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)

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

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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)

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 ...
Quaternary ammonium compounds, Benzyl compounds, Nicotinic agonists, Salicylates, All stub articles, Antiinfective agent stubs) ... It is formulated as a salt between the active pharmaceutical ingredient, bephenium, and 3-hydroxy-2-naphthoic acid. Bephenium ... Bephenium hydroxynaphthoate (INN, trade names Alcopara, Alcopar, Befenium, Debefenium, Francin, Nemex) is an anthelmintic agent ... ISBN 978-0-85369-840-1. Jayewardene G, Ismail MM, Wijayaratnam Y (July 1960). "Bephenium hydroxynaphthoate in treatment of ...
... bephenium compounds MeSH D02.092.877.096.333 - bretylium compounds MeSH D02.092.877.096.333.150 - bretylium tosylate MeSH ... benzalkonium compounds MeSH D02.675.276.090 - benzethonium MeSH D02.675.276.102 - bephenium compounds MeSH D02.675.276.125 - ... trialkyltin compounds MeSH D02.691.850.900.910 - triethyltin compounds MeSH D02.691.850.900.950 - trimethyltin compounds MeSH ... mustard compounds MeSH D02.455.526.728.468 - mustard gas MeSH D02.455.526.728.650 - nitrogen mustard compounds MeSH D02.455. ...
Isoquinolines are a class of compounds (benzopyridines) which are used in medical contexts (such as the anesthetic ... Hellgren, U.; Ericsson, Ö.; Aden Abdi, Y.; Gustafsson, L. L. (2003). "Bephenium hydroxynaphthoate". Handbook of Drugs for ... Benzylamine is an organic chemical compound with the condensed structural formula C6H5CH2NH2 (sometimes abbreviated as PhCH2NH2 ... cation in this salt is called benzylammonium and is a moiety found in pharmaceuticals such as the anthelmintic agent bephenium ...
Bephenium Compounds - Preferred Concept UI. M0002395. Scope note. Analogs or derivatives of bephenium (N,N-dimethyl-N-(2- ... Analogs or derivatives of bephenium (N,N-dimethyl-N-(2-phenoxyethyl)benzenemethanaminium).. ... Bephenium Derivatives. Compounds, Bephenium. Derivatives, Bephenium. Tree number(s):. D02.092.877.096.166. D02.675.276.102. ...
... these compounds were scopoletin, alfaxalone, bephenium hydroxynaphthoate, apramycin, 4,5-dianilinophthalimide, DL-thiorphan, ... Through connectivity map, we also identified eight compounds that may be used as targeted therapeutic agents for ACBD4 gene in ...
... bephenium compounds MeSH D02.092.877.096.333 - bretylium compounds MeSH D02.092.877.096 ... ... Quaternary Ammonium Compounds. Derivatives of ammonium compounds, NH4+ Y-, in which all four of the hydrogens bonded to ... benzethonium MeSH D02.675.276.102 - bephenium compounds MeSH D02.675.276.125 - betaine MeSH D02.675.276.136 - betalains MeSH ... AMMONIUM COMPOUNDS1. *Quaternary ammonium compounds (such as benzethonium chloride) are particularly harmful to the eyes. ( ...
Underdosing of iron and its compounds. Primarily systemic and hematological agents, NEC (T45). Dextriferron; Ferric [See Also: ... Bephenium hydroxy-naphthoate; Bitoscanate; Chenopodium; Dichlorophen; Diethylcarbamazine; Dithiazanine iodide; Fenbendazole; ... compounds) NEC; Bismuth saltssubcarbonate; Bismuth saltssubsalicylate; Bismuth saltssulfarsphenamine; Carbo me.... ...
Bephenium Compounds / therapeutic use* Actions. * Search in PubMed * Search in MeSH * Add to Search ... Bephenium hydroxynaphthoate (Alcopara). [No authors listed] [No authors listed] Med Lett Drugs Ther. 1968 Jul 26;10(15):60. Med ... Comparison of affects of bephenium hydroxynaphthoate, tetramisole hydrochloride and tetramisole pamoate in the treatment of ... Comparative study of pyrantel pamoate, bephenium hydroxynaphthoate, and tetrachloroethylene in the treatment of Necator ...
Bephenium Compounds Preferred Concept UI. M0002395. Registry Number. 0. Scope Note. Analogs or derivatives of bephenium (N,N- ... Bephenium Compounds Preferred Term Term UI T004615. Date01/01/1999. LexicalTag NON. ThesaurusID NLM (1966). ... BEPHENIUM CPDS. Entry Term(s). Bephenium Derivatives Pharm Action. Antinematodal Agents. Registry Number. 0. Date Established. ... Onium Compounds [D02.675] * Quaternary Ammonium Compounds [D02.675.276] * Ambenonium Chloride [D02.675.276.046] ...
Bephenium Compounds Preferred Concept UI. M0002395. Registry Number. 0. Scope Note. Analogs or derivatives of bephenium (N,N- ... Bephenium Compounds Preferred Term Term UI T004615. Date01/01/1999. LexicalTag NON. ThesaurusID NLM (1966). ... BEPHENIUM CPDS. Entry Term(s). Bephenium Derivatives Pharm Action. Antinematodal Agents. Registry Number. 0. Date Established. ... Onium Compounds [D02.675] * Quaternary Ammonium Compounds [D02.675.276] * Ambenonium Chloride [D02.675.276.046] ...
... benzyl-viologens Beograd Beospir Beospirs Bepadin bepanthen bepask bephenium bephenium compound bephenium compounds bephenium ... azocasein azocene azocine azocines azocoll azocompound azo compound azo-compound azocompounds azo compounds azo-compounds ... atrox batroxobin batroxobins bats batsman batsmen Batson Batsons Batsons compound Batsons compounds Batsons plexus Batsons ... malaria Algiers algin algin acid alginase alginate alginates alginic alginic acid alginic acid compound alginic acid compounds ...
Compounds N0000011356 Benzylisoquinolines N0000179051 benzylpenicilloyl G polylysine N0000166500 Bephenium Compounds ... Compounds N0000007682 Organomercury Compounds N0000007683 Organometallic Compounds N0000007684 Organophosphorus Compounds ... Compounds N0000007804 Organoselenium Compounds N0000008206 Organosilicon Compounds N0000008079 Organotechnetium Compounds ... 1-Ring N0000008260 Heterocyclic Compounds, 2-Ring N0000008096 Heterocyclic Compounds, 3-Ring N0000008258 Heterocyclic Compounds ...
... these compounds were scopoletin, alfaxalone, bephenium hydroxynaphthoate, apramycin, 4,5-dianilinophthalimide, DL-thiorphan, ... Through connectivity map, we also identified eight compounds that may be used as targeted therapeutic agents for ACBD4 gene in ...
ANTI-INFECTIVE AGENTS BEPHENIUM COMPOUNDS ANTI-INFECTIVE AGENTS BETA-DEFENSINS ANTI-INFECTIVE AGENTS BISBENZIMIDE ANTI- ... CHROMOGENIC COMPOUNDS CHROMOGENIC COMPOUNDS CHROMOGENIC COMPOUNDS 6-AMINOCAPROIC ACID COAGULANTS ANTIFIBRINOLYTIC AGENTS ... ANTIPARASITIC AGENTS BEPHENIUM COMPOUNDS ANTIPARASITIC AGENTS BISBENZIMIDE ANTIPARASITIC AGENTS BITHIONOL ANTIPARASITIC AGENTS ... ANTINEMATODAL AGENTS BEPHENIUM COMPOUNDS ANTINEMATODAL AGENTS BISBENZIMIDE ANTINEMATODAL AGENTS CAMBENDAZOLE ANTINEMATODAL ...
Not all compounds are given.. §A parasite-specific enzyme: thiol-dependent reductase.. ¶Reduced ferredoxin appears to be the ... Bephenium§§ Quaternary ammonium. Binds to B-type acetylcholine receptors. Induction of depolarization (spastic paralysis; also ... 2-nitroimidazole nitrofuran compound. Forms nitro-anion radical metabolites (DNA breakage), and produces O2- and H2O2; inhibits ... Compound. Immunomodulatory effects. Amphotericin B. ↑/↓oxidative burst, alters cytokine production (depending on formulation). ...
Product containing benzylisoquinolium compound (product) {766898008 , SNOMED-CT } Product containing bephenium (medicinal ... Quaternary ammonium compound product Current Synonym true false 3672400013 Product containing quaternary ammonium compound ... Product containing quaternary ammonium compound (product) {765420008 , SNOMED-CT } Parent/Child (Relationship Type) Product ... Product containing quaternary ammonium compound (product). Code System Preferred Concept Name. Product containing quaternary ...
  • Analogs or derivatives of bephenium (N,N-dimethyl-N-(2-phenoxyethyl)benzenemethanaminium). (nih.gov)
  • Derivatives of ammonium compounds, NH4+ Y-, in which all four of the hydrogens bonded to nitrogen have been replaced with hydrocarbyl groups. (lookformedical.com)
  • Analogs or derivatives of bephenium (N,N-dimethyl-N-(2-phenoxyethyl)benzenemethanaminium). (bvsalud.org)