Parasites tau hloov zuj zus zoo kawg nkaus txoj kev ciaj sia nyob ntau lab xyoo. Tsis tau ib qho molecule -fluralaner- tswj kom txiav los ntawm cov kev tiv thaiv nrog kev ua tau zoo. To taub yuav ua li cas lub compound dismantles parasite paj hlwb tsis yog ib qho teeb meem ntawm scientific xav paub. Nws kuj tseem qhia tias yog vim li cas fluralaner tau dhau los ua ib qho ntawm cov khoom siv tshuaj muaj txiaj ntsig zoo tshaj plaws hauv kev tshawb fawb veterinary thiab agrochemical niaj hnub no.
Kab lus no taug kev los ntawm cov txheej txheem tseem ceeb tom qab fluralaner qhov kev txiav txim, los ntawm nws txoj kev nkag mus rau hauv cov ntaub so ntswg neural mus rau cascade ntawm cov xwm txheej uas xaus rau hauv kev tuag tes tuag taw.
Fluralaner Drops
1. General Specification (hauv Tshuag)
(1) Kev daws teeb meem
(2) Tablet
(3) Txhaj tshuaj
(4) Txau
(5) Poob
2.Customization:
Peb yuav sib tham tus kheej, OEM / ODM, Tsis muaj hom, rau kev tshawb nrhiav kev ruaj ntseg nkaus xwb.
Internal Code: BM-9-007
Fluralaner CAS 864731-61-3
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
Yuav Ua Li Cas Thaum Fluralaner Blocks Parasite Chloride Channels?
Lub Architecture ntawm Kab Chloride Channel
Hauv kab kab mob paj hlwb, cov tshuaj chloride ua raws li lub rooj vag. Lawv qhib thaum inhibitory neurotransmitters tam sim no, cia cov tshuaj tsis zoo chloride ions nkag mus rau hauv lub cell. Qhov dej ntws sab hauv no ua rau cov cell membrane zoo dua, uas ua rau lub cev tsis muaj zog thiab tswj lub cev muaj zog. Yog tsis muaj cov txheej txheem no, cov paj hlwb uas tau ua haujlwm tsis tuaj yeem rov qab mus rau qhov chaw so.
Fluralaner xaiv lub hom phiaj chloride raws uas tswj los ntawm ligands. Raws li kev tshawb fawb uas tau kawm los ntawm cov kws tshaj lij hauv thaj chaw entomology, fluralaner khi rau qhov tsis yog -kev sib tw inhibitory site ntawm cov channel no. Qhov no txwv tsis pub lawv qhib txawm tias muaj cov tshuaj raug cai.
Nyob rau theem synaptic, qhov no txhais tau hais tias tsis muaj kev tswj hwm cov teeb meem inhibitory ntxiv lawm.
Vim li cas Parasites tsis tuaj yeem them
Arthropod parasites, zoo li dev mub, zuam, thiab mites, muaj ib tug ntau yooj yim neural tsim nrog tsawg dua redundant txoj kev tshaj li mammalian hosts. Thaum fluralaner khi rau chloride channel, tsis muaj lwm txoj hauv kev los coj cov ions rov qab mus rau qhov sib npaug. Tsis muaj teeb meem ntau npaum li cas neurotransmitter tam sim no, cov channel kaw, tsis muaj kev tawm tsam rau cov lus excitatory. Ntau qhov kev tshawb fawb tau pom tias qhov kev xav no yog qhov ua raufluralanerthiaj li muaj txiaj ntsig tiv thaiv kab mob kab mob thaum tseem muaj kev nyab xeeb rau cov tsiaj.
Fluralaner thiab Kev tawg ntawm Inhibitory Neural Signaling
Yuav Ua Li Cas Inhibitory Neurotransmission Nquag Ua Haujlwm
Nyob rau hauv kab kab lub paj hlwb uas noj qab haus huv, thaiv cov tshuaj txuas mus rau daim nyias nyias receptors thiab cia chloride ions hla dhau. Cov txheej txheem no sib npaug tawm cov kev nkag siab zoo thiab nres cov neurons los ntawm kev tua sai heev. Tag nrho cov txheej txheem yog nyob rau ntawm ib tug mos mos electrochemical tshuav nyiaj li cas. Yog tias koj qaij nws me ntsis, kev txav tsis tu ncua yuav tshee; Yog hais tias koj qaij nws ntau, lub cev pib co uncontrollably.
Fluralaner cuam tshuam qhov sib npaug ntawm qib ntawm cov receptors, tsis yog theem ntawm kev ua cov neurotransmitters. Qhov no yog qhov sib txawv tseem ceeb heev. Cov tshuaj uas txwv tsis pub tsim cov neurotransmitters tuaj yeem ua rau kho biosynthesis tshwm sim.
Fluralaner kiag li zam qhov ua tau los ntawm kev ua haujlwm ncaj qha ntawm ion channel protein qauv. Qhov no nres tus receptor los ntawm kev teb txawm tias ntau npaum li cas ntawm ib qho inhibitory neurotransmitter tus kab mob ua rau.
Selective Pressure ntawm Arthropod Neural Tissue
Qhov tseeb tias fluralaner yog xaiv tsis yog ib qho xwm txheej. Cov cheeb tsam tseem ceeb ntawm kev sib txuas ntawm arthropod GABA-gated chloride channels yog lub cev sib txawv ntawm lawv cov tsiaj txhu. Fluralaner siv qhov zoo ntawm cov qauv sib txawv; nws cov duab molecular haum rau arthropod receptor site zoo heev thaum cuam tshuam nrog tib neeg lub hlwb receptors tsawg heev. Raws li cov phooj ywg- tshuaj xyuas cov kev tshawb fawb tshuaj, cov khoom sib txuas ua ke ntau zog rau cov kab receptors dua li cov vertebrate receptors. Qhov no yog vim li cas nws muaj kev nyab xeeb heev rau cov tsiaj uas siv los ua tswv.
Yuav Ua Li Cas Fluralaner Ua Kom Muaj Neuronal Hyperexcitation?
Lub Cascade Los ntawm Thaiv Cov Kabmob mus rau lub cev muaj zog tsis ua haujlwm
Thaum cov tshuaj chloride tsis ua hauj lwm, cov teeb liab ib txwm inhibitory ntawm lub synapse tsis teb rau ib qho excitatory signals uas tuaj rau hauv. Kev ua kom muaj peev xwm mus rau pem hauv ntej vim yog sodium thiab potassium ion ntws, tab sis tsis muaj dab tsi txo qis cov membrane voltage rau nws thawj theem. Qhov no ua rau txuas ntxiv depolarization, uas txhais tau hais tias lub xovtooj hluav taws kub txhua lub sijhawm yam tsis tau nres.
Nyob rau hauv cov nqe lus ntawm tus cwj pwm, qhov no tshwm sim raws li tremors uas tsis tswj, txhav tuag tes tuag taw, thiab thaum kawg poob tag nrho cov leeg nqaij. Tus kab mob no tsis tuaj yeem txav mus los, noj, lossis ua ntau dua ntawm nws tus kheej. Electrophysiological kev ntsuam xyuas ntawm cais arthropod paj hlwb npaj qhia tau hais tias nanomolar concentrations ntawm fluralaner txaus los ua rau cov nyhuv no.
Qhov no qhia tau hais tias muaj zog npaum li cas cov compound nyob rau hauv lub cellular theem.
Duration thiab Pharmacokinetics
Fluralanertau ua rau muaj kev txaus siab rau kev kawm ntau vim nws nyob twj ywm rau lub sijhawm ntev. Vim tias nws cov molecules yog lipophilic, nws tuaj yeem txav mus rau hauv cov ntaub so ntswg rog hauv cov kab mob hauv lub cev thiab maj mam nkag mus rau hauv cov hlab ntsha hauv lub lis piam lossis hli. Qhov no ntev - lub sijhawm muaj nyob hauv cov ntshav ua kom paub tseeb tias cov kab mob cab uas ua rau noj yog raug rau qib ntawm cov khoom sib txuas uas txwv tsis pub ua haujlwm. Cov kws tshawb fawb uas ntsuas tus nqi ntawm fluralaner hauv cov ntshav ntawm cov tsiaj kho tau pom tias qib tseem tuaj yeem kuaj pom 12 lub lis piam tom qab muab tshuaj. Qhov no yog vim cov tshuaj pharmacokinetic yam ntxwv, uas txhawb nqa nws siv nyob rau hauv ntev - ua yeeb yam veterinary formulations.
Lub luag haujlwm ntawm GABA thiab Glutamate Channels hauv Fluralaner Kev Ua Si
GABA-Gated Chloride Channels raws li Lub Hom Phiaj Tseem Ceeb
Hauv arthropod paj hlwb, gamma{0}}aminobutyric acid (GABA) yog lub ntsiab neurotransmitter uas ua rau cov paj hlwb qeeb. Nws ua haujlwm los ntawm GABA-gated chloride channels, thiab fluralaner thaiv cov channel yam tsis muaj kev sib tw nrog GABA. Qhov no txhais tau li cas yog tias nws tsis sib tw nrog GABA rau agonist binding site. Hloov chaw, nws kaw cov channel kaw los ntawm kev khi rau lwm qhov chaw allosteric. Cov kev tshawb fawb uas twb tau luam tawm ntawm receptor binding qhia tau hais tias qhov kev sib cuam tshuam allosteric no muaj zog thiab kav ntev, nrog kev sib cais ntawm cov nqi qis txaus kom cov receptor nyob ntev.
Glutamate-Gated Chloride Channels thiab Dual-Target Pharmacology
Ntxiv rau qhov thaiv GABA receptors, fluralaner tseem thaiv glutamate-gated chloride channels (GluCls), uas tsuas pom muaj nyob hauv kab. Hauv crustacean peripheral paj hlwb, cov channel no kuj ua raws li inhibitors, thiab thaiv lawv nrog fluralaner ua rau cov synaptic puas pib los ntawm GABA channel antagonism txawm phem dua. Vim hais tias ntawm ob lub hom phiaj - lub hom phiaj mechanism, arthropods yuav tsum tau nrog qhov tsis ua hauj lwm ntawm ob txoj kev inhibitory nyob rau tib lub sijhawm. Qhov no txhais tau hais tias excitatory kis tau tus mob tsis muaj kev cai counterforce txhua.
Los ntawm Ion Channel Dysfunction mus rau Parasite Paralysis: Txoj Kev Fluralaner
Lub Molecular-rau-Txoj Kev Sib Txuas
Txhawm rau ua kom muaj kev sib txuas ntawm cov xwm txheej molecular thiab ua rau tag nrho lub cev, koj yuav tsum pom cov paj hlwb ua lub network. Qee cov tshuaj hu uafluralanertuaj yeem nres ob qho tib si GABA-gated thiab glutamate-gated chloride channels los ntawm kev ua haujlwm. Qhov no txwv tsis pub lub cev muaj zog neurons tsis tuaj yeem cuam tshuam cov leeg pob txha. Thaum cov neuromuscular junctions tau txais cov cim excitatory tas li yam tsis muaj kev txwv tsis pub, cov leeg tau cog lus ntev. Vim hais tias ntawm txoj kev cov tshuaj khi rau receptors, tus kab mob mus rau hauv lub xeev ntawm spastic tuag tes tuag taw los ntawm uas nws tsis tuaj yeem rov qab.
Vim li cas Qhov Mechanism no tseem ceeb rau kev tshawb fawb thiab kev tsim khoom
Fluralaner yog cov khoom muaj txiaj ntsig zoo heev rau cov qauv tsim vim tias nws ua haujlwm hauv txoj kev tshwj xeeb heev - tawm tsam dual chloride channels hauv arthropods. Cov kws tshawb fawb ua haujlwm ntawm ectoparasiticides tuaj yeem suav cov koob tshuaj - teb cov kev sib raug zoo uas tsis hloov pauv, thiab cov neeg tsim khoom tau txais txiaj ntsig los ntawm lub hom phiaj paub zoo uas tsis tas yuav hloov kho rau cov kab mob sib txawv. Pharmaceutical intermediate developers thiab cov chaw muag tshuaj tshwj xeeb uas ua haujlwm hauv chaw kho tsiaj yuav tsum nkag siab txog txoj hauv kev no.
Xaus
Fluralanercuam tshuam cov kab mob parasitic paj hlwb nyob rau hauv ib txoj kev tshwj xeeb: nws khi tsis yog - sib tw rau arthropod chloride channels uas yog tswj los ntawm ob qho tib si GABA thiab glutamate, txwv tsis pub cov teeb liab cuam tshuam los ntawm kev xa thiab ua rau cov neurons nyob twj ywm overexcited ntev. Cov tshuaj tiv thaiv kab mob pib nrog lub cev muaj zog neurons ua dhau los thiab xaus nrog cov kab mob ua rau tuag tes tuag taw tag. Nws yog ib qho kev sib xyaw ua ke hauv kev tshawb fawb niaj hnub no ntawm ectoparasiticides vim nws xaiv lub hom phiaj arthropod receptor cov qauv thiab muaj cov tshuaj pharmacokinetic zoo.
Cov lus nug nquag
1. Dab tsi ua rau fluralaner xaiv rau cov kab mob es tsis yog cov tsiaj?
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Fluralaner siv cov qauv sib txawv ntawm arthropod thiab vertebrate chloride channel receptors. Nws txoj kev sib raug zoo rau kab GABA-gated channels muaj ntau dua li cov tsiaj sib npaug, uas suav nrog nws qhov dav dav kev nyab xeeb hauv cov kab mob.
2. Puas yog fluralaner ua haujlwm tawm tsam txhua tus kab mob arthropod?
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Fluralaner nthuav qhia dav kev ua haujlwm tawm tsam ectoparasites xws li hma, zuam, thiab mites. Tag nrho cov arthropods no qhia txog GABA-gated thiab glutamate-gated chloride channel lub hom phiaj uas fluralaner inhibits, ua kom muaj txiaj ntsig thoob plaws ntau hom hauv pawg no.
3. Ntev npaum li cas fluralaner tseem ua haujlwm tom qab kev tswj hwm?
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Vim nws cov qauv lipophilic, fluralaner faib rau hauv cov ntaub so ntswg rog thiab tso tawm maj mam mus rau hauv lub cev. Kev ntsuas cov ntshav plasma ntau tau raug sau tseg dhau 12 lub lis piam hauv ntau qhov kev tshawb fawb tshuaj pharmacokinetic, ua rau muaj kev tiv thaiv txuas ntxiv hauv kev siv tshuaj kho tsiaj.
Koom Tes Nrog Bloomtechz rau Koj Cov Kev Xav Tau Fluralaner
Bloomtechz nyob ntawd thaum qhov tseeb, qhov zoo, thiab kev cia siab yog qhov tseem ceeb. Bloomtechz yog tus txhim khu kev qhafluralanertus kws kho mob nrog ntau tshaj 12 xyoo ntawm kev paub hauv cov organic synthesis thiab tshuaj intermediates. Lawv khiav 100,000-square-meter GMP- cov chaw tsim khoom muaj ntawv pov thawj uas ua tau raws li cov qauv ntawm US FDA, EU, Nyiv, thiab CFDA. Peb peb -txoj kev tswj kev ua tau zoo muaj xws li kev tshuaj xyuas chaw ua haujlwm, hauv -QA/QC hauv tsev, thiab kev tshuaj xyuas los ntawm tus neeg thib peb txoj cai. Qhov no ua kom paub tseeb tias txhua pawg ua tau raws li cov qauv thoob ntiaj teb nruj tshaj plaws. Peb pab neeg muab koj cov nqi raug, txhim khu kev qha cov sij hawm, thiab tag nrho cov ntaub ntawv koj xav tau kom yooj yim kev lis kev cai clearance, txawm koj xav tau me me rau kev tshawb fawb los yog loj npaum li cas rau ntau lawm. Tham nrog peb tam sim ntawd txog yuav ua li cas Bloomtechz tuaj yeem pab koj nrog koj lub hom phiaj kev lag luam lossis kev tshawb fawb.
Xa lus rau peb ntawmSales@bloomtechz.com.
Cov ntaub ntawv
1. Ozoe, Y., Asahi, M., Ozoe, F., Nakahira, K., & Mita, T. (2010). Cov tshuaj tiv thaiv kab mob isoxazoline A1443 yog ib qho tshuaj tiv thaiv kab mob ligand -gated chloride channels. Biochemical thiab Biophysical Research Communications, 391(1), 744–749.
2. Gassel, M., Wolf, C., Noack, S., Williams, H., & Ilg, T. (2014). Tus tshiab isoxazoline ectoparasiticide fluralaner: Xaiv inhibition ntawm arthropod -aminobutyric acid- thiab glutamate-gated chloride channels thiab insecticidal/acaricidal activation. Kab Biochemistry thiab Molecular Biology, 45, 111–124.
3. Dryden, MW, Canfield, MS, Grovatt, D., & Smith, V. (2015). Kev sib piv ceev ntawm kev tua ntawm fluralaner thiab afoxolaner tawm tsam fleas ntawm kev sim kab mob dev. Veterinary Parasitology, 212(3–4), 413–417.
4. Kilp, S., Ramirez, D., Allan, MJ, Roepke, RKA, & Nuernberger, MC (2014). Pharmacokinetics ntawm fluralaner nyob rau hauv cov dev tom qab ib tug tib lub qhov ncauj los yog intravenous tswj. Parasites & Vectors, 7, 85.
5. Taenzler, J., de Vos, C., Roepke, RKA, Frénais, R., & Heckeroth, AR (2014). Kev ua tau zoo ntawm fluralaner tiv thaiv Otodectes cynotis kab mob hauv dev thiab miv. Parasites & Vectors, 7, 425.
6. Wuertz, S., & Gassel, M. (2016). Isoxazoline compounds thiab lawv cov haujlwm ntawm ligand-gated chloride channels hauv arthropods: Kev nce qib hauv molecular entomology. Phau ntawv Journal of Insect Physiology, 88, 40–48.