Pramipexole hmoov, tseem hu ua Mirapa, yog ib qho dawb rau kev ua hmoov dawb-dawb, feem ntau nyob rau hauv daim ntawv ntawm hydrochloride monohydrate). Cov mis molecular yog c10h17n3s, cas 104632-26-0}}, thiab cov molecular hnyav yog 211.33 G / Mol. Feem ntau nyob rau hauv daim ntawv ntawm hydrochloride. Nyob rau hauv nws cov qauv tshuaj, nws yog tsuas yog tsim ntawm amphetamine qauv thiab thataminophenylamine, uas yog cov koob sib txuas ntawm thataminophenethylamine nyob rau ntawm amphetamine. Tsis meej, me ntsis iab, yooj yim soluble hauv dej, yuav luag insoluble hauv cov kuab tshuaj ethanol thiab crystal hydrate tsis ruaj khov nyob rau hauv huab cua. Pramipexole yog ib qho tshuaj antihistamine uas yog tsuas yog siv tsev kho mob los kho tus kab mob Parkinson thiab nws cov syndromes. Yuav siv tau ib leeg lossis ua ke nrog levodopa.
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Tshuaj Cov Qauv |
C10H17N3S |
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Muaj pes tsawg leej |
211 |
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Molecular hnyav |
211 |
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m/z |
211 (100.0%), 212 (10.8%), 213 (4.5%), 212 (1.1%) |
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Kev Ntsuam Xyuas |
C, 56.84; H, 8.11; N, 19.88; S, 15.17 |
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Pramipexole hmoov, tseem hu ua prasubrelor, yog qhov tsis-carbamine recept agonist siv dav hauv kev kho tus kab mob Parkinson thiab lwm yam kev tawm tsam. Ib qho ntxiv, nws tseem siv nyob rau hauv kev kho mob ntawm lwm yam kab mob, suav nrog kev ntxhov siab, kev ntxhov siab nrog kev ntxhov siab, Alzheimer tus kab mob thiab ntau yam kev tsis txaus ntseeg.
1. Kev kho mob ntawm Parkinson tus mob:
Qhov kev siv ntau tshaj plaws ntawm PramipeXole yog kho tus kab mob Parkinson, lub hauv paus loj plawv tsis sib haum xeeb los ntawm kev txhav, tshee, thiab kev ploj zuj zus. Prepipexole nce dopamine qib los ntawm kev txhawb nqa dopamine receptors hauv lub hlwb, yog li txo cov tsos mob ntawm cov kev tawm tsam hauv Parkinson tus mob tus mob. Cov kev sim kuaj mob tau qhia tias Pramipleexole zoo zoo relieves ob lub cev muaj zog thiab cov neeg muaj zog hauv Parkinson tus kab mob.
2. Kev kho mob ntawm ntau lub zog tsis txaus ntseeg:
Ntxiv rau Parkinson tus kab mob, PreMiplexole kuj tau siv los kho ntau yam kev txav mus los lwm yam kev ntxhov siab, xws li cov chorea tshee, myoclonus thiab dystonia. Pramipexole qhia cov peev txheej hauv kev cuam tshuam cov tsos mob ntawm cov kev sib tsoo no.
3. Kev kho mob ntxhov siab:
Pramipexole kuj tseem siv los saib xyuas me me rau kev ntxhov siab nruab nrab. Cov kev sim kuaj mob tau pom tias kev ua neeg muaj zog uas muaj cov txiaj ntsig thiab cov txiaj ntsig ntev dua benzodiazepines, thiab nws kuj txhim kho cov tsos mob ntxhov siab.
4. Kev kho mob ntawm kev ntxhov siab:
Pramipexole kuj tau pom muaj peev xwm los kho kev nyuaj siab. Cov chaw kuaj mob tau ua pov thawj tias Pramipexole tuaj yeem txhim kho kev nyuaj siab ntawm cov neeg mob thiab txo cov kev nyuaj siab, tab sis nws yuav tsum tau sau tseg, thiab qee cov neeg mob yuav muaj kev cuam tshuam tsis zoo.
5. Kev kho mob ntawm kev nyuaj siab nrog kev ntxhov siab:
Pramipexole kuj tseem siv los kho kev ntxhov siab hauv cov neeg mob uas muaj kev ntxhov siab. Cov chaw kuaj mob tau ua pov thawj tias Pramiplexole tuaj yeem txo qis cov tsos mob ntawm kev nyuaj siab thiab ntxhov siab, thiab txhim kho lub neej zoo ntawm cov neeg mob.
6. Kev kho mob ntawm Alzheimer tus kab mob:
Pramipexole kuj tau pom muaj peev xwm nyob rau hauv kev kho mob ntawm Alzheimer tus kab mob. Cov chaw kuaj mob tau pom tias cov tshuaj muaj cov txiaj ntsig zoo ntawm kev txhim kho kev ua haujlwm, txhim kho cov tsos mob zoo xws li ua kom zoo nkauj xws li ua rau cov khoom zoo xws li kev ua yeeb yam zoo xws li kev ua yeeb yam zoo xws li kev ua yeeb yam. Txawm li cas los xij, nws cov kev tshawb pom tau tsis sib xws, thiab xav tau kev tshawb fawb ntxiv kom paub meej tias nws txoj kev ua tau zoo.
7. Kev kho mob ntawm ntau yam kev tawm tsam hnyav hnyav:
Pramipexole kuj tseem siv los kho ntau yam kev cuam tshuam ntawm lwm yam kev lom zem neurological xws li akathisia thiab tej tentastic torticollis. Cov chaw sim khomob tau ua pov thawj tias Preenaspole tuaj yeem daws cov tsos mob ntawm cov kab mob no thiab txhim kho lub neej zoo ntawm cov neeg mob.
Pramipexole yog qhov tsis-carbamine receptor agonist siv dav hauv kev kho tus kab mob Parkinson thiab lwm yam kev tawm tsam.
Cov hauv qab no yuav qhia ntau txoj kev ntawm cov khoom siv hluavtaws ntawmpramipexole hmoovLos ntawm cov kev pom ntawm tshuaj schthesis.
1. Pyridine Qauv Synthesis:
Pyridine txoj kev synthesis yog cov txheej txheem ntxov tshaj plaws los nrhiav cov Premiplexole. Cov kauj ruam tshwj xeeb yog raws li hauv qab no:
Kauj ruam 1: Kev tawm tsam ntawm Styrene thiab Pyridine hauv Dioethyl succinate muab n-phenyl - - styrypropnoinine.
Kauj Ruam 2: Ntxiv TetrahyDrofuran rau cov tshuaj tiv thaiv kab mob hauv kauj ruam 1, ces maj mam ntxiv c. Kom tau txais n-pheny} ({5}} formylpheny.
Kauj Ruam 3: Ua kom cov khoom lag luam hauv Kauj Ruam 2 nrog pyridine hydroxide tov los ua tus nqi PH ncav cuag txog 14, thiab tau pramipexole tom qab ziab kom qhuav.
Txoj kev no yog qhov yooj yim rau cov synthesize, tab sis kev npaj ntawm nruab nrab 1 yog qhov nyuaj thiab tawm tau yog qhov muaj txiaj ntsig ntxiv.
2. Synthesis los ntawm isotope sib pauv qauv:
Synthesis los ntawm isotope sib pauv qauv yog ib txoj kev uas siv cov kev ua kom zoo los hloov cov nitrogen atom hauv molecule, yog li npaj preamipexole. Cov kauj ruam tshwj xeeb yog raws li hauv qab no:
Kauj Ruam 1: Cov tshuaj tiv thaiv ntawm N-Phenyl {{2} inechdreg acid nrog TrifhluorShanesulffonic animlsulforSulforShande muaj peev xwm n-pheny dibl triflate.
Kauj Ruam 2: Rov qab cov khoom hauv Kauj Ruam 1 nrog sodium hydroxide tov, tom qab ntawd ntxiv rau hauv lub tshuab nqus dej kom tau txais n-pheny}}} trideuterophenyl) propylamine.
Kauj ruam 3: Condensate cov khoom lag luam hauv Kauj Ruam 2 nrog pyridine hydroter hydroxide kom ua rau tus nqi PH ncav cuag txog 14, thiab tau pramipexole los ntawm lub tshuab nqus tsev qhuav.
Cov synthesis ntawm no txoj kev no tseem yooj yim, tab sis nws yuav tsum tau siv cov dej hnyav, yog li nws yog qhov yuav tsum tau them sai sai rau kev ua haujlwm kom nyab xeeb.
Lub tshuab kev ua ntawm pramipexole
Pramipexole, tseem hu ua Pramiplexole hydrochloride, yog cov tshuaj siv los kho cov kev tsis txaus ntseeg neurological, tshwj xeeb yog qhia cov txiaj ntsig tseem ceeb hauv kev kho mob ntawm Parkinson tus kab mob. Raws li Dopamine receptor agonist, cov tshuab kev ua ntawm pramipexole yog complex thiab intricate, cuam tshuam nrog ntau cov txheej txheem muaj sia thiab pathological.
Cov yam ntxwv yooj yim ntawm PreMipexole
Pramipexole yog ib qho tshuaj uas artificialized nrog ib tug xaiv tau heev thiab cov qauv tshuaj tshwj xeeb uas tuaj yeem khi khi rau lub hom phiaj receptor. Raws li Dopamine receptor agonist, pramipole feem ntau ua rau Dopamine D2 thiab D3 receptor, yog li simulating lub cev muaj nuj nqis ntawm dopamine. Qhov kev xaiv khi no thiab cov nyhuv zoo siab muab kev ua kom muaj txiaj ntsig tshwj xeeb hauv kev kho kev cuam tshuam ntawm neurological xws li Parkinson tus kab mob.
Lub tshuab kev ua ntawm pramipexole
Lub tshuab ntawm kev ua ntawm pramipexole feem ntau suav nrog cov hauv qab no:
1. Dopamine receptor agonistic cuam tshuam:
(1) D2 Receptor ua kom tiav:
Thaum pramipexole khi rau D2 receptor, nws tuaj yeem qhib dopamine kos npe rau hauv Parkinson cov neeg mob cov kab mob. D2 Receptors ua si lub luag haujlwm tseem ceeb hauv kev tswj hwm cov leeg nqaij, lub cev muaj zog tswj, thiab kev sib koom tes. PreMipexole activates D2 cov receptors, txo cov leeg nqaij nce siab, txo cov leeg leeg txhav txhav txhav txhav, thiab txhim kho cov cev muaj zog thiab kev sib koom tes.
(2) d3 receptor prefinity:
Pramipexole muaj ib tug muaj affinity rau D3 receptor, uas ua rau nws muaj lub hom phiaj zoo rau kev kho cov kab mob Parkinson. D3 receptors ua si lub luag haujlwm tseem ceeb hauv kev tswj hwm kev xav, kev txawj ntse, thiab cov nqi zog. Premipexole yuav pab txhim kho kev puas tsuaj, kev xav hloov pauv, thiab kev nyuaj siab cov tsos mob hauv Parminson tus mob tus mob los ntawm kev ua kom cov D3 receptors.
2. Neuroprotective nyhuv:
(1) Inhibition ntawm oxidative kev nyuaj siab:
Pramipexole yuav txo cov kev puas tsuaj ntawm cov neeg neuronal los ntawm kev tiv thaiv oxidative oxidative cov lus teb. Oxidative kev ntxhov siab yog ib qho tseem ceeb hauv Parkogenesis ntawm Pargid Peroxidation, protein oxidation, thiab DNA kev puas tsuaj ntawm neuronal weef. Pramipexole tiv thaiv neurons los ntawm kev puas tsuaj los ntawm kev txo cov khoom ntawm oxidative cov khoom lag luam.
(2) Txo cov xov tooj ntawm tes)
Pramipexole kuj tseem tuaj yeem tiv thaiv cov neurons los ntawm inhibiting lub apoptotic txoj kev. Apoptosis yog ib daim ntawv ntawm neuronal tuag uas yog ze ze rau kev nce qib ntawm cov kab mob nev xws li Parkinson tus kab mob. Pramipexole inhibits neuronal apoptosis los ntawm kev tswj hwm qhov kev qhia ntawm Apoptosis ntsig txog cov noob.
3. Kev tswj hwm neurotransmitter tshuav nyiaj li cas:
(1) qhov sib npaug ntawm dopamine thiab lwm cov neurotransmitters:
Pramipexole tuaj yeem tswj qhov sib npaug ntawm dopamine thiab lwm cov neurotransmitters (xws li acetylcholine). Qhov nyiaj tshuav no yog qhov tseem ceeb rau kev tswj hwm cov haujlwm ib txwm muaj ntawm lub paj hlwb. Cov neeg mob uas ua yeeb ncuab ua si tau txo cov kev ua haujlwm hauv chaw nres tsheb, ua rau txheeb ze hyperactivity ntawm neurotransmitters xws li acetylcholine. Pramipexole txhim kho cov neurological discorders los ntawm kev nce siab ntawm dopamine thiab txo lub xeev siab ntawm acetylcholine.
(2) Txhim kho cov neuronal muaj nuj nqi:
Pramipexole kuj tseem tuaj yeem txhim kho cov ciaj sia taus thiab ua haujlwm ntawm neurons. Pramipexole pab rov qab ua haujlwm li qub ntawm cov neurons puas los ntawm kev txhawb nqa lawv txoj kev loj hlob thiab kev sib txawv, thiab txhim kho lawv lub peev xwm metabolic.
4. Cuam tshuam rau cov teeb meem hloov chaw:
(1) tswj cov neuronal expitability:
Pramipexole txhim kho txoj haujlwm ntawm lub paj hlwb los ntawm kev tswj hwm qhov kev txaus siab thiab inhibitory signing ntawm neurons. Qhov kev tswj hwm cov txiaj ntsig no pab tswj cov kev nquag ntawm neural tes hauj lwm, txo qhov tshwm sim ntawm kev tsis txaus siab thiab kev ua si synchronous ntawm neurons.
(2) Txhim kho qhov sib npaug tsis zoo:
Pramipexole tuaj yeem tswj txoj kev ua haujlwm ntawm Ganglia ntawm lub hlwb thiab txhim kho kev sib npaug tshwm sim los ntawm Parkinson tus kab mob. Qhov no pab cov neeg mob tswj kom muaj kev pheej hmoo thiab gait, txo qis kev pheej hmoo ntawm kev poob.
Tshuaj Lom Zempramipexole hmoovMuaj ntau cov chaw nquag xws li pawg amine, carbonyl pawg thiab pyridyl pab pawg, thiab tuaj yeem nqa tawm ntau yam tshuaj lom neeg cov kev txiav txim siab.
(1) Cov tshuaj tiv thaiv hydrogen atom ntawm lub carbonyl txoj hauj lwm hauv pramipyl
(2) Nucleophilic hloov cov nitrogen atom ntawm pyridine Ring hauv Premleople, thiab Nucleophilic hloov tshwm sim los tsim cov khoom hloov pauv hloov.
(3) Kev tawm cov tshuaj tiv thaiv pamipexole tuaj yeem yauv txo cov tshuaj tiv thaiv nyob hauv lub xub ntiag ntawm tus neeg sawv cev txo cov khoom lag luam kom tsim cov khoom.
(4) Kev Tiv Thaiv Cov Khoom Siv Amine Group thiab CarbonyL Pawg hauv PreGiplexole tuaj yeem tiv thaiv cov khoom hws hws sib haum.
Kev ruaj khov Pramipexole yog qhov ruaj khov nyob rau hauv chav tsev kub, thiab decompose nyob rau hauv ib co huab cua sov xws li kub siab, thiab oxidizing cov neeg sawv cev. Yog li ntawd, kev saib xyuas yuav tsum tau coj los tiv thaiv cov ntsiab lus tsis txaus ntseeg thaum lub sij hawm npaj, cia thiab siv.
Cim npe nrov: Pramipexole hmoov cas {{104632-26-0, cov chaw muag khoom, chaw tsim khoom, Hoobkas, yuav, nqe, loj, rau muag