Dithethefatsi Tse Senyang Lipatlisiso Tse Amanang le Maloetse a Parkinson ho tloha Tšimolohong
Meriana e bitsoang dopamine agonists e kang Requip (ropinirole) le Mirapex (pramipexole) e atisa ho sebelisoa ho phekola matšoao a lefu la Parkinson , haholo-holo matsatsing a pele.
Li-agonists tsa Dopamine hangata li laeloa ke litsebi tsa methapo ea mafu ka mokhoa oa ho lelefatsa nako eo motho a lokelang ho e qala pele kapa ho eketsa lebelo la levodopa .
Levodopa ke eona meriana e sebetsang ka ho fetisisa bakeng sa Parkinson, empa katleho ea eona e fokotseha ha motho e mong a se a le meriana.
Ntle le ho ba tlase ho levodopa ho phekola matšoao a likoloi , dopamine agonists ha e etse letho ho fokotsa lefu lena.
Ts'ebetso ena e entse hore bafuputsi ba hlahise mofuta o mocha oa agonist, o bitsoang D-512, o sa hlaheleng o phahametse tse ling tsa li-agonists ka ho laola lisebelisoa tsa motlakase empa o ka sireletsa lisele tse nang le methapo ea mmele, e ka 'nang ea beha marake holim'a lefu la motho (e tsotehang feat.
Ke habohlokoa ho utloisisa hore D-512 e mekhahlelo ea pele ea lipatlisiso. Ha e le hantle, e 'nile ea ithutoa liphoofolong. Leha ho le joalo, ke mohato o motle oa ho fumana meriana e loantšang lefu la Parkinson ho tloha qalong.
Tlhaloso ea D-512
Boloetse ba Parkinson bo amana le ho lahleheloa ke lisele tsa meriana tse hlahisang dopamine sebakeng sa boko se bitsoang substantia nigra.
Kaha dopamine ke lik'hemik'hale tsa boko (tse bitsoang neurotransmitter) tse hlokahalang bakeng sa 'mele hore o tsamaee, matšoao a amanang le ho tsamaea a tsoa ho tahlehelo ena.
Le hoja ho na le matšoao a mangata a motlakase a amanang le boloetse ba Parkinson, makhadiana a mane a:
- Ho thothomela
- Bradykinesia (e fokotseha bokhoni ba ho falla)
Joaloka dopamine agonist, D-512 e tlama ho dopamine receptors, kapa libaka tsa ho koala, bokong. Ka ho hlasimolla li-receptor tsena ka ho toba, D-512 e etsisa lik'hemik'hale tsa dibamine tsa boko (kahoo boko bo nahana hore bo na le dopamine ha e hlile e se).
D-512 e fapane le li-agonists tse ling tsa dopamine, leha ho le joalo, hobane e na le kamano e phahameng ea dopamine receptors. Sena se bolela hore se ka tlamisa habonolo mme se tiile haholo, se etsang hore se tšoarelle nako e telele.
Ntle le ho ba le kamano e phahameng ea li-receptor, D-512 ho lumeloa hore e sireletsa lisele tsa meriana tse hlahisang dopamine tse ntseng li phela, mohlomong ka ho fokotsa khatello ea mali (e leng ntho ea bohlokoa ho "hobane'ng" ka mor'a lefu la Parkinson). Ka ho fokotsa khatello ea lik'hemik'hale, D-512 e tla nkoa e na le li-antioxidant.
Ka mantsoe a mang, bafuputsi ba lumela hore D-512 e ka ba phekolo ea ho fetola mafu bakeng sa lefu la Parkinson hobane e ka fokotsa tsoelo-pele ea eona.
The Science Behind D-512: Thuto ea Liphoofolo
Phuputsong e 'ngoe British Journal ea Pharmacology, boko ba likhoto bo ile ba kenngoa ka 6-hydroxydopamine (dopamine neurotoxin ho etsisa lefu la Parkinson ho batho). Joale, likhooe li ile tsa fuoa D-512 kapa tsa hlomella (ropinirole), 'me liphello tsa bapisoa.
Liphetho
Liphello tsa thuto li senola hore boko bo phahameng bo fumanoa le ho feta D-512 ea mali ho feta ropinirole.
Ho phaella moo, ha D-512 le ropinirole li eketseha ka tsela e itekanetseng (ka likhoto) ho ea ka tekanyo e tšoanang hang ka mor'a hore e entsoe, nako ea nako ea ho kenya motlakase e ne e le telele bakeng sa D-512 ho feta ropinirole.
Ka ho khetheha, liphello tse khahlanong le Parkinsonia tsa ropinirole li qetile lihora tse ka bang peli feela empa phello ea anti-Parkinsonian ea D-512 e nka bonyane lihora tse 'nè.
Phello e Ntle: Dyskinesia
D-512 e ne e hlokomeloa hore e baka dyskinesia, empa ka matla a tšoanang le a Requip (ropinirole), ka likhoto. Dyskinesia e bolela ho sisinyeha ho sa tloaelehang ho kang ho kenyelletsa kapa ho senya ho se nang taolo ea motho.
Ke habohlokoa ho hlokomela hore le hoja dyskinesias e le phello e tloaelehileng ea levodopa, e hlahelang hoo e ka bang karolo ea 50 lekholong ea batho ba nang le lefu la Parkinson ka lilemo tse hlano, ha ba tloaelehe haholo ho batho ba nkang li-agonists tsa dopamine.
Ha e le hantle, lipatlisiso li senola hore li-dyskinesias, ha motho a nka li-agonists feela, li etsa karolo ea 5 ho ea ho 7 lekholong ea batho ba nang le Parkinson-'me haeba li-dyskinesias li etsahala, hangata li matlafala ka matla 'me lia etsahala hamorao.
Ntho e ka tlaase
Ha e le hantle, dyskinesias hase bothata bo boholo ho batho ba nkang dopamine agonists feela (ntle le levodopa), ka hona ho ntse ho ka etsahala hore ebe ho na le phalliso e ntlafetseng ea liphello tsa ho nka D-512, ha e bapisoa le li-agonists tse ling tsa Dopamine joaloka Requip (ropinirole) .
Hopola, ena ke thuto ea liphoofolo, kahoo e mathoasong haholo ho etsa liqeto leha ho le joalo. Ntlha ea bohlokoa mona ke hore liphello tsa D-512 li hloka ho fetoleloa ho sebelisoa ha batho.
Dopamine Agonists le Boikarabello ba Ts'ebetsong e sa Bitsoang Matšoao
Ho phaella tabeng ea ho phekola matšoao a koloi setsing sa pele sa Parkinson, bopaki ba saense bo fana ka maikutlo a hore dopamine agonists e na le matšoao a se nang motlakase, haholo-holo mathata a maikutlo a kang ho tšoenyeha, ho tepella maikutlong le / kapa ho iphapanyetsa.
Li-agonists tsa Dopamine li ka boela tsa ntlafatsa mathata a itseng a boipheliso a kang ho sebetsa ka thobalano kapa ho fufuleloa, hammoho le mathata a itseng a boroko matšoao a Parkinson joaloka lefu la leoto la phomolo kapa ho arohana ha lesifa.
Sena se tšepisa, kaha litsebi li lebisa tlhokomelo le ho feta ka matšoao a se nang motlakase, kaha hangata li qala pejana ho matšoao a likoloi 'me li ka fokolisa.
Seo se bolela hore D-512 e ne e tla ba ea phahametseng mekhoa ea bo-ralinine ea dopamine joaloka Requip (ropinirole) kapa Mirapex (pramipexole) ho fokotsa matšoao ana a se nang motlakase.
Lentsoe le Tsoang ho
Thupong ea liphoofolo e boletsoeng, phaello e kholo ka ho fetisisa ea D-512 ho feta ho Requip (ropinirole) ke hore e nka nako e teletsana ebile e molemo ha phello ea eona e fihla.
Leha ho le joalo, ho hlokahala lithuto tse eketsehileng ho utloisisa habonolo haeba motsoako o kang D-512 o hlile o molemo ho feta mehleng ea kajeno ea bo -agonist ea ho phekola batho ka Parkinson.
Ntle le matšoao a motlakase le litla-morao, lintlha tse ling li lokela ho nkoa e le boleng ba bophelo ba motho, nako e khutliselitsoeng ho qala levodopa, le hore na D-512 e hlile e fetola mafu (e ka sireletsa lisele tsa meriana tse hlahisang dopamine tse ntseng li le teng phela).
> Mehloli:
> Batla A, Stamelou M, Mencacci N, Schapira AH, Bhatia KP. Ropinirole monotherapy e baketse dyskinesias e matla e ts'oanelang ho hlaseloa ke lefu la Parkinson. Mov Disord . 2013 Jul; 28 (8): 1159-60.
> Lindenbach D, Das B, Conti MM, Meadows SM, Dutta AK, Mobishopo C. D-512, buka e ncha ea dopamine D2 / 3 ea batho ba amohelang likokoana-hloko, e bonts'a katleho ea mefuta e mengata ea mefuta e mengata ho feta ropinirole likhoto tsa Parkinsonian. Br J Pharmacol. 2017 Sep; 174 (18): 3058-71.
> Poewe W et al. Phoso e fetisitsoeng ea lefu la pele la Parkinson: teko ea libeke tse 33 e laoloang ka nako e telele. Neurology. 2011 Aug 23; 77 (8): 759-66.
> Michael J. Fox Motheo oa Phuputso ea Parkinson. D-512: Ntho e Ncha, Multifunctional D2 / D3 Receptor Agonist bakeng sa Phekolo ea Maloetse a Parkinson.
> Schaeffer E, Berg D. Dopaminergic ea phekolo ea mafu a se nang motlakase mafu a Parkinson. CNS Lithethefatsi . 2017 Jul; 31 (7): 551-70.