Kev Tshawb Fawb Tom Qab Fipronil: GABA Channels thiab Parasites

Fipronil tau txais ib qho chaw zoo -chaw saib xyuas tsiaj thiab kev ua liaj ua teb - thiab yog vim li cas. Qhov no phenylpyrazole compound fipronil poob, ua hauj lwm nyob rau hauv lub paj hlwb ntawm kab thiab arachnids, cuam tshuam ib qho tseem ceeb taw qhia txoj kev uas ua rau lawv lub paj hlwb ua hauj lwm. Kev nkag siab tias nws ua haujlwm li cas muab cov kws tshawb fawb, cov tuam txhab tsim khoom, thiab cov neeg yuav khoom kom pom tseeb tias yog vim li cas cov fipronil tee tseem yog ib qho mus rau - rau kev daws cov kab mob parasite tswj thoob ntiaj teb.

Txawm hais tias koj tab tom nrhiav cov khoom xyaw tshuaj nquag, tsim cov khoom siv tshuaj tua tsiaj, lossis tswj cov kev tswj xyuas kab tsuag, cov txheej txheem tom qab fipronil tsim nyog paub tob. Cia peb taug kev los ntawm kev tshawb fawb - kom meej meej thiab tsis muaj qhov nyuaj.

Compound Fipronil Thiab Praziquantel Spot On Solution

1. General Specification (hauv Tshuag)
(1) Kev daws teeb meem
2.Customization:
Peb yuav sib tham tus kheej, OEM / ODM, Tsis muaj hom, rau kev tshawb nrhiav kev ruaj ntseg nkaus xwb.
PIB: BM-9-022
Compound Fipronil thiab Praziquantel Spot On Solution
Lub khw tseem ceeb: Tebchaws Asmeskas, Australia, Brazil, Nyiv, Lub Tebchaws Yelemees, Indonesia, UK, New Zealand, Canada thiab lwm yam.
Chaw tsim tshuaj paus: BLOOM TECH Xi'an Hoobkas
Kev tshuaj xyuas: HPLC, LC-MS, HNMR
Kev them nyiaj yug Technology: R & D Dept.-4

Lub luag haujlwm ntawm GABA hauv Kab Neurology

GABA yog lub ntsiab neurotransmitter nyob rau hauv lub hlwb ntawm kab laug sab, kab, thiab ntau lwm yam parasitic tsiaj uas slows down paj hlwb. Muaj peev xwm khi rau GABA qhib txoj hauv kev rau chloride ions. Qhov no cia Cl⁻ ions nkag mus rau hauv lub cell. Qhov spike no nres cov neurons los ntawm kev tua, uas yog tib yam li qhia cov paj hlwb kom "tso tseg." Lub paj hlwb thiab cov hlab ntsha tuaj yeem tau txais kev zoo siab heev thiab poob tswj yog tias tus nres no tsis ua haujlwm.

Tib neeg kuj muaj GABA receptors, tab sis txoj kev uas lawv tsim yog txawv heev los ntawm qhov lawv tau tsim nyob rau hauv kab. Qhov sib txawv ntawm cov qauv no yog dab tsi ua rau fipronil xws li cov tshuaj muaj zog uas tuaj yeem ua haujlwm ntawm qee yam.

Fipronil koom nrog Channel

Chitin txwv tsis pub chloride ions nkag mus rau hauv vim nws nyob hauv qhov chaw no. Channel tsis muaj txiaj ntsig ntxiv lawm. Cov paj hlwb uas yuav tsum tsis txhob tua pib tua yam tsis tau hais kom nres. Tus kab mob tsis tuaj yeem rov qab mus rau qhov qub tom qab cov kab mob sib kis ntawm hyperexcitation. Cov kws tshawb fawb sau ntawv hauv phau ntawv Journal Pesticide Biochemistry thiab Physiology tau qhia tias fipronil khi zoo heev rau GABA receptors hauv kab. Nyob rau hauv parasitology tam sim no, qhov no ua rau nws yog ib qho ntawm cov muaj zog chloride channel blockers uas tuaj yeem siv tau.Los ntawm qhov chaw no, fipronil lub cev thaiv cov tshuaj chloride ion nkag. Cov channel ua tsis tau - ua haujlwm. Neurons uas yuav tsum nyob twj ywm inhibited pib firing yam tsis muaj kev txwv, ua rau ib tug cascade ntawm hyperexcitation uas parasite tsis tuaj yeem rov qab los.

Cov kev tshawb fawb luam tawm hauv Pesticide Biochemistry thiab Physiology tau lees paub tias fipronil's nanomolar binding affinity rau kab GABA receptors, ua rau nws yog ib qho muaj zog tshaj chloride channel blockers muaj nyob rau hauv niaj hnub parasitology.

Kev xaiv tus qauv hauv Flea Receptors

Fleas (Ctenocephalides felis) thiab lwm hom tsiaj muaj GABA-gated chloride channels uas txawv heev ntawm GABA-A receptors nyob rau hauv cov tsiaj nyeg raws li lawv tsim. Cov kab receptor subunit Rdl (ua haujlwm rau dieldrin) muaj cov duab tshwj xeeb rau nws qhov chaw khi uas fipronil siv kom zoo dua.

Nyob rau hauv thaj tsam ntawm entomological toxicology, cov kws tshawb fawb tau pom tias fipronil khi rau Rdl subunit 500 lub sij hawm muaj zog hauv cov kab ntau dua li ntawm cov kab mob vertebrates. Nws tsis yog qhov yuam kev uas qhov kev xaiv no tau ua; nws qhia tau hais tias yuav ua li cas lub hlwb ntawm cov kab thiab tsiaj txhu tau hloov pauv raws sijhawm. Qhov kev sib txawv no yog siv los ntawmcompound fipronil poobmus tua fleas los ntawm messing nrog lawv cov hlab ntsha.

Thaum siv cov koob tshuaj zoo, cov tee no feem ntau muaj kev nyab xeeb rau cov tsiaj uas lawv nyob.

Yog vim li cas Binding Persistence Matters

Ib qho zoo ntawm fipronil lub peev xwm los khi yog tias nws nyob ntawm qhov chaw receptor ntev. Fipronil nyob twj ywm hauv cov chloride channel qhov ntev, thaum qee cov tshuaj tawg sai sai. Tus dev tsis tuaj yeem nkag mus rau tus tswv tsev kho mob ntev, yog li txawm tias qhov kov luv luv yog txaus los tua nws. Ntau cov kev tshawb fawb hauv thaj teb tau pom tias cov tshuaj fipronil tee ua haujlwm rau ob peb lub lis piam tom qab siv ib zaug xwb. Vim li no, lawv zoo rau ntev - cov phiaj xwm tshem tawm cov kab mob.

Kev cuam tshuam ntawm Ionic Homeostasis

Cov paj hlwb hauv arthropods nyob ruaj khov vim tias chloride ions tuaj yeem txav mus los ntawm lawv. Thaum txhua yam ua haujlwm tau zoo, ua kom GABA receptors tswj lub peev xwm ntawm daim nyias nyias los ntawm kev cia Cl⁻ ntws hauv txoj kev tswj hwm. Thaum fipronil thaiv cov channel no, GABA cov cim tsis tuaj yeem xa cov tshuaj chloride ions mus rau hauv lub cell. Qhov no ua rau cov neuron so daim nyias nyias muaj peev xwm tsis ruaj khov, uas ua rau lub cell kom depolarized txhua lub sijhawm.

Qhov teeb meem no kis tau sai. Lub cev muaj zog neurons, hnov ​​neurons, thiab interneurons yog qee cov neurons uas nyob ntawm GABAergic inhibition. Lawv txhua tus pib ua haujlwm dua yam tsis raug tso tseg. Yog tias tus kab mob nkag mus rau hauv cov hlab ntsha, nws cuam tshuam cov paj hlwb uas tswj nws, thiab qhov teeb meem sai sai kis mus rau lwm qhov ntawm lub paj hlwb.

Cov tee ntawm cov compound fipronil ua haujlwm zoo rau txoj kev no vim tias lawv tuaj yeem muab tso rau ntawm daim tawv nqaij ncaj qha lossis los ntawm kev sib cuag transdermal. Qhov no ua rau kom cov active compound nkag mus rau hauv lub cev sai.

Irreversibility thiab Speed ​​of Action

Ib qho tseem ceeb uas yuav tsum paub txog fipronil cov txiaj ntsig ntawm kev thauj khoom chloride yog tias nws feem ntau tsis tuaj yeem thim rov qab hauv thaj teb. Nws yog tsis yooj yim sua rau tus kab mob los kho qhov sib npaug ntawm ions ib zaug fipronil nyob rau hauv cov channel. Lub sijhawm -rau-tua nkhaus tam sim no siab heev. Cov kev tshawb fawb tau pom tias cov dev mub pib tuag nyob rau hauv cov sij hawm ntawm nyob ib ncig ntawm cov neeg kho mob thiab feem ntau ploj mus hauv 24 mus rau 48 teev.

Vim hais tias cov compound yog lipophilic, nws lo rau oily, lipid- nplua nuj txheej ntawm daim tawv nqaij thiab plaub. Qhov no ua rau lub concentration siab txaus los tua cov kab mob tshiab uas tuaj rau hauv.

Los ntawm Channel Blockade mus rau Cwj Pwm Quav

Sai li GABAergic kev tawm tsam xaus, tus kab mob sai sai poob lub peev xwm txav mus los. Qee cov kab thiab kab laug sab coj txawv txawv heev thaum lawv raug fipronil. Lawv tsiv mus nyob ib ncig ntawm randomly, lawv cov leeg cog lus tsis muaj lawv tswj, lawv ua tuag tes tuag taw, thiab ces lawv tuag. Txoj kev uas tib neeg ua tau hloov pauv vim yog qhov tshwm sim hauv lub hlwb ntawm qib receptor. Thaum cov neurons tau zoo siab heev, lawv xa tawm cov peev txheej ua haujlwm ntau dua yam tsis tau nres. Qhov no ua rau nws nyuaj rau cov leeg ua haujlwm ua ke.

Nws tsis yog ib qho xwm txheej ntawm ib qho.

Qhov tsis ua haujlwm kis tau vim GABA tswj hwm cov haujlwm ntawm cov neurons uas ua rau lub hlwb qeeb hauv ntau txoj hauv kev neural. Kev nkag siab qhov rooj nres ua haujlwm, cov tshuaj tiv thaiv arcs luv luv -circuit, thiab cov txheej txheem autonomic yuav phem zuj zus rau tib lub sijhawm. Tus kab mob muaj lub sijhawm nyuaj los tswj nws cov kev txav, txawm tias nws tsis tau sim.

Selectivity Versus Non-Cov Hom Phiaj

Kab laug sab thiab kab laug sab muaj zog GABA receptors uas fipronil khi rau ntau dua li tib neeg receptors. Qhov no yog vim li cas cov receptor subunits tau muab tso ua ke thiab cov duab ntawm lub hnab ntawv khi. Peb qhov chaw uas ua rau nas GABA-A receptors yog , , thiab . Lawv cov qauv thiab qhov pore tsim txawv, thiab fipronil tsis haum rau lawv thiab.

Tsis tas li ntawd,compound fipronil poobNws yog qhov zoo heev ntawm kev tua kab mob thaum muaj kev nyab xeeb ntau dua rau tus tswv tsev thaum lawv siv kom raug.

Mechanistic tiav ntawm tus qauv

Tag nrho txoj kev uas fipronil ua haujlwm tau piav qhia los ntawm GABA channel blockage mus kom ze. Invertebrates 'cov paj hlwb tsuas yog cov tshuaj cuam tshuam, thiab nws cov teebmeem tsis tuaj yeem thim rov qab. Qhov no yog vim li cas nws ua haujlwm sai heev thiab muaj zog heev ntawm nanomolar qib. Kev kho tsiaj tau tshem tawm hma, zuam, thiab nab, thiab lwm yam. Tag nrho cov teebmeem no tuaj yeem txuas rau qhov kev sib cuam tshuam tshuaj lom neeg.

Cov teb chaws loj xws li Asmeskas, EU, thiab Nyij Pooj kuj tau pom zoo fipronil vim nws paub meej tias nws ua haujlwm li cas. Lub Chaw Haujlwm Saib Xyuas Tshuaj Hauv Tebchaws Europe (ECHA) thiab US Environmental Protection Agency (EPA) ob leeg tau them nyiaj ntau rau cov receptor- khi cov ntaub ntawv.

Txoj kev sib xyaw ua haujlwm tseem yog ib qho kev nkag siab zoo tshaj plaws hauv thaj chaw parasitology hauv cov tsiaj.

Cov kev cuam tshuam rau kev tsim qauv Science

Paub txog yuav ua li cas GABA channel thaiv kev ua haujlwm kuj pab cov neeg uas ua cov tshuaj fipronil tee ua rau lawv zoo dua. Muab fipronil rau ntawm tus tswv tsev daim tawv nqaij tsis txaus; nws yuav tsum muaj peev xwm ncav cuag thiab nyob rau theem siab hauv qhov chaw uas cov kab mob cab noj lossis kov tus tswv tsev. Qhov no yog ua tau vim hais tias ntawm physicochemical zoo ntawm fipronil, kev sib xyaw ntawm excipients thiab cov kuab tshuaj, thiab lub thickness ntawm lub tsheb. Nrog rau lub log P tus nqi ntawm 4.0, cov molecule yog lipophilic heev, uas txhais tau tias nws yuav siv sij hawm me ntsis qhov chaw nyob rau hauv lub fatty txheej ntawm lub integument.

Qhov no ua rau lub ntuj tso tseg uas ua rau cov khoom sib xyaw ua haujlwm ntev dua li lub sijhawm nws tau hais kom siv.

Ib txoj hauv kev zoo tshaj plaws - paub thiab muaj tseeb tshaj plaws kom tshem tau cov kab hauv kev tshawb fawb niaj hnub no yog siv covcompound fipronil poobkom nres GABA-gated chloride channels. Ib tug phooj ywg- tshuaj xyuas kev kawm los ntawm ntau dua 30 xyoo dhau los tuaj yeem siv los thaub qab thiab taug qab txhua qhov kev txav mus los. Nws pib nrog qhov tseeb khi rau kab Rdl receptor subunits thiab xaus nrog cov tshuaj tiv thaiv kab mob ntawm cov neurons ua zoo siab heev.

Bloomtechz nyob ntawd thaum koj xav tau cov chemistry meej thiab cov saw hlau koj tuaj yeem suav rau. Bloomtechz yog lub tuam txhab ntseeg siab uas tau ua cov organic synthesis thiab tshuaj zoo rau ntau tshaj 16 xyoo. Lawv yog tus paub txog cov khoom sivcompound fipronil poob. US FDA, EU GMP, JP, thiab CFDA txhua tus tau pom zoo rau lawv 100,000-square-meter GMP- tau ntawv pov thawj qhov chaw tsim khoom, qhov chaw lawv ua haujlwm. Muaj peb theem kev tswj xyuas zoo hauv peb lub tuam txhab: kev tshuaj xyuas los ntawm lub Hoobkas, sab hauv QA / QC, thiab kev pov thawj los ntawm peb lub koom haum - tog. Nws ua kom paub tseeb tias txhua batch ua tau raws li cov qauv siab tshaj plaws los ntawm tag nrho lub ntiaj teb. Yog tias koj xav tau cov tshuaj intermediates, tsiaj cov khoom xyaw, lossis kev cai tshuaj synthesis, peb pab neeg npaj txhij los pab koj kom ncav cuag koj cov hom phiaj tsim. Peb muab cov sij hawm coj mus kuaj kom raug, tus nqi meej, thiab kev cog lus ntawm kev sib raug zoo mus ntev. Peb xav tham txog koj cov kev xav tau tam sim ntawd, yog li thov email rau peb pab neeg ntawm Sales@bloomtechz.com.

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2. Hosie, AM, Baylis, HA, Buckingham, SD, & Sattelle, DB (1995). Kev ua ntawm cov tshuaj tua kab fipronil ntawm dieldrin{11}}rhiab heev thiab resistant GABA receptors ntawm Drosophila melanogaster. British Journal of Pharmacology, 115(6), 909–912.

3. Cole, LM, Nicholson, RA, & Casida, JE (1993). Kev ua ntawm phenylpyrazole tshuaj tua kab ntawm GABA-gated chloride channel. Pesticide Biochemistry thiab Physiology, 46(1), 47–54.

4. Ikeda, T., Nagata, K., Shono, T., & Narahashi, T. (1998). Dieldrin thiab fipronil thaiv GABA- qhib cov tshuaj chloride ntawm dorsal cag ganglion neurons. European Journal of Pharmacology, 347(1), 1–8.

5. US Environmental Protection Agency. (1996). Fipronil: Daim ntawv qhia txog tshuaj tua kab. Office of Prevention, Tshuaj tua kab thiab tshuaj lom, Washington, DC.

6. Tingle, CCD, Rother, JA, Dewhurst, CF, Lauer, S., & King, WJ (2003). Fipronil: Ib puag ncig txoj hmoo, ecotoxicology, thiab kev txhawj xeeb ntawm tib neeg kev noj qab haus huv. Kev tshuaj xyuas ntawm Environmental Contamination thiab Toxicology, 176, 1–66.