Shaanxi Bloom Tech Co., Ltd. yog ib qho ntawm cov neeg tsim khoom thiab cov khoom lag luam ntawm Palonosetron HLL CAS 135729-62-3 nyob hauv Suav teb. Txais tos rau kev lag luam wholesale ntau lub palonosetron HLL CAS 135729-62-3 rau muag ntawm no los ntawm peb lub hoobkas. Cov kev pabcuam zoo thiab tus nqi tsim nyog muaj.
Palonosetron hclyog ib qho kev xaiv siab thiab muaj zog thib ob {{0} {{{{{} HT} HT₃ Receptor Alonsist. Nws tshwj xeeb ISOQUEINOLINE RING system thiab thiazole pob txha hauv cov qauv milecular muab nws lub kinetic zoo dua thawj {{} tiam siv yeeb tshuaj. Daim ntaub ntawv siv tshuaj no rau 5 {{{10} HT₃ receptation ntawm kev ua kom muaj kev ntxhov siab ntawm cov kev tswj hwm ntawm Modulla, yog li ua tiav qib kev tswj hwm ntawm ob qho tseem ceeb. Nws cov xeeb ceem tseem ceeb tshaj plaws yog cov nyhuv tsis zoo {}} Thaum cov tshuaj sib hloov, nws txo cov khoom siv khi ntawm lwm qhov kev laus rau cov chaw nyob uas nyob ib sab. Qhov no "txoj haujlwm xauv tawm" ua kom muaj kev pheej hmoo thiab ruaj khov cov nyhuv antiemetic nyhuv. Piv rau luv- Ua yeeb yam tshuaj xws li ondansetron, Palonosetron muaj qhov cuam tshuam ntawm NK-1 Cov Kev Nyab Xeeb Kev Nyab Xeeb Kev Kho Mob los ntawm P Khoom. Qhov no ua rau nws cov kev tiv thaiv kev tiv thaiv ntawm kev siv tshuaj kho mob - induced ncua ntuav tshwj xeeb. Ib qho 0.25Mg lub hauv paus tswj tau tuaj yeem siv hluav taws xob tsis sib haum xeeb (mobile kev sib xyaw ua ke ntawm lub sijhawm kws tshuaj (mobile)
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Tshuaj Cov Qauv |
C19H25Cln2O |
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Muaj pes tsawg leej |
332 |
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Molecular hnyav |
333 |
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m/z |
332 (100.0%), 334 (32.0%), 333 (20.5%), 335 |
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Kev Ntsuam Xyuas |
C, 68.56; H, 7.57; Cl, 10.65; N, 8.42; O, 4.81 |
Palonosetron hcl, raws li ib tug heev meej 5 {{{{4} ht3 (5-hydroxyptamine 3) Receror Wulty hauv Kev Tswj Xyuas Kev Kho Mob, tau ua rau muaj kev pab cuam kho tshuaj kho mob - Indusive Nowinga thiab ntuav (CINV). Nws molecular qauv yog ingeniously tsim kom nruj nreem khi thiab thaiv 5-HT3 receptors. Qhov no muaj kev sib raug zoo uas cov tshuaj muaj peev xwm siv tau rau ntuav ntawm 5-hydrotands), thaum tsis muaj kev sib cuam tshuam tsis tsim nyog nrog cov phiaj xwm tsis tsim nyog. Yog li ntawd, nws muaj yuav luag tsis muaj ib qho txawv rau lwm hom receptor lossis tsuas yog qhia qhov tsawg kawg nkaus, muaj kev phom sij tsawg heev, txo qis kev pheej hmoo ntawm cov kev pheej hmoo ntawm kev phiv.
5 - HT3 Receptors ua si lub luag haujlwm tseem ceeb hauv kev saib xyuas me me thiab cov chaw ntuav rau hauv plawv nroog, nrog rau qhov chaw siab mos txwv tsis txaus ntseeg. Cov chaw no tseem ceeb heev rau kev tswj hwm lub cev ua haujlwm ib txwm muaj, tab sis lawv kuj yog cov chaw tseem ceeb ntawm kev siv tshuaj kho mob thiab ntuav.
Thaum cov tshuaj siv tshuaj siv rau hauv lub cev, lawv txhawb cov chromaffin hlwb hauv cov hnyuv me me kom tso tawm ntau npaum li cas ntawm 5-ht. Cov yeeb yaj kiab no 5-hts tom qab khi rau 5-HT3 cov receptors nyob ntawm cov neeg tsis muaj zog ntawm lub paum, ua kom kawg cov lus tshwm sim ntawm ntuav ntawm ntuav refainx. Cov txheej txheem no tsis tsuas yog coj kev tsis xis nyob rau cov neeg mob, tab sis tej zaum yuav cuam tshuam txog kev ua raws thiab kev ua tau zoo ntawm kev siv tshuaj kho mob.
Palonosetron hydrochloride, los ntawm nws lub zog thiab xaiv 5-HT3 kev tiv thaiv kev tawm tsam, yog li inhibiting kev tiv thaiv rau cov neeg mob kis cov tshuaj kho mob. Ib qho ntxiv, vim nws cov kev mob tshwm sim qis, palonosetron hydrochloride tseem tuaj yeem pab txhim kho cov neeg mob lub neej zoo, ua rau lawv ua tiav cov chav kawm siv kho mob kom zoo dua.
Cov hau hluav taws xob
Txoj Kev 1
Nws yog cov lus qhia luv luv txog cov xwm txheej ntawm Palonosetron Hydrochloride los ntawm 1,8-naphthalene dicarboxylic anhydride li cov khoom pib.
1,8-naphthalene dicarboxylic anhydride + h2→ 1,8-naphthalene dicarboxylic acid
1,8-naphqualene dicarboxylic anhydride ua ntej rov ua thawj hydrochloric acid nyob rau hauv ib tug sib tov ntawm ethanol dej (v / v=3: 2). Tom qab ntxiv tus nqi tsim nyog ntawm palladium (PD / C) catalalt thiab disporing nws rau cov tshuaj lom neeg yog nqa tawm kom tau txais 1,8-naphthalene dicarboxylic acid (NPA). Cov kauj ruam no feem ntau yog tsom rau txo cov pab pawg carbonyL ntawm anhydrides rau carbonL pab pawg ntawm aldehydes.
C12H8O4+ NH31,8-naphthylacetic acid
Daws lub npa no tau nyob hauv kauj ruam 1 hauv kev sib xyaw ntawm ammonia dej / isopropanol thiab hnov qab nyob rau hauv cov amino acid (pw). Kev tswj hwm ntawm cov tshuaj tiv thaiv kub thiab sijhawm muaj qhov cuam tshuam tseem ceeb ntawm cov txiaj ntsig thiab cov khoom lag luam.
1,8-naphthylacetic Acid + SoCl21,8-naphyylacetyl chloride
RAWS LI NAP tau nyob hauv Kauj Ruam 2 nrog chlorine sulfite (socl2) Kom tau txais cov lus sib nug sulfonyl chloride complex. Thaum lub sijhawm cov txheej txheem no, dej yuav tsum zam kom tsis txhob nkag mus rau cov tshuaj tiv thaiv kev tiv thaiv kom tsis txhob cuam tshuam cov tshuaj tiv thaiv.
1,8-naphyylacetyl chloride + c6H5Ch=ch2→ penylmethylene n {-} sulfonyl {}} n- (1-naphy) formamide
Sulfonyl chloride tau nyob rau hauv kauj ruam 3 yog condensed nrog phenyyletylene kom tau txais phenylmethylene n}}}}}} (1-naphyyl) formamide compound.
Phenyyllene n {-} sulfonyl -}}- (1-nah → c19H25Npuag2O
Cov compound tau nyob rau hauv Kauj Ruam Hydroxide (Naoh) kom yauv nucleophilic ntxiv thiab ua kom muaj acylation ntau ntxiv kom tau palonosetron hydrochloride.
Txoj Kev 2
Nws yog siv TetrahyDronaphthalene raws li cov khoom pib, thiab cov kauj ruam tshwj xeeb yog raws li hauv qab no:
C10H12+O2 → C10H10O+H2O
Firstly, Tetrahadronaphthalene undergoes ib qho tshuaj tiv thaiv oxidation nrog oxygen. Cov oxidants feem ntau suav nrog ammonium persulfate (NH4) 2S2o8 lossis cov poov tshuaj Persassium Persundffate K2S2O8. Qhov tshuaj tiv thaiv no yuav tsim tsim kom muaj kev sib piv TetrahyDronaphhalene Ketone.
C10H10O + socl2→ tetrahydronaphthalenesulfonyl chloride + hcl
Rov qab lub TetrahyDronaphthalene Ketone tau txais nyob rau hauv kauj ruam 1 nrog chlorine sulfite (socl2), thiab ua cov tshuaj sufranhadronaphthalene Ketone Sulgoride ntau.
TetrahyDromaphthone Sulfonyl Chloride + R - nh2→ TetrahyDroofroofroofroofroofmide R + HCL
Ua cov tshuaj tiv thaiv hws ntawm TetrahydRonicaphthalenesulfonyl chloride tau nyob hauv kauj ruam 2 thiab tus amine sib txuas. Nyob rau hauv cov tshuaj tiv thaiv no, Amine compound tuaj yeem yog ib feem ntawm cov txheej txheem ua ntej ntawm palonosetron lossis tebchaw nrog cov qauv zoo sib xws. Cov kev cuam tshuam kev cuam tshuam feem ntau tau nqa nyob rau hauv Alkaline tej yam kev mob, thiab cov pib siv tau suav nrog cov sodium carbonate (na2co3) lossis sodium bicarbonate (Nahaco3).
Tetrahadronaphthalenesulfonamide - r + naoh → C19H25Npuag2O + na2Yog li3+H2O
Nthuav cov khoom hws tawm tau hauv kauj ruam 3 kom siv cov kev mob hydrocoxide (Naoh) lossis sodium bicarbonate (Nahco3) daws rau kev ua kom muaj kev sib cav sib ceg. Qhov kev sib txuas lus ntau tshaj plaws yuav ua rau nucleophilic ntxiv thiab endoandation tshua nyob rau hauv molecule, kawg uaPalonosetron hcl.
Kev Tshawb Fawb Txog Kev Tshawb Fawb
Carcinogenicity
Hauv 104 lub lim tiam carcinogenicity kawm ntawm cd - 1 mg / kg / hnub pom tau hais tias palonosetron yog tsis carcinogenic. Lub systemicic xwm txheej qib (ntshav AUC) ntawm Palonosetron tsim los ntawm kev sim siab tshaj plaws ntawm 0.25mg palonosetron (auc=29.8 ng. H / ml). Hauv 104 lub lim tiam kev kawm cov nas, txiv neej thiab cov poj niam thiab 60 mg / kg / hnub, thiab 90 mg / kg / hnub, feem. Qhov koob tshuaj ntau tshaj plaws tsim lub cev Palonosetron Organic Raug (Plasma Auc) uas yog 137-308 lub sij hawm cov koob tshuaj tib neeg pom zoo. Kev siv palonosetron nce qhov tshwm sim ntawm benign adrenal phaochromocytoma thiab malcedary cell, nws coj mus rau cov nas tsuag nas, nws tau coj mus rau cov nas cellular adenomular adenoma thiab sarcoma, thiab cov Qhov tshwm sim ntawm cov thyroid c-cell adenoma, sib xyaw Adenoma, thiab SARCOMA.
Kev hloov pauv
Cov kab mob ames xeem, Suav hamster ovaby celemary fna synthesis (UDS) kuaj, lossis nas micronetron tsis muaj mutagicity toxicity. Txawm li cas los xij, palonosetron muaj chromosomal aberrations nyob rau hauv Suav hamster ovary hlwb.
Muaj me nyuam yaus
Thaum Oraly muab rau cov nas ntawm ib qho koob tshuaj ntawm 60mg / kg (kwv yees li ntawm lub cev nqaij daim tawv thiab muaj peev xwm deev muaj peev xwm ntawm txiv neej thiab poj niam nas.
Palonosetron hcl, belongs rau chav kawm ntawm serotonin 5 {- HT3 repeptor antagonisers. Nws ua kom muaj kev ua tau zoo siab thiab ib qho kev ua tau zoo rau 5-HT3 receptor, nrog tus nqi IC50 ntawm 0.24 nm rau 5-HT3a thiab PKE tus nqi ntawm 10.4. Cov tshuaj no ua rau pom qeeb ua haujlwm qeeb, ua tau zoo nyob rau hauv cov lus teb cellular rau tshuaj p ob hauv vitro thiab hauv vivo.
Nws yog muab kev txhaj tshuaj, feem ntau nyob rau hauv ib koob ntawm 0.25 mg rau cov neeg laus los tiv thaiv kom tsis txhob muaj 30 feeb, kwv yees li 30 feeb ua ntej pib kho tshuaj kho mob. Rau ncua sij hawm xeev thiab ntuav, ib qho qis dua ntawm 0.075 mg yog muab tshuaj tiv thaiv 0.075 tau muab tshuaj tivthaiv ntxiv lawm 10 vib nas this tam sim ntawd ua ntej kev ua kom loog.
Qhov cia yuav tsum tau nyob ntawm kev tswj kub ntawm 20 {{}} 25℃(68-7 xyoos f), thaum tiv thaiv kom khov thiab tiv thaiv kom khov.
Hauv cov ntsiab lus xaus,Palonosetron hclyog cov tshuaj kho kom zoo thiab tseem ceeb heev rau kev tswj hwm xeev siab thiab ntuav cuam tshuam nrog kev siv tshuaj khomob, txhim kho cov neeg mob lub neej thaum kho.
Palonosetron hydrochloride yog ib tug xaiv heev thiab muaj ib qho zoo 5}} HT3 recinction agingist, teej tug-} tiam antiemetic cov tshuaj. Txij li thaum nws tshwm sim thaum ntxov xyoo pua 21, nws tau dhau los ua kev siv tshuaj kho mob-}} augment (cinv) thiab ntuav (PONV). Kev siv tshuaj kho mob ua rau xeev siab thiab ntuav (cinv) tau ntev yog ib qho ntawm cov neeg mob lub neej thiab kev kho mob kev coj ua. In the late 1980s to early 1990s, the successful development of first generation 5-HT3 receptor antagonists such as Ondansetron, Granisetron, and Dolasetron marked an important breakthrough in the treatment of CINV. Txawm li cas los xij, kev tshawb fawb tau txais kev ntsuas pom tseeb ntawm thawj zaug cov tshuaj: yog qhov muaj txiaj ntsig nyob hauv 24-9 teev) yog txwv tsis pub dhau 24- lub sijhawm ua haujlwm hauv kev kho ntuav ntuav ntuav tej tsos mob. Cov kev ua tsis zoo no tau ua rau kev lag luam kws tshuaj ntsuam xyuas tshiab 5-HT3 receptor antagonists nrog ntev kawg kev ua haujlwm thiab nce receptor affinty. Nyob rau hauv cov ntsiab lus no, helsinnn heltscare (tam sim no Helsinnare Group tau tsim kev tshawb fawb thiab kev txhim kho cov tshuaj tshiab. Lub tuam txhab muaj cov kev paub ntau ntxiv hauv kev kho mob qog thiab paub txog kev txhim kho tshiab ntawm 5-HT3 receptor antagonists nrog ntev ntev ntawm kev ua thiab muaj txiaj ntsig zoo. Qhov kev txiav txim siab tshiab no ncaj qha rau Palonosetron qhov kev tshawb pom.
Cim npe nrov: Palonosetron HLL CAS 135729-62-3, cov neeg muag khoom, chaw tsim khoom, chaw tsim khoom, lag luam, yuav, nqe, loj, rau muag