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864731-61-3

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864731-61-3 Usage

Description

Fluralaner (INN) is a systemic insecticide and acaricide that is administered orally. The U.S. Food and Drug Administration (FDA) approved it under the trade name Bravecto for flea treatment in dogs in May 2014. The EU approved the drug in February 2014. Australia approved it for the treatment and prevention of ticks and fleas on dogs in January 2015.

Uses

Different sources of media describe the Uses of 864731-61-3 differently. You can refer to the following data:
1. Fluralaner is an insecticide and acaricide used to treat Sarcoptes scabiei var. canis infestation in dogs. Flea treatment. A possible anti-malarial found to kill disease-spreading mosquitoes when they bite treated people.
2. Fluralaner is a novel systemically administered insecticidal and acaricidal compound that provides long-acting efficacy after oral administration to dogs. Fluralaner belongs to a new class of compounds, the isoxazolines. A field study has shown that a single fluralaner dose administered orally to dogs provides at least twelve weeks of flea- and tick-control. The long duration of activity offers a more convenient treatment over monthly flea and tick control treatments with a potential compliance advantage, reducing the risk of vector-transmitted diseases.

Mode of action

Fluralaner inhibits γ-aminobutyric acid (GABA)-gated chloride channels (GABAA receptors) and L-glutamate-gated chloride channels (GluCls). Potency of fluralaner is comparable to fipronil (a related GABA-antagonist insecticide and acaricide).

Pharmacodynamic properties

Fluralaner is an acaricide and insecticide. It is efficacious against ticks (Ixodes spp., Dermacentor spp. and Rhipicephalus sanguineus) and fleas (Ctenocephalides spp.) on the dog. Fluralaner has a high potency against ticks and fleas by exposure via feeding, i.e. it is systemically active on target parasites. Fluralaner is a potent inhibitor of parts of the arthropod nervous system by acting antagonistically on ligand-gated chloride channels (GABA-receptor and glutamate-receptor). In molecular on-target studies on insect GABA receptors of flea and fly, fluralaner is not affected by dieldrin resistance. In in vitro bio-assays, fluralaner is not affected by proven field resistances against amidines (tick), organophosphates (tick, mite), cyclodienes (tick, flea, fly), macrocyclic lactones (sea lice), phenylpyrazoles (tick, flea), benzophenyl ureas (tick), pyrethroids (tick, mite) and carbamates (mite). The product contributes towards the control of the environmental flea populations in areas to which treated dogs have access. Newly emerged fleas on a dog are killed before viable eggs are produced. An in vitro study also demonstrated that very low concentrations of fluralaner stop the production of viable eggs by fleas. The flea life cycle is broken due to the rapid onset of action and long lasting efficacy against adult fleas on the animal and the absence of viable egg production.

Pharmacokinetics

Following oral administration, fluralaner is readily absorbed reaching maximum plasma concentrations within 1 day. Food enhances the absorption. Fluralaner is systemically distributed and reaches the highest concentrations in fat, followed by liver, kidney and muscle. The prolonged persistence and slow elimination from plasma (t1/2 = 12 days) and the lack of extensive metabolism provide effective concentrations of fluralaner for the duration of the inter-dosing interval. Individual variation in Cmax and t1/2 was observed. The major route of elimination is the excretion of unchanged fluralaner in faeces (~90% of the dose). Renal clearance is the minor route of elimination.

Drug interactions

Fluralaner is highly bound to plasma proteins and might compete with other highly bound drugs such as non-steroidal anti-inflammatory drugs (NSAIDs) and the cumarin derivative warfarin. Incubation of fluralaner in the presence of carprofen or warfarin in dog plasma at maximum expected plasma concentrations did not reduce the protein binding of fluralaner, carprofen or warfarin. During clinical field testing, no interactions between Bravecto chewable tablets for dogs and routinely used veterinary medicinal products were observed.

Overdosage

No adverse reactions were observed following oral administration to puppies aged 8–9 weeks and weighing 2.0–3.6 kg treated with overdoses of up to 5 times the maximum recommended dose (56 mg, 168 mg and 280 mg fluralaner/kg bodyweight) on three occasions at shorter intervals than recommended (8-week intervals). There were no findings on reproductive performance and no findings of concern on offspring viability when fluralaner was administered orally to Beagle dogs at overdoses of up to 3 times the maximum recommended dose (up to 168 mg/kg bodyweight of fluralaner). The veterinary medicinal product was well tolerated in Collies with a deficient multidrug-resistanceprotein 1 (MDR1 -/-) following single oral administration at 3 times the recommended dose (168 mg/kg bodyweight). No treatment-related clinical signs were observed.

Check Digit Verification of cas no

The CAS Registry Mumber 864731-61-3 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 8,6,4,7,3 and 1 respectively; the second part has 2 digits, 6 and 1 respectively.
Calculate Digit Verification of CAS Registry Number 864731-61:
(8*8)+(7*6)+(6*4)+(5*7)+(4*3)+(3*1)+(2*6)+(1*1)=193
193 % 10 = 3
So 864731-61-3 is a valid CAS Registry Number.

864731-61-3Downstream Products

864731-61-3Relevant articles and documents

Synthetic method of fluralana

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, (2022/04/15)

According to the method, 2-methyl-5-bromobenzoic acid is adopted as a raw material, and Suzuki coupling reaction, condensation reaction, dehydration cyclization reaction and amide condensation reaction are performed to finally obtain the fluralan. According to the synthesis method, the reaction cost is reduced, the yield is improved, and the reaction period is shortened.

Fluorine thramine intermediate and method for preparing flumbine by using same

-

, (2021/12/07)

The invention discloses a fluororesonide intermediate and a method for preparing the same, and a fluororesonide intermediate -5. Routes include the use of m-xylene as starting materials, halogenation. Oxidation reaction The intermediate -5 is further obtained by hydroximation, cyanolation, hydrolysis reaction or cyanation, oximation, and hydrolysis reaction. As some examples of the present invention, synthetic routes were increased 2 steps from 5 steps in the prior art, but surprisingly high overall yields were obtained and the purity of intermediate -5 was significantly increased. , The starting material of the intermediate -5 is prepared from high 4 - bromo -2 - methylbenzoic acid to low-priced m-xylene, so that the cost of the intermediate -5 is greatly reduced. , The reaction condition is mild, the synthesis difficulty is low, and the environment is more environmentally friendly.

Method for preparing fluralana intermediate, prepared intermediate and application of fluralana intermediate

-

, (2021/10/05)

A method for preparing a fluralana intermediate, provided by the invention, comprises the following steps: carrying out nucleophilic addition reaction on 1-(3, 5-dichlorophenyl)-2, 2, 2-trifluoroethanone, carrying out acidolysis, reacting with a Grignard reagent, carrying out oxidation, carrying out oxidation cyclization reaction, reacting with hydroxyl(toluenesulfonyloxy)benzene iodide, and reacting with a trimethoxyphosphorus solution to finally generate the fluralan. In the preparation process, a catalyst and dimethoxy zinc are not needed, ultralow-temperature reaction conditions of -78 DEG C are not needed, operation is easy and convenient, meanwhile, reagents such as ozone and dimethyl sulfide which are harmful to the environment are replaced, and the method is more environmentally friendly. The invention also provides the intermediate for preparing the fluralan.

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