D-512: Inogona Kuita Dopamine Agonist yePasinson

Imwe Mishonga Investigational Inotambudza Kurwara kwaPasinson Kubvira Pakutanga

Mishonga inonzi dopamine agonists seRequip (ropinirole) uye Mirapex (pramipexole) inowanzoshandiswa kurapa zviratidzo zvehosha yaPasinson , kunyanya mumatanho ekutanga.

Dopamine agonist inowanzotarisirwa neurologist sezvimwe nzira yekuwedzera nguva inotora munhu asati atanga (kana kuwedzera) muzana wavo wevodopa .

Levodopa ndiyo mishonga inobatsira zvikuru yePacinson, asi kubudirira kwayo kunoderedza nguva refu munhu ari pamishonga.

Mukuwedzera pakuva pasi peevodopa mukurapa zviratidzo zvemotokari , dopamine agonist haiti chinhu chinogona kuderedza chirwere chacho.

Izvi zvakashamisa vatsvakurudzi kuvaka dopamine agonist, inonzi D-512, iyo isingori kuoneka yakakwirira pane dzimwe dopamine agonist maererano nekugadzirisa zviratidzo zvemotokari asi inogona kudzivirira masero emagetsi aripo, zvichida kuisa mabheki pachirwere chomunhu (inoshamisa feat).

Zvakakosha kunzwisisa kuti D-512 iri mumapato ekutanga ekutsvakurudza. Chaizvoizvo, zvinongodzidzwa mhuka. Kunyange zvakadaro, iri danho rakanaka rekutanga kune kuwana mishonga inorwisa zvirwere zvePasinson kubva pakutanga.

Kuratidzwa kweD-512

Chirwere chePacinsinson chinosanganisira kurasikirwa kwema-cell-producing-cells cells munzvimbo yeuropi inonzi substantia nigra.

Sezvo dopamine ikemikari yomuuropi (inonzi neurotransmitter) iyo inodiwa kuti muviri upfuurire, motokari (inoenderana-kufamba) zviratidzo zvinobva pakurasikirwa uku.

Nepo kune huwandu hwemotokari dzinofananidzwa nehosha yaPasinson, vana makadhiina ndevokuti:

Sezvo dopamine agonist, D-512 inosunga kune dopamine receptors, kana nzvimbo dzekuvhara, muuropi. Nokuratidza zvakananga izvi zvinogamuchirwa, D-512 inofananidza neuropi yemakemikari dopamine (saka uropi inofunga kuti ine dopamine kana ichokwadi haisi).

D-512 yakasiyana nedzimwe dopamine agonists, kunyange zvakadaro, nokuti ine hukama hwepamusoro hwe dopamine receptors. Izvi zvinoreva kuti inogona kusunga zviri nyore uye zvakasimba zvakasimba, izvo zvinoita kuti igare kwenguva refu.

Mukuwedzera pakuva nehukama hwepamusoro hwe dopamine receptors, D-512 inofungidzirwa kuti inodzivirira dopamine-inobudisa masero emasero achiri kurarama, zvichida nekuderedza kushushikana kwehutachiona (chinhu chinokosha kune "nei" seri kwechirwere chePasinson). Nokuderedza kusagadzikana kweakisidi, D-512 yaizoonekwa seine antioxidant.

Mune mamwe mazwi, vatsvakurudzi vanodavira kuti D-512 inogona kuva chirwere chinoshandura zvirwere zvePalinson's disease nokuti inogona kuderedza kuwedzera kwayo.

Sayenzi Pasi D-512: Chidzidzo cheMhuka

Mune rumwe ruzivo muBritish Journal of Pharmacology, ubongo hwehave hwakakonzerwa ne 6-hydroxydopamine (a dopamine neurotoxin kutevedzera chirwere chePasinson mumunhu). Zvadaro, makonzo akapiwa D-512 kana kuti Requip (ropinirole), uye migumisiro yakaenzaniswa.

Mhinduro

Zvidzidzo zvidzidzo zvakaratidza huro hwepamusoro hutachiona uye ropa reD-512 kupfuura ropinirole.

Uyezve, apo zvose D-512 uye ropinirole zvakanyanya kufambira mberi (mumakonzo) kune imwe yero yepamusoro apo mushure mejisi, nguva yekubvambiswa kwemoto yakanga yakareba kweD-512 kupfuura ropinirole.

Kunyanya zvakanyanya, mishonga inopesana nePasinsinoni yeR ropinirole yakaguma kwemaawa maviri chete asi simba reAn anti-Parkinsonian raD-512 rakagara kwemaawa mana.

Nzira Yechikamu: Dyskinesia

D-512 yakaonekwa kuti inokonzera dyskinesia, asi kuoma kwakanyanya seRequip (ropinirole), mumakonzo. Dyskinesia inoreva kusvibiswa kusingadikanwi kwakafanana nekukwikwidza kana kukanganisa izvo zvisingabvi mumunhu.

Zvakakosha kucherechedza kuti nepo dyskinesias inowanzobatana nehutachiona hweLevodopa, inowanikwa mumapfumbamwe makumi mashanu evanhu vane chirwere chePasinson mumakore mashanu, ivo havasati vashoma kune vanhu vanotora dopamine agonist.

Kutaura zvazviri, kutsvakurudza kunoratidza kuti dyskinesias, apo munhu ari kutora dopamine agonist chete, anoitika munenge 5 kusvika ku7 muzana yevanhu vane Parkinson-uye kana dyskinesias ichiitika, inowanzova yakaoma mukuoma uye inoitika gare gare.

Pasi Pasi

Zvose mune zvose, dyskinesias haisi dambudziko guru kune vanhu vanotora dopamine agonist chete (pasina levodopa), saka kune imwe nguva inogona kunge yakagadziriswa-yechirongwa chekubata D-512, kana ichienzaniswa nedzimwe dopamine agonist seRequip (ropinirole) .

Yeuka, ichi chidzidzo chemhuka, saka zvakakurumidza kuti zviite zvisarudzo zvakadaro. Chinokosha apa ndechekuti migumisiro yeD-512 inoda kushandurwa mukushandiswa kwevanhu.

Dopamine Agonist uye Basa Ravo MuHasina-Mumiriridzo

Mukuwedzera pakurapa zviratidzo zvemotokari mu chirwere chepachivande chePasinson's, uchapupu hwezvesayenzi hunoratidza kuti dopamine agonist inobatsira zviratidzo zvisiri-motokari, kunyanya zvinetso zvepfungwa zvakadai sokuzvidya mwoyo, kuora mwoyo, uye / kana kusava nehanya.

Dopamine agonist inogonawo kugadzirisa zvimwe zvinetso zvekuzvidzivirira zvakadai sekuita zvepabonde kana kutuka, uyewo matambudziko chaiwo ekurara muhosha yaPasinson sekusununguka kwemagumbo kana kuti kuparara kwekurara.

Izvi zvinopikira, sezvo nyanzvi dziri kutarisa zvakanyanya uye zvakanyanya pane zviratidzo zvisiri-motokari, sezvavanowanzotangira mberi kupfuura zviratidzo zvemuviri uye zvinogona kuora mwoyo.

Izvo zvakati, hazvina kujeka kana D-512 ingave yakakosha kudarika dopamine agonist seRequip (ropinirole) kana Mirapex (pramipexole) mukugadzirisa zviratidzo izvi zvisiri mhepo.

Shoko Rinobva

Muchidzidzo chemhuka chakataurwa, ruzivo rukuru rweD-512 pamusoro peRquip (ropinirole) nderokuti runogara kwenguva refu uye zviri nani pakureba kwayo.

Kunyange zvakadaro, zvidzidzo zvakawanda zvinodikanwa kuti zvive nani kunzwisisa kana chidimbu chakafanana neD-512 chiri nani kupfuura ikozvino dopamine agonist yekurapa vanhu naPasinson.

Kunze kwezviratidzo zvemotokari nemigumisiro, zvimwe zvikonzero zvinofanirwa kuonekwa sehupenyu hwomunhu, nguva inotarirwa kutanga kutora levodopa, uye kana D-512 ichokwadi zvirwere-kuchinja (inogona kuchengetedza dopamine-inobudisa masero emasero achiripo kurarama).

> Sources:

> Batla A, Stamelou M, Mencacci N, Schapira AH, Bhatia KP. Ropinirole monotherapy inokonzera zvakanyanya kuderedzwa dyskinesias muhosha yaPasinson. Mov Disord . 2013 Jul; 28 (8): 1159-60.

> Lindenbach D, Das B, Conti MM, Meadows SM, Dutta AK, Bishop C. D-512, nhau dopamine D2 / 3 receptor agonist, inoratidza girasi inopesana nePasinsinsonian inobudirira kupfuura ropinirole muRatsinsonian rats. Br J Pharmacol. 2017 Sep; 174 (18): 3058-71.

> Poewe W et al. Extended-release pramipexole mukutanga kwePasinsonon: chirwere chemavhiki makumi matatu nemakumi matatu. Neurology. 2011 Aug 23; 77 (8): 759-66.

> Michael J. Fox Nheyo yePilinson's Research. D-512: ANew, Multifunctional D2 / D3 Receptor Agonist nokuda kweKurapwa kwezvirwere zvePasinson.

> Schaeffer E, Berg D. Dopaminergic mishonga yevasiri zviratidzo zvepachirwere chePasinson. CNS Zvinodhaka . 2017 Jul; 31 (7): 551-70.