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Sanduuqa IDRA-21 (22503-72-6) fiidiyow
Macluumaadka Saldhigga budada ee IDRA-21
magaca | Sanduuqa IDRA-21 |
CAS | 22503-72-6 |
xagiisayna | 98% |
Magaca kiimikada | 7-Chloro-3-methyl-3,4-dihydro-2H-1,2,4-benzothiadiazine S,S-dioxide |
Isku mid ahaanshaha | IDRA-21; IDRA 21; IDRA21. |
Formula kelli | C8H9ClN2O2S |
Miisaanka kelli | 232.682 |
Dhibicda Biyaha | Lama yaqaan |
Muhiimadda InChI | VZRNTCHTJRLTMU-UHFFFAOYSA-N |
Form | adag |
Imaanshaha | Caddaan cad-cad oo budada ah |
Nolosha badh | 24/36 saacadood |
milmi | ku milma DMSO (100mM) |
kaydinta Xaaladda | Dukaanka RT |
Codsiga | Isweydaarsiga loo yaqaan 'cyclothiazide' ee xannibaysa quwad ka-hortagga AMPA receptor |
Dukumentiga Tijaabinta | Available |
Budada IDRA-21 Sharraxaadda Guud
Budada IDRA-21 waxaa loo kala saaraa "ampakine". Waxay awood u leedahay inay hagaajiso diiradda iyo feejignaanta sidoo kale kor u qaadista barashada iyo xusuusta. Ampakines waxay ku soo badanayaan caanka ah sababta oo ah waxay bixiyaan faa'iidooyinka garashada ee kicinta iyada oo aaney jirin waxyeelada aan loo baahnayn.
Daraasad 1995 lagu sameeyay jiirka, IDRA-21 ayaa hoos u dhigtay garashada garashada ee ay keento alprazolam (Xanax). Isla sannadkaas, daraasad kale ayaa muujisay cillad garasho oo ay sababtay scopolamine waxaa rogay daanyeero by IDRA-21. Daraasad aadane lama samayn.
Budada IDRA-21 (22503-72-6) Taariikh
Budada IDRA-21 waa qalab koronto oo toosan oo ah aaladda soo dhaweynta AMPA iyo soo saarista benzothiadiazine. Waa unug molaaydh ah, oo leh (+) - IDRA-21 oo ah qaabka firfircoon.
IDRA-21 wuxuu ahaa mid firfircoon xagga cilmiga xoolaha, si weynna u wanaajiyey barashada iyo xusuusta. Waxay ku dhawaad 10-30 jeer ka awood badan tahay aniracetam xagga dib-ula-noqoshada cilladaha garashada ee ay kiciso Albazalam ama Scopolamine, waxayna soo saartaa saameyn joogto ah ilaa 48 saacadood kadib hal cabir. Awoodda mudada-dheer ee udhaxeysa maskaxda maskaxda.
IDRA-21 ma soo saarto neurotoxicity xaaladdo caadi ah, in kasta oo ay uga sii dari karto dhaawaca neuronal ee soo raaca ischemia adduunka ka dib faaligga ama suuxdinta.
Marka la barbar dhigo ampakines ama benzoylpiperidine-ka soo saarta AMPA receptor potentiators, IDRA-21 waxay ka awood badnayd CX-516, laakiin waxay ka awood yar tahay CX-546. Soosaarayaasha cusub ee benzothiadiazide oo leh awood aad u kordhay marka la barbar dhigo IDRA-21 ayaa la sameeyay, laakiin kuwan looma sameynin cilmi baaris ilaa heer ah, iyadoo maadooyinka benzoylpiperidine iyo benzoylpyrrolidine ee loo yaqaan 'CX-taxane' ay ka kooban yihiin unugyada loo doorbiday hormarinta kiliinikada, oo ay u badan tahay inay ugu wacan tahay sumcad wanaagsan astaamaha qiyaasta sare.
IDRA-21 (22503-72-6) Farsamooyinka Ficil
IDRA-21 oo ah daroogada kicisa ampakine, kiciyayaashu waa kuwa wax ka beddelaya allosteric AMP qaboojiyeyaasha maskaxda. Kuwani soo-dhoweeyeyaasha AMPA waxay mas'uul ka yihiin gudbinta dhaqsaha badan ee 'synaptik' waxayna ku lug leeyihiin baaxadda synaptic iyo xoog-saaridda muddada-dheer. Ahaanshaha 'ampakine' IDRA-21 wuxuu ku shaqeeyaa iyada oo loo marayo wax ka beddelka soo dhaweynta AMPA ee maskaxda. Waxay mas'uul ka tahay xiritaanka goobta allosteric iyo ka dib oo lagu qasbo isbeddel wanaagsan. Qaarkood waxay tixraacayaan nidaamkan sida firfircoonaanta allosteric.
IDRA-21 waa aasaaska benzothiadiazine oo leh astaamo nootropic ah. Waxay u egtahay "IDRA 21 inay faa iidooyinkeeda dabeecad xumo ka muujiso diidmada AMPA receptor desensitization." Ampakines waxay kicisaa dadka qaata dawada glutamatergic AMPA. Tani waxay kor u qaadeysaa feejignaanta iyo feejignaanta, taas oo ka dhigeysa fasalkan dawooyinka murashaxiinta xiisaha leh ee daaweynta daaweynta naafada iyo sidoo kale xoojinta guud. Sumowga xad-dhaafka ahi waxay ku dambayn kartaa walaac ama cabsi, xanaaq badan iyo naxariis la’aan.
IDRA-21 (22503-72-6) Codsi
IDRA-21 waa astaamo benzothiadiazine ah iyo qaab-dhismeedka wanaagsan ee allosteric ofglutamate AMPA reseptors (1,2,3,4). Waxay awood u leedahay inay kordhiso awoodda firfircoonida 'synaptic' iyadoo la joojinayo miyir beelka AMPA. IDRA 21 waxay soo bandhigi kartaa saameyn daaweyn si loo hagaajiyo maqnaanshaha xusuusta bukaanka qaba cillad xagga garashada sida cudurka Alzheimers.
IDRA-21 ayaa sidoo kale loo malaynayaa inay kiciso awood-dheer (LTP). LTP waa horumar waara oo ku saabsan sida neerfayaasha ula xiriiraan maskaxda. Waxay muhiim u tahay hagaajinta baaxadda synaptic, oo xoojisa sharoobooyinka maskaxda gudaheeda. Maadaama sifeynta ay inta badan mas'uul ka yihiin xusuusto, kor u qaadidda xooggooda iyo shaqadooda ayaa muhiim u ah hagaajinta garashada guud.
IDRA-21 (22503-72-6) Cilmi Baaris Dheeraad ah
Marka la barbar dhigo ampakines ama benzoylpiperidine-ka soo saarta AMPA receptor potentiators, IDRA-21 waxay ka awood badnayd CX-516, laakiin waxay ka awood yar tahay CX-546. Soosaarayaasha cusub ee benzothiadiazide oo leh awood aad u kordhay marka loo barbar dhigo IDRA-21 ayaa la sameeyay, laakiin kuwan looma sameynin daraasad isku mid ah, iyadoo taxanaha benzoylpiperidine iyo benzoylpyrrolidine CX-da ee dawooyinka loo doorbiday horumarinta kiliinikada, oo ay u badan tahay inay sabab u tahay sumcad wanaagsan astaamaha qiyaasta sare.
IDRA-21 waa kiimikal cilmi-baaris oo loo istcimaalo cilmi-baarista ay ansaxiyaan hay'adaha sharci dejinta ee gobolkaaga.
IDRA-21 (22503-72-6) Tixraac
- Malkova L, Kozikowski AP, Gale K. Saamaynta huperzine A iyo IDRA 21 ee xusuusta aqoonsiga muuqaalka ee makarayaasha dhalinyarada ah. Neuropharmacology. 2011 Jun; 60 (7-8): 1262-8. doi: 10.1016 / j.neuropharm.2010.12.018. Epub 2010 Dec 23. Waxaa la daabacay PMID: 21185313; PubMed Central PMCID: PMC3073152.
- Buccafusco JJ, Weiser T, Jiilaalka K, Klinder K, Terry AV. Saamaynta IDRA 21, oo ah hagaha toosan ee qaataha AMPA, ee dib u dhaca ku yimid waxqabadka barbaro da 'yarta iyo da' weyn. Neuropharmacology. 2004 Jan; 46 (1): 10-22. PubMed PMID: 14654093.
- Losi G, Puia G, Braghiroli D, Baraldi M. IDRA-21, modulator wanaagsan oo ah AMPA, wuxuu xanibay synaptik iyo extrasynaptic NMDA receptor dhexdhexaadinta munaasabadaha unugyada abaabulan ee unugyada caloosha ee abaabulan. Neuropharmacology. 2004 Jun; 46 (8): 1105-13. PubMed PMID: 15111017.
- IDRA-21 Qaddarka budada, nolosha badh, Faa'iidooyinka, waxyeelooyinka, iyo dib u eegista.
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