IDRA-21 phofo (22503-72-6)

IDRA-21 phofo (22503-72-6) video

 

Tlhahisoleseling ea Base ea IDRA-21 ea phofo

lebitso	IDRA-21 phofo
CAS	22503-72-6
Ho hloeka	98%
Lebitso la k'hemik'hale	7-Chloro-3-methyl-3,4-dihydro-2H-1,2,4-benzothiadiazine S,S-dioxide
Li-synonyms	IDRA-21; IDRA 21; IDRA21.
Molecular Formula	C8H9ClN2O2S
Boima ba 'mele	232.682
Melting Point	Ha re tsebe
InChI Key	VZRNTCHTJRLTMU-UHFFFAOYSA-N
foromo	E tiile
Ponahalo	Ho soeufala ho ea ho phofshoana e tšoeu ea phofo
Halofo ea bophelo	Lihora tse 24/36
Solubility	qhibilihang ka DMSO (100mM)
Boemo Storage	Boloka ho RT
kopo	Analog ea cyclothiazide e Inhibits AMPA receptor desensitization
Tokomane ea Teko	fumaneha

 

Tlhaloso e akaretsang ea IDRA-21 phofo

IDRA-21 phofo e thathamisitsoe e le ampakine. E khona ho ntlafatsa mohopolo le tlhokomelo le ho khothaletsa ho ithuta le ho hopola. Ampakines e ntse e eketseha haholo hobane e fana ka melemo ea kelello ea li-stimulants ntle le litlamorao tse sa rateheng.

Phuputsong ea 1995 e entsoeng ka likhoto, IDRA-21 e fokolitse likhaello tsa kutloisiso tse bakoang ke alprazolam (Xanax). Selemong sona seo, phuputso e 'ngoe e bonts'itse ho holofala ha kelello ho bakoang ke scopolamine ho ile ha fetoloa litšoene ke IDRA-21. Ha ho lithuto tsa batho tse entsoeng.

 

Nalane ea IDRA-21 (22503-72-6) Nalane

IDRA-21 phofo ke sethala se matla sa allitoric of receptor ea AMPA le benzothiadiazine. Ke molek'hule ea chiral, eo (+) - IDRA-21 e leng sebopeho se sebetsang.

IDRA-21 e ne e le mafolofolo lithutong tsa liphoofolo, e ntlafatsa haholo ho ithuta le ho hopola. E potoloha ka makhetlo a 10-30 e le matla ho feta aniracetam ho khutliseng liphoso tsa kelello tse hlahisitsoeng ke alprazolam kapa scopolamine, mme e hlahisa litlamorao tse tsitsitseng tse ka fihlang ho lihora tse 48 kamora hore e be e le 'ngoe mokhoa. tšebeliso ea nako e telele lipakeng tsa li-synapses bokong.

IDRA-21 ha e hlahise neurotoxicity tlasa maemo a tloaelehileng, leha e ka mpefatsa ts'enyo ea neuronal ka mor'a ischemia ea lefats'e ka mor'a ho otloa kapa ho tsukutloa.

Ha ho bapisoa le li-ampakine kapa benzoylpiperidine tse hlahisitsoeng ke AMPA receptor potentiators, IDRA-21 e ne e le matla ho feta CX-516, empa e le matla ho feta CX-546. Mefuta e mecha ea benzothiadiazide e nang le potency e ngata haholo ha e bapisoa le IDRA-21 e se e ntlafalitsoe, empa tsena ha li sa etsoa lipatlisiso ho isa tekanyong e tšoanang, ka li-complex tsa benzoylpiperidine le benzoylpyrrolidine CX tse fumanehang bakeng sa nts'etsopele ea tleliniki, haholo holo ka lebaka la chefo e ntle haholoanyane. profiles tse phahameng tekanyetso.

 

IDRA-21 (22503-72-6) Mechanism Of Ts'ebetso

IDRA-21 joalo ka sethethefatsi se matlafatsang sa ampakine, li-stimulant ke li-modulator tsa allosteric tsa li-receptor tsa AMPA bokong. Li-receptor tsena tsa AMPA li ikarabella bakeng sa phetisetso e potlakileng ea "synaptic" mme li kentse letsoho ho polasetiki ea synaptic le ho ba le monyetla oa nako e telele. Ho ba ampakine IDRA-21 e sebetsa ka ho feto-fetoha ha li-receptor tsa AMPA bokong. E na le boikarabello ba ho tlama sebaka sa allosteric le ho qobella ho feto-fetoha ha maemo ho nepahetseng. Ba bang ba bua ka ts'ebetso ena e le ts'ebetso ea allosteric.

IDRA-21 ke benzothiadiazine e nkiloeng ka thepa ea nootropic. Mohlomong "IDRA 21 e fana ka litlamorao tsa eona tsa boitsoaro ka ho susumetsa takatso ea AMPA receptor." Ampakines e hlohlelletsa li-receptor tsa glutamatergic AMPA. Sena se ntlafatsa nako ea ho tsepamisa mohopolo le ho tsepamisa mohopolo, se etsa hore sehlopha sena sa lithethefatsi se khahlise bakeng sa kalafo ea mathata a ho ithuta le ntlafatso e akaretsang. Ho ja haholo ho ka fella ka ho tšoenyeha kapa ho tšoha, hanyane feela ka lebaka la ho hloka moea le ho hloka thahasello.

 

Kopo ea IDRA-21 (22503-72-6) Kopo

IDRA-21 ke sehlahisoa sa benzothiadiazine le e ntle ea allosteric modulator eaglutamate AMPA receptors (1,2,3,4). E khona ho eketsa matla a nyarosang a synaptic ka ho thibela AMPA receptor desensitization. IDRA 21 e ka hlahisa litlamorao tsa kalafo ho ntlafatsa bofokoli ba memori ho bakuli ba nang le mathata a kelello a kang lefu la Alzheimer's.

IDRA-21 e boetse e nahanoa hore e susumetsa tšebeliso ea nako e telele (LTP). LTP ke keketseho ea nako e telele ea kamoo li-neurons li buisanang le bokong. Ho bohlokoa ho ntlafatsa polasetiki ea synaptic, e matlafatsang li-synapsic kahare ho bokong. Joalo ka ha li-synapses li ikarabella haholo bakeng sa mehopolo, ho matlafatsa matla le ts'ebetso ea bona ho bohlokoa ho ntlafatsa kutlwisiso e akaretsang.

 

IDRA-21 (22503-72-6) Patlisiso e Eketsehileng

Ha ho bapisoa le li-ampakine kapa benzoylpiperidine tse hlahisitsoeng ke AMPA receptor potentiators, IDRA-21 e ne e le matla ho feta CX-516, empa e le matla ho feta CX-546. Mefuta e mecha ea benzothiadiazide e nang le potency e ngata haholo ha e bapisoa le IDRA-21 e se e ntlafalitsoe, empa tsena ha li sa etsoa lipatlisiso ho isa tekong e tšoanang, ka benzoylpiperidine le benzoylpyrrolidine CX-letoto la lithethefatsi li ratoa bakeng sa nts'etsopele ea bongaka, haholoholo ka lebaka la chefo e ntle haholoanyane. profiles tse phahameng tekanyetso.

IDRA-21 ke k'hemik'hale ea lipatlisiso e tla sebelisoa ho etsa lipatlisiso tse amohetsoeng ke li-agency tsa taolo sebakeng sa heno.

 

Tšupiso ea IDRA-21 (22503-72-6)

• Malkova L, Kozikowski AP, Gale K. Litlamorao tsa huperzine A le IDRA 21 molemong oa memori e lemohuoang ka li-macaque tse nyane. Neuropharmacology. 2011 Jun; 60 (7-8): 1262-8. Doi: 10.1016 / j.neuropharm.2010.12.018. Epub 2010 Dec 23. PubMed PMID: 21185313; PubMed Central PMCID: PMC3073152.
• Buccafusco JJ, Weiser T, Mariha K, Klinder K, Terry AV. Litlamorao tsa IDRA 21, modulasetulo ea nepahetseng oa AMPA receptor, mabapi le ts'ebetso e ts'oanang ea ts'ebeliso ea litšoene tse nyane le tse holileng tsa rhesus. Neuropharmacology. 2004 Jan; 46 (1): 10-22. PubMed PMID: 14654093.
• Losi G, Puia G, Braghiroli D, Baraldi M. IDRA-21, modulelli ea sebetsang hantle oa AMPA receptor, o thibela liketsahalo tsa synaptic le extrasynaptic NMDA receptor tse kenelletseng liseleng tse cultured tsa granule. Neuropharmacology. 2004 Jun; 46 (8): 1105-13. PubMed PMID: 15111017.
• Tekanyo ea phofo ea IDRA-21, Half-life, Melemo, litla-morao, le Tlhahlobo.