Isidakamizwa Esiphuthumayo Esilwa Nezifo Zase-Parkinson Kusukela Ekuqaleni
Imithi ebizwa ngokuthi i-dopamine agonists njenge-Requip (ropinirole) ne-Mirapex (pramipexole) isetshenziselwa ukuphatha izimpawu zesifo sika- Parkinson , ikakhulukazi ekuqaleni.
I-dopamine agonists ivame ukushiwo yizinzwa ze-neurologists njengendlela yokulula isikhathi esithatha ngaphambi kokuba umuntu aqale (noma akhulise) umthamo wabo we- levodopa .
I-Levodopa ingumuthi ophumelelayo kakhulu weParkinson, kodwa ukusebenza kwayo kunciphisa isikhathi eside somuntu onemithi.
Ngaphezu kokungaphansi kwe-levodopa ekwelapheni izimpawu zemoto , i-dopamine agonists ayenzi lutho lokunciphisa lesi sifo.
Lezi zinkinga zenze abacwaningi bakwazi ukuthuthukisa i-dopamine agonist, ebizwa ngokuthi i-D-512, engabonakali nje ephakeme kunezinye i-dopamine agonists ngokulawula izimpawu zezimoto kodwa ingavikela amangqamuzana e-nervous ekhona, okungenzeka abeke ama-brake kwisifo somuntu (okuphawulekayo feat).
Kubalulekile ukuqonda ukuthi u-D-512 usezigaba zokuqala zocwaningo. Eqinisweni, kufundwe kuphela ezilwaneni. Noma kunjalo, kuyisinyathelo esihle sokuqala ukuthola imithi elwa nesifo sikaParkinson kusukela ekuqaleni.
Sibutsetelo se-D-512
Isifo sikaParkinson sihilela ukulahlekelwa amangqamuzana omzimba we-dopamine endaweni yesimo sobuchopho okuthiwa i-substantia nigra.
Njengoba i-dopamine ingumuthi wezobuchopho (obizwa ngokuthi i-neurotransmitter) edingekayo ukuze umzimba uhambe, izimoto (ezihlobene nokuhamba) zivela ekulahlekeni lokhu.
Nakuba kunezibonakaliso eziningana zezimoto ezihlobene nesifo sikaParkinson, ezine ezikhazimulayo ziyizi:
- Ukuqeda ukuthuthumela
- I-Bradykinesia (ihlehliwe ikhono lokuhambisa)
- Ubuqotho
- Ukungazinzi kokuthunyelwe
Njengoba i-dopamine agonist, i-D-512 ibopha kuma-receptors, noma amasayithi wokungena, ebuchosheni. Ngokukhuthaza ngokuqondile lezi zitholampilo, u-D-512 ulingisa ubuchopho be-chemical dopamine (ngakho ubuchopho becabanga ukuthi bunomdopamine uma lungenjalo).
I-D-512 ihlukile kwamanye ama-agonists e-dopamine, noma kunjalo, ngoba ine-affinity ephezulu ye-dopamine receptors. Lokhu kusho ukuthi kungabopha kalula futhi kufinyelele ngokwengeziwe, okwenza kube isikhathi eside.
Ngaphandle kokuba nomunye ohlangothini oluphakeme lwe-dopamine receptors, i-D-512 ikholelwa ukuthi ivikela amangqamuzana omzimba we-dopamine asaphila, mhlawumbe ngokunciphisa ukucindezeleka kwe-oxidative (isici esiyinhloko esiya "kungani" ngemuva kwesifo sika-Parkinson). Ngokunciphisa ukucindezeleka kwe-oxidative, i-D-512 izocatshangwa ukuthi inezakhiwo ze-antioxidant.
Ngamanye amazwi, abacwaningi bakholelwa ukuthi i-D-512 ingaba yindlela yokwelapha isifo se-Parkinson ngoba inganciphisa ukuqhubeka kwayo.
I-Science Behind D-512: Ukufundwa Kwezilwane
Kwesinye isifundo eBritish Journal of Pharmacology, ubuchopho bezintuthwane kwafakwa 6-hydroxydopamine (i-dopamine neurotoxin ukulingisa isifo se-Parkinson kubantu). Khona-ke, amagundane anikezwa u-D-512 noma ahlomise (ropinirole), nemiphumela yafaniswa.
Imiphumela
Imiphumela yocwaningo yembula ukuphakama kobuchopho obuphezulu kanye negazi le-D-512 kune-ropinirole.
Ngaphezu kwalokho, ngenkathi kokubili i-D-512 ne-ropinirole yanda ukunyakaza okuzenzekelayo (kumagundane) kuya ezingeni elifanayo ngemva kokujova, isikhathi sokusebenza sensimbi sasisele u-D-512 kune-ropinirole.
Ngokuqondile, imiphumela ephikisana ne-Parkinsonia ye-ropinirole yahlala cishe amahora amabili kanti umphumela we-anti-Parkinsonian ka-D-512 waba khona okungenani amahora amane.
Imiphumela yecala: i-Dyskinesia
I-D-512 ibonwe ukuthi ibangele i-dyskinesia, kodwa ngokuqinela okufanayo njenge-Requip (ropinirole), kumagundane. I-Dyskinesia ibhekisela ekunyameni okungavamile njengokuncintisana noma ukukhipha okungaveli ekulawuleni komuntu.
Kubalulekile ukuphawula ukuthi nakuba ama-dyskinesias engumphumela ovamile ohlangothini lwe-levodopa, okwenzeka kuma-50 amaphesenti abantu abanesifo sika-Parkinson eminyakeni emihlanu, ajwayelekile kakhulu kubantu abathwala ama-dopamine agonists.
Eqinisweni, ucwaningo lwembula ukuthi i-dyskinesias, lapho umuntu ethatha i-dopamine agonists yedwa, kwenzeka emaphesenti angaba ngu-5 kuya kwangu-7 abantu abane-Parkinson-futhi uma kwenzeka i-dyskinesias, ngokuvamile ikhula ngamandla futhi ivele kamuva.
Ngaphansi
Konke, ama-dyskinesias akuyona inkinga enkulu kubantu abasebenzisa i-dopamine agonists yedwa (ngaphandle kwe-levodopa), ngakho-ke kusengenzeka kube ngcono isilinganiso somvuzo-side effect wokuthatha u-D-512, uma kuqhathaniswa namanye ama-agonist e-dopamine njenge-Requip (ropinirole) .
Khumbula, lokhu kuyisifundo sezilwane, ngakho kusenesikhathi kakhulu ukwenza iziphetho okwamanje. Okubalulekile lapha ukuthi imiphumela ye-D-512 idinga ukuhunyushwa ekusetshenzisweni komuntu.
I-Dopamine Agonists Nendima Yabo Ezingezona Izimpawu Zezimoto
Ngaphandle kokwelapha izimpawu zamagciwane esesifo sokuqala se-Parkinson, ubufakazi besayensi buveza ukuthi i-dopamine agonists izuzisa izimpawu ezingekho emotweni, ikakhulukazi izinkinga zemizwa ezifana nokukhathazeka, ukucindezeleka, kanye / noma ukunganakwa.
I-dopamine agonists ingase iphinde ithuthukise izinkinga ezithile ezizimele ezifana nomsebenzi wezocansi noma ukujuluka, kanye nezinkinga ezithile zokulala esifundeni sikaParkinson njenge-syndrome yokungenalutho noma ukuhlukana kokulala.
Lokhu kuthembisayo, njengoba ochwepheshe begxila kakhulu ezimpawu ezingezona izimoto, njengoba zivame ukuqala ngaphambi kwezimpawu zezimoto futhi zingadambisa.
Lokho kusho, akucaci ukuthi ngabe i-D-512 ingaba yini ephakeme kunama-agonist yendabuko njenge-Requip (ropinirole) noma iM Mirapex (pramipexole) ekunciphiseni lezi zimpawu ezingezona izimoto.
Izwi elivela
Esifundweni sesilwane esishiwo, inzuzo enkulu kakhulu ye-D-512 ngaphezu kokuhlomisa (i-ropinirole) ukuthi ihlala isikhathi eside futhi ingcono kumphumela wayo wokuphakama.
Noma kunjalo, kudingekile izifundo ezengeziwe ukuqonda kangcono uma i-compound efana no-D-512 ingcono ngempela kunamanje ama-agonists amanje okwelapha abantu abane-Parkinson.
Ngaphandle kwezimpawu zamagciwane nemiphumela emibi, ezinye izinto kudingeka zibhekwe njengekhwalithi yokuphila yomuntu, isikhathi sihlehliselwe ukuqala i-levodopa, nokuthi ngabe i-D-512 ishintshe ngempela yini isifo (ingabe ingavikela amaseli we-nerve producing producing ukuhlala).
> Imithombo:
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> Lindenbach D, Das B, Conti MM, Amapheshana SM, uDutta AK, uMbhishobhi C. D-512, i-dopamine entsha ye-dopamine D2 / 3 i-agonist receptor, ibonisa ukusebenza kwama-greate anti-Parkinsonian kune-ropinirole kumaRats ePinsinsonian. Br J Pharmacol. 2017 Sep; 174 (18): 3058-71.
> Poewe W et al. I-pramipexole enwetshiwe ekuqaleni kwesifo se-Parkinson: isilingo esingama-33 esingama-random esilawulwa ngokungahleliwe. I-Neurology. 2011 Aug 23; 77 (8): 759-66.
> UMichael J. Fox Foundation For Research's Parkinson. D-512: i-Noveli, i-Multifunctional D2 / D3 Umamukeli we-Agonist we-Treatment of the Parkinson's.
> Schaeffer E, Berg D. Dopaminergic zokwelapha izimpawu ezingezona izimoto zesifo sikaParkinson. I-CNS Izidakamizwa . 2017 Jul; 31 (7): 551-70.