthesis of pharmaceuticals (e.g. bephenium. (pharmachemm.com)
  • Benzylammonium Compounds" is a descriptor in the National Library of Medicine's controlled vocabulary thesaurus, MeSH (Medical Subject Headings) . (harvard.edu)
  • This graph shows the total number of publications written about "Benzylammonium Compounds" by people in Harvard Catalyst Profiles by year, and whether "Benzylammonium Compounds" was a major or minor topic of these publication. (harvard.edu)
  • L-Alpha glycerylphosphorylcholine ( alpha-GPC , choline alfoscerate ) is a natural choline compound found in the brain. (kiwix.org)
  • Isoquinolines are a class of compounds (benzopyridines) which are used in medical contexts (such as the anesthetic dimethisoquin, the antihypertensive debrisoquine, and the vasodilator papaverine) and in other areas (such as disinfectant N-laurylisoquinolinium bromide). (wikipedia.org)
  • Below are the most recent publications written about "Benzylammonium Compounds" by people in Profiles. (harvard.edu)