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Ho notlolla Monyetla oa Coluracetam: Ho Ntlafatsa Mosebetsi oa Kelello le Ho Laola Matšoenyeho

/Blog/Gallery/Ho notlolla Monyetla oa Coluracetam: Ho Ntlafatsa Mosebetsi oa Kelello le Ho Laola Matšoenyeho

Posted on by o ngotse Gallery.
Coluracetam
" Coluracetam (BCI-540, eo hape e tsejoang e le MKC-231) ke nootropic ea racetam-class-fat-soluble nootropic. Coluracetam e matla ho feta Piracetam, racetam ea pele. Mitsubishi Tanabe Pharma ea Japane e nang le patented coluracetam ka 2005. Ka hona ke e 'ngoe ea li-nootropics tsa morao-rao tse thehiloeng ho racetam. "

Racetam Lelapa la Nootropic- Coluracetam

Coluracetam (BCI-540, kapa MKC-231) ke nootropic e qhibilihang mafura sehlopheng sa metsoako ea racetam. Coluracetam e matla haholo ho feta racetam ea mantlha, Piracetam. Coluracetam e ne e e-na le tokelo ea molao ke Mitsubishi Tanabe Pharma oa Japane ka 2005. Ho e etsa e 'ngoe ea li-nootropics tse ncha ka ho fetisisa tse thehiloeng ho racetam.

Patent ea Coluracetam hamorao e ile ea rekisetsoa BrainCells, Inc. ho San Diego, California. BrainCells ke k'hamphani e nyane ea biopharmaceutical e ikemetseng e ikemetseng ho nts'etsapele metsoako ea kalafo ea khatello e kholo ea khatello ea maikutlo (MDD), khatello ea maikutlo e sa thibeleng kalafo (TRD) le Lefu la Alzheimer.

Coluracetam e ts'oana le sebopeho sa Piracetam. Mme joalo ka li-nootropics tsohle tsa racetam, e na le khubung ea pyrrolidone mokokotlong oa eona. Phuputso ea morao-rao ea bongaka e bontša monyetla oa ho phekola maloetse a tepelletseng maikutlo, le ts'enyo ea methapo ea mahlo le mahlo.

Coluracetam e matla haholo choline e lebisang ho supplement. E matlafatsa phetoho ea "choline" ea boko ba hau ho acetylcholine (ACh) ka ts'ebetso e phahameng ea kamano ea choline (HACU). E leng ho eketsang ho falimeha, ho ela hloko lintlha le mohopolo.

Phuputso e 'ngoe, le boiphihlelo ba motho ka mong li bonts'a Coluracetam e ka ama liamoheli tsa AMPA. Ho e etsa nootropic ea ampakine. E ka hlalosang litlamorao tse ts'oanang le tse khothatsang ntle le litlamorao tsa litlamorao tsa setso. Coluracetam e boetse e bonts'a litšoaneleho tsa khatello ea maikutlo tse thusang ho ntlafatsa maikutlo le ho khutsisa matšoenyeho.

Kamoo Coluracetam e Sebetsang (Mokhoa oa Ts'ebetso)

Joaloka metsoako e mengata ea racetam, coluracetam (CAS:135463-81-9e sebetsa haholoholo ka ho eketsa maemo a "neurotransmitter acetylcholine", e amanang haholo le ho ithuta, ho hopola le ho tseba.

Leha ho le joalo, tsela eo coluracetam e hlophisang maemo a acetylcholine e ikhethile. Ka tloaelo, li-racetam li baka tlhahiso ea acetylcholine ka ho hlasimolla li-receptor tse loketseng, empa coluracetam e etsa joalo ka ho matlafatsa ts'ebeliso e phahameng ea kamano ea choline, kapa HACU. Sistimi ea HACU e khetholla sekhahla seo choline e huloang ka har'a methapo bakeng sa ho fetoha acetylcholine.

Ka ho eketsa sekhahla seo choline e huleloang liseleng tsa methapo ea kutlo, coluracetam e khothalletsang tlhahiso ea acetylcholine mme e baka maemo a boko a neurotransmitter ena ea bohlokoa ho phahama. ho fumaneha ha kapele ha choline bakeng sa ho nkoa.

Hammoho liketso tsena li lebisa maemong a phahameng a acetylcholine, tse amanang le ts'ebeliso e ntlafalitsoeng ea kutloisiso le mohopolo.

Coluracetam

Melemo le Liphello Tsa Coluracetam

❶ Coluracetam e ntlafatsa mohopolo le thuto

Melemo ea Coluracetam e paka ho sebetsa ho tiisa ts'ebetso ea mohopolo le mohopolo ho likhoto le litlamorao tse ts'oanang ho batho. Brain Cells Inc. e entse phuputso e senolang ntlafatso ea kelello likhoto kamora ho amohela AF64A matsatsi a robeli. Nts'etsopele e ile ea tsoela pele ho tšoarella le ho feta kalafo. Lefu la Alzheimer e lebisa maemong a tlase a acetylcholine. Ka ho holisa acetylcholine ho hippocampus, coluracetam e tla eketsa matšoao a lefu la Alzheimer joalo ka mathata a ho ithuta le mohopolo o fosahetseng.

❷ Coluracetam e fokotsa khatello ea maikutlo e hanang kalafo

Phuputsong ea batho ba 101 ba nang le khatello ea maikutlo, ba sa kang ba fihlela kalafo ea sephetho le li-anti-depressing, e bile le phello e ntle ho ntlafatso e bonahalang ea boleng ba bophelo ka makhetlo a 80 mg makhetlo a mararo ka letsatsi. Leha ho le joalo, ena ke eona feela thuto e mabapi le batho. Bokhoni boo e nang le bona ba ho fokotsa bonyollo ba glutamate bo ka ikarabella bakeng sa litlamorao tsa bona tse ntle kalafong ea khatello ea maikutlo.

❸ Coluracetam e fokotsa ho tšoenyeha

Phuputsong ea likhoto, matsatsi a 21 a coluracetam a bonts'a ntlafatso ea 20% matšoenyehong, a neng a phahame ho feta phello ea 12% ea valium ka tekanyetso e le 'ngoe thutong e le' ngoe.

❹ Coluracetam E khothaletsa Neurogeneis

Boithuto bo bong bo re e thusa ka neurogeneis. Mechini ea mantlha ha e so hlake, empa e amana le tsamaiso ea eona bakeng sa libeke tse 'maloa, e eketsang acetylcholine sebakeng sa hippocampus.' 'Litokelo tsa molao li re e khothaletsa kholo ea lisele tsa methapo (neurogenesis). Mochini ha o tsejoe, leha ho le joalo ho nahanoa hore o amana le keketseho ea hippocampal acetylcholine ha coluracetam e tekoa letsatsi le letsatsi libeke tse 'maloa.' '

❺ Coluracetam E thusa ka Schizophrenia

Coluracetam e eketsa tšebetso ea CHAT ka likhoto tse nang le tšenyo ea lisele tsa methapo. Keketseho ena e fana ka maikutlo a hore e ka thusa bakuli ba nang le schizophrenia ka enzyme eona ena. Liphuputso tse ling ka kotloloho ho batho ba nang le schizophrenia lia etsoa.

❻ Coluracetam E ntlafatsa pono

Coluracetam e bonts'itse matla a eona a optic joalo ka ntlafatso ea ho tseba mmala, pono le ho hlaka. Ka ho khetheha, e khothaletsa kholo ea methapo bakeng sa lefu le holofatsang la retina. Liphuputso tse ngata li bua ka pono e ntlafetseng ea 'mala le ho chorisa mahlo, empa ha ho lipatlisiso tsa mahlale tse netefalitseng litlamorao tsena.

Coluracetam e Sebetsa Joang Brain?

Coluracetam e matlafatsa bophelo bo botle ba boko le ho sebetsa ka litsela tse 'maloa. Empa tse peli ka ho khetheha lia hlahella.

Coluracetam e matlafatsa boko ba hau'Ho nka choline ka ho lebisa tlhokomelo le ho sebetsana le ts'ebetso e phahameng ea kamano ea choline (HACU) methapong ea boko.

Acetylcholine (ACh) e entsoe ka choline le acetate. Tsena li tlameha ho fumaneha ho setsi sa methapo ea kutlo ka linako tsohle. E le hore ACh e ka hlophisoa neng kapa neng ha ho hlokahala.

Choline ea mahala e potolohang maling e tšela tšitiso ea mali le bokong. E nkuoa ke li-terminals tsa cholinergic neuron. E kenella methapong ea methapo ea kutlo ke sistimi e phahameng ea kamano ea choline (HACU). Ts'ebetso ea ACh e etsahala kahare ea synaptic. Sebaka se lipakeng tsa methapo ea kutlo ha se ea neuron.

Sisteme ea HACU e its'etleha ka mocheso, matla- le sodium. Sisteme ena ke eona mokhoa o ka sehloohong oo choline e hlokahalang bakeng sa ho kopanya ACh e isoa neuron. Mme ha mohato ona o putlama kapa o sa sebetse ka nepo joalo ka ha o ne o raliloe, o ba le mathata a ho hopola, ho ithuta le moholi oa boko.

Coluracetam e ama ts'ebetso ena mme e e thusa ho sebetsa ka nepo. Ebile, ho bonahala e matlafatsa ts'ebetso ea HACU. Esita le li-neuron tse senyehileng. Keketseho ea acetylcholine ka methapo ea kutlo e thusa ho ntlafatsa mohopolo, matlafatsa temoho hape e fana ka bokhoni bo betere ba ho etsa liqeto.

Coluracetam e boetse e bonahala e ntlafatsa bokhoni ba AMPA. Li-receptor tsa AMPA li angoa ke glutamate. E sebetsang bokong le sistimi e bohareng ea methapo ho ntlafatsa tlhokomeliso le kutloisiso.

Coluracetam e sebetsana le matla a mabeli a AMPA le ntlafatso ea tšebeliso ea choline. Motsoako ona o bonahala o thusa ho ntlafatsa mathata a maikutlo ntle le ho ama maemo a serotonin.

Serotonin Selective Reuptake Inhibitors (SSRIs) ke mokhoa o tloaelehileng oa bongaka oa ho sebetsana le mathata a maikutlo le khatello ea maikutlo. Ba tla le lethathamo la litla-morao tse kotsi. Hape u se ke oa sebeletsa mokuli e mong le e mong ea tepelletseng maikutlo.

Bafuputsi ba tlalehile hore Coluracetam e ne e le molemo ho phekola khatello ea maikutlo le khatello ea maikutlo. Ntle le ho ama maemo a serotonin bokong. Le ntle le litla-morao tse tsamaeang le ho senya serotonin.

Coluracetam

Tšebeliso ea Coluracetam: Tekanyo le Stack Bakeng sa Reference Feela

Coluracetam ke motsoako o sa fumanoeng lijong life kapa life mme 'mele ea rona e ke ke ea o hlahisa. Kahoo, tsela feela ea ho hlahisa melemo ea molek'hule ena ke ka tlatsetso.

Coluracetam hangata e rekisoa ka phofo kapa foromo ea capsule mme e ka nkoa ka molomo. Litekanyetso li ka boela tsa nkoa ka mokhoa o nyane (tlasa leleme) bakeng sa ho kenella ka potlako le ka nepo.

Kaha coluracetam ke moemeli ea matla haholo, ho eletsoa ho qala ka lethal dose e tlase haholo. Haeba o fumana o hloka ho eketsa lethal dose ho utloa melemo, sena se lokela ho etsoa butle butle mme se se ke sa feta 80mg.

Coluracetam ha e na chefo ebile e nkuoa e bolokehile ebile e mamelloa hantle Ho na le litla-morao tse fokolang tse amanang le kompone, joalo ka ho tšoenyeha, ho opeloa ke hlooho, mokhathala le ho nyekeloa ke pelo. Litla-morao tsena ha li fumanehe hangata li etsahala ha feela ho se na letamo le leholo la pele ho choline le ka sebelisoang bakeng sa synthesis ea acetylcholine. Ke ka lebaka lena re khothalletsang ho qala coluracetam ea pele-keketso ka ntlafatso ea boemo ba choline joalo ka citicoline.

Coluracetam e ka sebelisana le lithethefatsi tse ling, haholo-holo tse sebetsanang le mokamo oa NMDA. Sena se kenyelletsa khatello ea khohlela le meriana e thethefatsang kutlo. Lintho tse ling tse sebelisanang le sistimi ea cholinergic, joalo ka meriana ea glaucoma le nicotine, le tsona li ka sebelisana le litlamorao tsa coluracetam. Coluracetam e ka loantša litlamorao tsa lithethefatsi tse khahlanong le cholinergic (joalo ka Benadryl, li-antipsychotic le meriana ea Parkinson).

Joalo ka tlatsetso efe kapa efe, haeba u le meriana kapa u na le maemo a bophelo bo botle, hoa utloahala hore u bue le ngaka ea hau pele u qala. tlatsetsa puso.

※ How To Litsela Well With Lithethefatsi tse ling

Ur Coluracetam ke molek'hule e qhibilihang mafura, ka hona e hantle haholo ho bokelloa ka mafura a phetseng hantle joalo ka coconut kapa oli ea MCT.

Coluracetam le eona e lokela ho bokelloa ka choline supplement joalo ka citicoline. Citicoline e eketsa letamo la choline e fumanehang bakeng sa synthesis. Saka se ka hlahisa litlamorao tse matla ka ho eketsa choline (citicoline) e fumanehang le bokhoni ba ho e kopanya le acetylcholine (coluracetam).

※ Khothaletso e khothalletsoang: 5-80mg ka letsatsi

Re khothaletsa lipakeng tsa 5-80mg ea coluracetam ka letsatsi.

Moeli o kaholimo o bolokehileng oa coluracetam ke 80mg ka letsatsi. Leha ho le joalo, re khothaletsa ho lula le 35mg ka letsatsi kaha litlamorao tsa litekanyetso tse phahameng ha li so hlahlojoe ka botlalo bathong.

Ho nepahetse ho arola litekanyetso tsena hoseng kapa thapama. Mohlala, tekanyetso ea 20mg ea 10mg hoseng le 10mg e ngoe thapama.

Joalokaha ho boletsoe pejana, o lokela ho qala pheletsong e tlase ea tekanyo ea dosing. Ho qala ha lethal dose e tlaase ka ho fetisisa ho tla fokotsa menyetla ea ho ba le litla-morao.

Litla-morao tsa Coluracetam

Coluracetam ha e na chefo. Kahoo e nkuoa e mamelloa hantle ebile e bolokehile. Basebelisi ba bangata ba lekhetlo la pele ba Coluracetam ba tlaleha mokhathala oo hangata e leng litholoana tsa ho qala ka tekanyetso e phahameng haholo.

Hopola, Coluracetam e sebetsa ka ho ntlafatsa tlhahiso ea choline bokong ba hau. Choline ke selelekela sa tlhahiso ea acetylcholine. Haeba choline e sa lekane tsamaisong ea hau, o tla utloa litlamorao.

Litla-morao ha li fumanehe hangata empa li ka kenyelletsa matšoenyeho, mokhathala, hlooho ea hlooho, ho tšoha le ho nyeheloa ke pelo. Hape, litla-morao li atisa ho bakoa ke tekanyo e sa tloaelehang ea nootropic.

Hlooho e bakoang ke ho sebelisa Coluracetam hangata e etsahala ha o lebala ho e kopanya le tlatsetso e ntle ea choline. Hangata ho opeloa ke hlooho ke letšoao la khaello ea choline bokong ba hau.

Kakaretso- Coluracetam

Coluracetam ke e 'ngoe ea litho tse ncha le tse sa tloaelehang tsa sehlopha sa racetam sa nootropics, empa e ratoa haholo ke basebelisi ba bangata.

E eketsa maemo a '' neurotransmitter ea ho ithuta '' acetylcholine, e ka matlafatsang kutloisiso, 'me lithuto tsa liphoofolo li bontša hore e ka koala likhaello tsa mohopolo ntle le litlamorao tse kholo. Le ha ho na le lipatlisiso tsa batho tse seng kae tse ngotsoeng ka coluracetam, lithuto tse teng li bonts'a hore e kanna ea ba kalafo ea bohlokoahali ea khatello ea maikutlo le khatello ea maikutlo.

Basebelisi ba bangata ba e nka e le e ts'episang maikutlo e ts'ehetsang le ho ntlafatsa mohopolo e ba fang mohopolo o motle le ho tsepamisa mohopolo. Ba bang ba re e ba fa se lekanang le "pono ​​ea HD", e etsa hore mebala e khanye, e bapise le ho feta, ebe mabone a khanya haholoanyane.

Coluracetam ke motsoako o matla, kahoo litekanyo tsa litekanyetso li tlaase, 'me ho tsejoa hore li sebetsa ka potlako. E rekisoa e le lijo tlatsetsa naheng ea Amerika mme e ka romelloa ka molao Canada le UK ka chelete e nyane.

Ho ntse ho na le ho hongata ho ka ithutoang ka coluracetam, empa ho bonahala ho bolokehile ho basebelisi ba bangata ha e nkuoa ka boikarabello. Haeba u thahasella ho eketsa ntho e ncha le e fapaneng le ea hau sethala sa nootropic, coluracetam e ka ba e lokelang ho nahanoa.

Coluracetam ha e na lipatlisiso tse ngata, lithuto tse fumanehang li bontša monyetla o moholo oa ts'ebeliso ea eona. Ke e 'ngoe ea li-racetams tse sa tsoa etsahala, tse bapileng le Fasoracetam. Leha ho le joalo, haufinyane tjena, FDA e amohetse mofuta "o ntlafalitsoeng" oa Fasoracetam bakeng sa kalafo ea ADHD.

AASraw ke moetsi ea hloahloa oa Coluracetam (BCI-540, kapa MKC-231) e nang le lab e ikemetseng le fektheri e kholo joalo ka ts'ehetso, tlhahiso eohle e tla etsoa tlasa taolo ea CGMP le sistimi ea taolo ea boleng bo fumanehang. Tsamaiso ea phepelo e tsitsitse, litaelo tse peli tsa thekiso le tse rekisoang li amoheleha.Rea u amohela ho ithuta boitsebiso bo eketsehileng ka AASraw!

O mphihlise Joale

Mongoli oa sengoloa sena:

Ngaka Monique Hong o fumane lengolo UK Imperial College London Faculty of Medicine 

Sengoli sa pampiri sa Scientific Journal:

1.Yukihiko Shirayama
Lefapha la Psychiatry, Sekolo sa Bongaka sa Univesithi ea Chiba, 1-8-1 Inohana, Chiba 260-8677, Japane. 

2.Akinori Akaike
Lefapha la Pharmacology, Sekolo sa Graduate sa Lisaense tsa Meriana, Univesithi ea Kyoto, Kyoto 606-01, Japane

3. Shigeo Murai
Lefapha la Pharmacology. Sekolo sa Bongaka ba Meno. Univesithi ea Bongaka ea Iwate. Morioka. 020, Japane.

4.Tomoko Bessho

Pharmacculicals Laboraiory 1, Yokohama Research Center, Mitsubishi Chemical Corporation, Yokohama 227, JAPAN.

5.Ken Takashina

Pharmaceutical Lab. Ke, Mitsubishi Chemical Co., Yokohama 227, Japan

6.Uemura Kazumasa

Lefapha la Boraro la Meriana ea ka hare, 65 Tsuruma-cho, Showa-ku, Nagoya 466-8550, Japane

Ha ho ka tsela leha e le efe ngaka/saense ena e buellang kapa ho buella ho rekoa, thekiso, kapa tšebeliso ea sehlahisoa sena ka lebaka lefe kapa lefe. Aasraw ha e na kamano kapa kamano, ho boleloa kapa ho seng joalo, le ngaka ena. Sepheo sa ho qotsa ngaka ena ke ho ananela, ho ananela le ho babatsa lipatlisiso tse felletseng le mosebetsi oa nts'etsopele o entsoeng ke bo-ramahlale ba sebetsanang le ntho ena.

References

[1] Shirayama Y, Yamamoto A, Nishimura T, Katayama S, Kawahara R (September 2007). "Ho pepeseha ka morao ho MKC-231 ho hanyetsana le bofokoli ba boitšoaro bo bakoang ke phencyclidine le ho fokotsa li-neuron tsa septal cholinergic ho likhoto". Neuropsychopharmacology ea Europe. 17 (9): 616–26.

[2] BrainCells Inc. E Tsebahatsa Liphetho ho Tsoa ho Exploratory Phase 2a Teko ea BCI-540 E bolokiloe ka La 21 Pulungoana 2011, ho Wayback Machine.

[3] Uemura K, Yoshioka S, Ueda M, Tamaya N, Iguchi A, Hotta N.” Liphello tsa methapo ea kutlo e bohareng-mediated hyperglycemic ea NIK-247, cholinesterase inhibitor, le MKC-231, choline uptake enhancer, ho likhoto. ”.Jpn J Pharmacol. 1999 Jan;79(1):113-5. doi: 10.1254/jjp.79.113.PMID: 10082325.

[4] Takashina K., Bessho T., Mori R., Eguchi J., Saito K. "MKC-231, a choline uptake enhancer: (2) Phello ea ho kopanya le ho lokolloa ha acetylcholine ho likhoto tse phekoloang ke AF64A." Journal of Neural Transmission (Vienna). 2008 Jul;115(7):1027-35.

[5] Akaike A, Maeda T, Kaneko S, Tamura Y. "Phello ea ts'ireletso ea MKC-231, buka ea "high affinity choline uptake enhancer", ho glutamate cytotoxicity ho li-neuron tsa cortical ".Jpn J Pharmacol. 1998 Feb;76(2):219-22. doi: 10.1254/jjp.76.219.PMID: 9541286.

[6] Lin M, Hu G, Wang Z, Yu B, Tan W. "Ts'ebetso ea High-Affinity Choline Transporter 1 ka Spinal Cord e Fokotsa Hyperalgesia e Bakiloeng ke Khatello" .Dig Dis Sci. 2023 Jun;68(6):2414-2426. doi: 10.1007/s10620-022-07765-5. Epub 2023 Feb 18. PMID: 36808325.

[7] Malykh, AG, & Sadaie, MR (2010). Lithethefatsi tse Tšoanang le Piracetam le Piracetam. Lithethefatsi, 70 (3), 287-312.

[8] Morris BJ, Cochran SM, Pratt JAPCP: ho tloha pharmacology ho ea ho mohlala oa schizophreniaCurr Opin Pharmacol.(2005 Feb).

[9] Yamamura HI, Snyder SHHigh affinity transport of choline into synaptosomes of rat brainJ Neurochem.(1973 Dec).

[10] Brauser D. "Lik'hemik'hale Tse Kholisang Neurogenesis li Bontša Tšepiso ea Phekolo ea ho Tepella Maikutlo a Maholo" Medscape Medical News September 21, 2009.

[11] Murai S., Saito H., Abe E., Masuda Y., Odashima J., Itoh T. "MKC-231, choline uptake enhancer, e ntlafatsa bofokoli ba mohopolo o sebetsang le ho fokotseha ha hippocampal acetylcholine e bakoang ke ethylcholine aziridinium ion ho litoeba." Journal of Neural Transmission General Karolo. 1994;98(1):1-13.

[12] Slotkin TA, Seidler FJ, Crain BJ, Bell JM, Bissette G, Nemeroff CBLiphetoho tsa taolo tšebetsong ea presynaptic cholinergic e hlahlobiloeng ka thepa e potlakileng ea autopsy ho tsoa ho bakuli ba nang le lefu la Alzheimer: litlamorao tsa etiology le kalafoProc Natl Acad Sci US A.(1990 Apr).

[13] Akaike A., Maeda T., Kaneko S., Tamura Y. "Ts'ireletso ea MKC-231, buka e ncha e amanang le choline e matlafatsang, ho glutamate cytotoxicity ho li-neuron tsa cortical." Journal ea Japane ea Pharmacology. 1998 Feb;76(2):219-22

[14] Rylett RJ, Ball MJ, Colhoun EHEvidence bakeng sa lipalangoang tse phahameng tsa choline ka li-synaptosomes tse lokiselitsoeng ho tloha hippocampus le neocortex ea bakuli ba nang le lefu la AlzheimerBrain Res.(1983 Dec 19).

[15] Fisher A, Mantione CR, Abraham DJ, Hanin ILong-term central cholinergic hypofunction induced ho litoeba ke ethylcholine aziridinium ion (AF64A) in vivoJ Pharmacol Exp Ther.(1982 Jul).

[16] Bessho T., Takashina K., Eguchi J., Komatsu T., Saito K. "MKC-231, e matlafatsang choline-uptake: (1) ntlafatso ea nako e telele ea kelello ka mor'a tsamaiso e pheta-phetoang ho likhoto tse phekoloang ke AF64A." Journal of Neural Transmission (Vienna). 2008 Jul;115(7):1019-25.

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