Esafoxolaner EPRINOMECTIN THIAB PAZQUICANTEL SALICAL SUAV

Esfoxolane yog qhov s - Entantiomer ntawm Afoxolane, nrog molecat hnyav ntawm 625.9 G / Mol, tus nqi logp ntawm 4.8, thiab siab lipid solubility. Lub trifluorrethylphenylphenylphenylphenylphenylphenylphenyl thiab cov nplhaib hauv nws cov qauv molecular tas nws nrog lub peev xwm loj heev:
Liposoluble pab: Trifluoromethyl (- cf α) thiab immidazole lub nplhaib txhim kho molecular hydrone lipid lipid lipid liprix;
Hydrogen Ber receptor: cov nitrogen atom nyob rau hauv lub imidazole lub nplhaib tuaj yeem ua raws li lub pas dej lipid pawg ntawm stratum kws ua haujlwm los txo OSMOTOTIONS.

Esafoxolane, raws li lub zog inhibitor ntawm gamma aminobutyric acid (gaba) {} gated chloride raws cov txheej txheem hauv qab no:
Neuroinhhibition: Thaiv Gaba / glucl raws nyob rau hauv lub posssynaptic ntawm dev mub thiab zuam hypePolarization, thiab neeg tuag tes tuag taw tsis taus;
Selective toxicity: The affinity for mammalian GABA receptors is more than 1000 times lower (cat GABA receptor IC50>10 μ m), txhawm rau kev nyab xeeb;
Autotoxicity nyhuv: Thaum cov quav flea tom, cov tshuaj accumulates nyob rau hauv Flea lub plab zom mov los ntawm kev nqus cov ntshav nqus cov txheej txheem, tua tus dev mub thiab tiv thaiv nws los ntawm kev nteg qe.

Thawj zaug nkag mus: Tom qab ntawv thov sab nraud, cov txheej txheem Esafolane sai sai rau hauv cov follicular funnel (nrog rau kev nkag mus ntawm 30% tsis pub dhau 1 teev);
System faib:
Kev Phem: tsub zuj zuj hauv adipose ntaub so ntswg (ib nrab {{} lub neej t}}}-} kav dej.

Kev hloov kho molecular thiab cov tawv nqaij affinity
Epinomectin yog ib qho kev ua yeeb yam ntawm Avermectility yog qhov zoo los ntawm Averylate C4-Au ntawm Averylate C4, Solubility 0.5 mg / mL) thaum khaws nws lipophilic skeleton (logp tus nqi 3.8); Ntxiv lub nplhaib hloov kho lub nplhaib (xws li PentACSALCLIC-kom txo cov tawv nqaij ua kom tsis kam. Nws cov molecular hnyav yog 914.13 G / Mol, thiab nws thaj chaw thaj tsam yog nce ntxiv los ntawm nanocrystal technology (particle loj<200 nm) to promote permeation. Preclinical studies have shown that the dermal concentration reaches its peak (Cmax 4.2 μ g/g) 12 hours after topical application, with a distribution volume of Vd=3.2 L/kg, indicating that the drug can penetrate deep tissues.

Epinomectin tua nematodes thiab arthropodes los ntawm cov txheej txheem nram qab no:
GlucL Channel Ua Kom Tiav: Tsim Parasitic Neuromuscular tuag tes tuag tes tuag taw, ua rau lub cev muaj zog thiab kev tuag;
Gaba receptor kev cai: txhim kho Gaba Mediaed Chloride Ion Incorx, interhibits Parasite pub mis thiab luam;
Kev Nkag Siab ntawm Ntshav -}} {{-}}}}}}} ecinomectin muaj peev xwm tua cov cab (xws li lub plawv dhia tawm) hauv cov ntaub so ntswg.

Cov plaub hau follicle nqus: Hauv 30 feeb tom qab daim ntawv thov sab nraud, nws yog nrawm nrawm los ntawm cov hauv paus plaub hau thiab hws cov qog ntawm 25%);
Kev Thauj Ua Si Lymphatic: Nkag mus rau hauv cov hlab ntshav los ntawm cov hlab ntsha Dymal tessels kom tsis txhob ua ntej hla kev cuam tshuam;
Adipose nqaij ntxiv: txuam hauv subcutaneous rog (siab 5-10 npaug ntawm ntshav), sib sau cov tshuaj muaj tshuaj.

Prazatantel muaj cov molecular hnyav ntawm 3541 g / mol thiab lub cimp tus nqi ntawm 2.8. Nws zwm rau cov tshuaj hydrophilic (dej ayophilic (dej {{2} Soluble 4 mg / ml) thiab yog kev coj ua nyuaj los dhau ntawm daim tawv nqaij tawv nqaij. Nws cov kev puas tsuaj tiv thaiv feem ntau yog los ntawm:
Tsawg roj ua solubility: logp tus nqi<3, difficult to penetrate the lipid matrix of the stratum corneum;
Lub siab polarity muaj cov pyrazine ntau thiab cov nplhaib benzene, sib sau cov qauv polar ruaj khov uas tsis muaj kev cuam tshuam passive diffusion.

Prazatequantel tua cov kab mob los ntawm cov txheej txheem hauv qab no:
Calcium channel cuam tshuam: activates l- Hom Tshuaj calceworms ntawm cov kab mob calhews, ua rau cov kab mob calcium calcium thiab txhawb nqa cov leeg thiab txhuam hniav;
Nto membrane raug mob: rhuav tshem cov qauv glycoprouplein ntawm ob lub ntsej muag ntsej muag, nce mem caj ces, thiab ua rau muaj cab tsis taus thiab tuag;
Kev Txhaj Tshuaj Tiv Thaiv: Raug rau TapuardS antigens ua kom cov tswv tsev muaj zog tiv thaiv tus kheej (xws li macrophage phagocytosis) kom tshem tawm cab.
Nws LC50 rau Dipylidium Caninum hauv cov dev yog 0.1 μ G / ML, thiab nws yog rhiab rau cov tootherorms hauv miv xws li Taenia Solium.

Nano crystal dispersion: prazateantel nanocrystals tau nkag mus los ntawm cov hauv paus plaub hau, nrog tus nqi rau cov plaub hau ntawm 15% hauv 1 teev;
Lipid Carrier effectures: Cov pawg lipophilic ntawm Esfroxolane thiab epinomectin form nrog prazathantel, txhawb lawv cov kev hla dhau ntawm Stratum Corneum;
PH Hloov Kho: Ntxiv citric acid tsis)