Shaanxi Bloom Tech Co., Ltd. yog ib qho ntawm cov khoom lag luam thiab cov khoom lag luam uas yeej 35428 CAS 50370-56-4 hauv Suav. Txais tos rau kev lag luam wholesale? Zoo zoo yeej 35428 CAS 50542-8 Cas 50370-56-4 Kev Muag Khoom Ntawm No Los Ntawm Peb Lub Hoobkas. Cov kev pabcuam zoo thiab tus nqi tsim nyog muaj.
Yeej 35428Yog cov tshuaj sib txuas ua ke uas yog cov phenylcyclidine (PCP) chav kawm ntawm cov derivatives. Cov lus sib txuas no feem ntau muaj cov tshuaj phenymashexylrohylpiperidation (PCP, suav nrog cov qauv tshuaj lom neeg "lossis" cov roj ua npuas) muaj pes tsawg leeg thiab lwm yam}} carbomethy-3- fluorophenyl) yog siv rau kev tshawb fawb tshawb fawb, tshwj xeeb tshaj plaws hauv kev tshawb fawb thiab chaw muag tshuaj. Nws ntseeg tau tias cuam tshuam rau neurotransmitter kis tau tus mob hauv nruab nrab ntawm nruab nrab, yog li hloov kho lub hlwb ua haujlwm thiab tus cwj pwm. Txawm li cas los xij, vim nws cov peev txheej muaj peev xwm thiab kev pheej hmoo ntawm kev tsim txom, 2-carbometoxy-3- Fluorophenyl) tropane muaj kev kho mob tsawg heev lossis kho cov ntawv thov.
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| Tshuaj Cov Qauv | C16h20FNO2 |
| Molecular hnyav | 277.33 |
| Muaj pes tsawg leej | 277.15 |
| m/z | 277.15 (100.0%), 278.15 (17.3%), 279.15 (1.4%) |
| Kev Ntsuam Xyuas | C, 69.29; H, 7.27; F, 6.85; N, 5.05; O, 11.54 |
| Melting taw tes | 91-92 Qib |
| Kub taw tes | 349 degree |
| Ceev | 1.155 |
| Kev Cia | Muab ntim rau hauv qhuav, 2-8 degree |
| So | H2O: Soluble |
| Flash point | 165 degree |
| Acidity Coefficient (PKA) | Acidity Coefficient (PKA) |
| Puab | khov kho |
| Xim | xim dawb |
Yeej 35428(Tshuaj lom neeg lub npe: {- craft, tus lej tseem ceeb, thiab kev tshawb fawb tseem ceeb raws li nws qhov kev kho mob rau dopamine transpor (dat).
1. Dopamine Transporter (DAT) Tshawb Nrhiav Cov Cuab Yeej
(1) Radiolabeled Tracer
Lub xov tooj cua isotope sau daim ntawv ntawm yeej 35428 (xws li [¹¹ c] yeej 35428) yog tus qauv kub rau POSITRON EPURSION BOSRY (TSIAJ). Qhov hloov cov roj carbon atoms (n {{{}} methyl lossis 2-carboxymethyl pawg, zam kev siv cov tshuaj uas ua ntej xws li cov tshuaj yeeb tshuaj yeeb zoo li cocaine derivatives.
Cov ntaub ntawv thov daim ntawv thov: Hauv Parkinson cov kev tshawb fawb ntawm tus kab mob, [tus tsiaj tuaj yeem lav cov hluav taws xob ntom ntom, pabcuam thaum kuaj mob thiab kuaj mob.
Kev sim tsiaj tau pom tias kev siv teeb liab yog qhov tsis zoo nrog cov poob ntawm dopamininer neurons nyob rau hauv lub txiaj ntsig nigra (r =-0.82, p<0.01).
(2) hauv vitro khi kev sim
Tritium sau daim ntawv sau tseg yeej 35428 ([³ h] yeej 35428) yog dav siv los ntsuas kev sib raug zoo ntawm kev ua yeeb yam rau dat. Nws cov kev sib cais tsis tu ncua (KD ≈ 1.2 nm) yog qhov zoo sib xws los ntawm 7 zaug, ua rau nws tsim nyog dua rau kev kawm ntev ntxiv.
Kev ua tiav kev ua kom zoo dua: piv rau cov yeeb dawb, qhov tsis {{}}}} Txoj hlua khi tshwj xeeb ntawm 40%, txhim kho cov ntaub ntawv ntseeg tau.
2. Kev tsom xam ntawm lub tshuab ntawm cov nruab nrab ntawm cov hlab ntsha
(1) DOPAMINE DOPAMINE FUXUS
Yeej 35428, raws li xaiv data inhibitor, yog 3-10 zaug ntau dua cov yeeb dawb tshaj li yeeb (IC} {μ m vs {}} {m). Hauv Ex Vivo synaptic kev sim, thim rov qab ntawm Dopamine Ruptake yog siv los kawm synaptic plarient thiab kev quav yeeb tshuaj xaiv kev yoog.
Cov kev sim tsiaj: Ib tus kheej - Cov thawj coj ntawm cov tshuaj tiv thaiv yeeb tshuaj 35}}}} Kuv)
(2) Kev tshawb fawb hla ntawm serotonin thauj (soter)
Txawm hais tias yeej 35428 muaj qis ater rau sert (k}} {μ m rau detore dopamine system kev sib cuam tshuam. Piv txwv li, hauv 5 {{{5 5}} ht-ib qho kev cuam tshuam ntawm cov nas, qhia txog cov kev tswj hwm lub luag haujlwm ntawm Sergamine cov nqi zog txoj kev.
3. Kev Tshawb Nrhiav Cov Cuab Yeej Rau Cov Hlau Ua Kom
(1) Qhov chaw uas muaj kev nyiam ua ke (CPP) qauv
Yeej 35428 (0.5-2 mg / kg) tuaj yeem ntxias cpp cwj pwm hauv cov nas, thiab nws qhov kev nyhuv yog ob zaug ntawm cov yeeb dawb. Los ntawm cov txheej txheem Optogenetic sib xyaw ua ke nrog yeej 35428 ua tiav, nws tau pom tias ua kom muaj kev ua haujlwm ntawm Dopamine Neural (VTA) yog qhov tsim nyog rau CPP tsim.
(2) Kev Ntsuam Xyuas Kev Kho Mob Cov Tshuaj Kho Mob
Raws li ntev - Ua yeeb yam Dopamine ruptorget, yeej 35428 cov khoom pov thawj muaj peev xwm hloov yeeb dawb hauv cov tsiaj quav. Cov thawj coj mus txuas ntxiv ntawm 2 mg / kgYeej 35428Txog 7 hnub tuaj yeem txo tus kheej {1} kev tswj hwm tus nqi ntawm tus kheej ntawm cov yeeb yaj kiab, qhia tias nws muaj kev hloov yeeb tshuaj ntxiv.
Cov Lus Qhia Kev Kho Mob Muaj Peev Xwm
1. Kev kuaj mob ntawm cov kab mob neurodegenerative
(1) Thaum Ntxov Nrhiav Tau Ntawm Parkinson Tus Kab Mob
Yeej 35428-pev tuaj yeem tshawb xyuas cov kev hloov pauv hauv cov chaw ntom ntom hauv txoj hauv kev uas tsis zoo hauv txoj kev nyob hauv txoj kev uas tsis raug cai, thiab ntes Nigronal Degenteration 3-5 xyoos dhau los ntawm kev kuaj mob. Cov kev tshawb fawb soj ntsuam tau pom tias nws qhov kev kuaj mob yog 92% thiab tshwj xeeb yog 89%, zoo dua li kev kuaj ib txwm muaj.
(2) Daim Ntawv Qhia Txog Lewy Lub Cev Dementia
Lub dat khi tus nqi ntawm cov striatum hauv cov neeg mob Lewy Dementia yog txo los ntawm 45428-}}}}}}}}}}}}}}}}}}}}}}}}}}}}}}}}}}}}}}}}}}}}}}}}}}}}}}
2. Kev tshawb nrhiav hauv kev kho mob hlwb
(1) Mloog tsis txaus ntseeg hyperactivity tsis meej (ADHD)
Yeej 35428 derivatives tau pom los txhim kho lub cim xeeb ua haujlwm hauv cov tsiaj ua haujlwm, thiab lawv cov tshuab kev nqis tes cuam tshuam nrog enhanced dopamine tso tawm hauv qhov Prefortex. Cov kev tshawb fawb preclinical qhia tias tsawg tshuaj (0.1-0.3 mg / kg) yuav txhim kho cov tsos mob adtulating los ntawm kev tswj hwm dat tsis muaj kev pheej hmoo txaus ntshai.
(2) kev sib raug zoo kho rau kev nyuaj siab
Cov tshuaj tiv thaiv sai sai ntawm yeej 35428 (pib sijhawm<2 hours) in refractory depression may be related to its promotion of dopamine release in the ventral tegmental area. Preliminary clinical trials have shown that a single intravenous injection of 0.5 mg/kg can reduce Hamilton Depression Rating Scale scores by 50% and the effect lasts for 48 hours.
3. Kev tsim kev txhim kho kev txhim kho intermediates
(1) Tsim kev tiv thaiv yeeb tshuaj tshiab
Benzotropane Skeleton ntawm yeej 35428 muab ib tus qauv rau kev txhim kho ntawm xaiv dat inibitors. Ntau lub derivatives nrog 10-20 quav nce kev ua haujlwm tau txais los ntawm kev hloov kho cov txheej txheem, xws li qhia cov tshuaj fluorine lossis kev txuas ntxiv sab. Ntawm lawv, JHW 007 tau qhia tsis muaj cov peev txheej muaj quav nyob hauv kev ua yeeb yam thiab tau nkag rau theem II kev sim tshuaj.
(2) Radioopharmaceutical prefursor
Its sulfate form (WIN 35428 sulfate, CAS: 2068138-14-5) is widely used as a water-soluble intermediate in the synthesis of [¹¹ C]/[¹⁸ F] labeled probes. In the production process, by controlling the pH value (4.5-5.5) and reaction temperature (60-70 ℃), a radioactive labeling yield of>95% tuaj yeem ua tiav.
Cov txheej txheem hluavtaws rau Win35428 cuam tshuam nrog ntau cov kauj ruam, thiab cov txuj ci tshwj xeeb yuav sib txawv nyob ntawm chav kuaj thiab cov kev xav tau ntawm cov khoom lag luam.
Hauv qab no yog cov kev ua hluavtaws ib txwm rau Win35428:
1.starting cov ntaub ntawv
Feem ntau, pib cov ntaub ntawv rau synthesis ntawm win35428 tuaj yeem suav nrog Eyclohexanone lossis cyclohexanol, thiab tej zaum muaj nitrogen qhov (piv txwv li, amine lossis ammonia).
2.Txhob ntawm lub cyclohexyl nplhaib
Ua ntej, nws yuav tsim nyog los tsim lub cyclohexyl nplhaib. Qhov no tuaj yeem ua tiav los ntawm cov phenol derol deriv nrog cyclohexanone lossis cyclohexanol nyob rau hauv kev siv tsim nyog, piv txwv los ntawm alkylation, hws lossis kev kub ntxhov lossis kev kub ntxhov.
3.Qhov ntawm cov pab pawg ua haujlwm
Tom ntej no, cov pab pawg ua haujlwm tsim nyog, xws li pawg hydroxyl thiab methylenedioxy, yuav tsum tau qhia txog cov molecule. Qhov no tej zaum yuav tau ua los ntawm oxidation, txo, habogenation, etherification lossis lwm yam organic.
4. spintroduction ntawm nitrogen atoms
Tom qab kev tsim kho ntawm cov cyclohexyl nplhaib thiab pawg ua haujlwm tiav, cov atomsal atoms yuav tsum tau qhia rau hauv cov lwg me me. Qhov no tuaj yeem ua tiav los ntawm kev rov ua haujlwm nrog amine lossis ammonia los tsim cov qauv nitrogen heterocyclic.
5.Purification thiab tshaj tawm - kev kho
Thaum kawg, dawb huv Win35428 yog tau los ntawm cov kauj ruam tsim nyog ua kom haum (distillation, cov khoom lag luam chromatographic, thiab lwm yam khoom pib, thiab lwm yam impurities.
Yeej 35428 Thov Kev Pab Cuam
2-carbometoxy-3- (4-fluorophenyl) tropane, raws li ib qho kev cog lus phenycyclohexylohexy) yuav raug cov kev tswj hwm nruj thiab cov kev txwv.
Cov hauv qab no yog cov ntawv thov tau ntawm 2-carbomethoxy-3- (4-fluorophenyl) tropane:
Kev Tshawb Nrhiav Kev Tshawb Fawb
2-carbometoxy-3- Fluorophenyl) Tropane tuaj yeem siv los kawm nws cov nyhuv ntawm cov kev ua haujlwm ntawm cov hlab ntsha thiab kab mob kab mob. Xws li cov kev tshawb fawb yog qhov tseem ceeb rau kev nkag siab txog cov kab mob neurological (piv txwv li, schizophrenia, kev nyuaj siab, thiab kev tsim kho cov kev kho tshiab.
Tshuaj Kho Mob Tshuaj
Txawm hais tias 2 {{-}}}}}}}} fluorophenyl) tropane nws tus kheej yuav muab cov tswv yim thiab cov lus qhia tshiab rau kev txhim kho cov tshuaj tshiab. Los ntawm kev tshawb fawb hauv-2-carbometoxy-3- (4-fluoropheny)
Toxicology thiab Addiction kev tshawb fawb
Kev pheej hmoo ntawm kev tsim txom thiab kev quav ntawm 2-carbomethoxy-3- (4-fluorophenyl) tropane ua rau nws lub hom phiaj rau kev tshawb fawb toxicology thiab kev tshawb fawb ntxiv. Kev tshawb fawb ntawm cov txheej txheem ntawm kev ua thiab lom ntawm 2-carbometoxy-3- (4-fluoropheny-3- Fluorophenyl) tropane, thiab pab txhim kho kev ntsuas kev tiv thaiv zoo dua
Hauv cov ntsiab lus xaus, kev siv thawj zaug ntawm Win35428 Puas yog txhawm rau tshawb xyuas nws cov kev siv tshuaj pharapacological thiab muaj peev xwm kho cov ntaub ntawv kev tshawb fawb hauv kev tshawb fawb, nrog rau kev siv yeeb quav tshuaj thiab kev tshawb fawb ntxiv. Hauv txhua qhov xwm txheej, nws siv yuav tsum ua raws li kev cai lij choj thiab kev nyab xeeb.
Cim npe nrov: Yeej 35428 CAS 50370-56-4, cov neeg tsim khoom, chaw tsim khoom, Hoobkas, lag luam wholesale, yuav, nqe, loj, loj, rau muag