Pregabalin

Tlhaloso e Khutšoanyane:

Lebitso la API Sesupo Ga tlhaloso US DMF  EU DMF  CEP
Pregabalin Sethoathoa / Neuralgia Ka Ntlong / EP 22223 CEP2016-141

Product Qaqileng

Lihlahisoa tsa Product

TLHOKOMELISO PRODUCT

Pregabalin ha se GABAA kapa GABAB receptor agonist.
Pregabalin ke gabapentinoid mme e sebetsa ka ho thibela liteishene tse ling tsa calcium. Haholo-holo ke mokokotlo oa sebaka sa thusang sa α2δ sa subunit sa li-chaline tse itseng tse itšetlehileng ka voltage (VDCCs), ka hona e sebetsa e le sesithibi sa li-VDCC tse nang le α2α. Ho na le li-subunits tse peli tse tlamang lithethefatsi α2δ, α2δ-1 le α2δ-2, 'me pregabalin e bonts'a kamano e ts'oanang (mme ka hona ho hloka khethollo lipakeng tsa) libaka tsena tse peli. Pregabalin e ea ikamahanya le α2δ VDCC subunit. Leha e le hore pregabalin ke analogue ea GABA, ha e itlamme ho li-receptor tsa GABA, ha e fetohe GABA kapa e 'ngoe ea GABA receptor agonist in vivo, ebile ha e fetole ka kotloloho lipalami tsa GABA kapa metabolism. Leha ho le joalo, pregabalin e fumanoe e hlahisa keketseho e itšetlehileng ka lethal dose ea boko ba L-glutamic acid decarboxylase (GAD), enzyme e ikarabellang bakeng sa ho hlophisa GABA, ka hona e ka ba le litlamorao tse sa tobang tsa GABAergic ka ho eketsa maemo a GABA bokong. Hajoale ha ho na bopaki ba hore litlamorao tsa pregabalin li buelloa ke mochini ofe kapa ofe ntle le ho thibela li-VDCC tse nang le α2α. Ho latela, thibelo ea li-VDCC tse nang le α2δ-1 tse nang le pregabalin e bonahala e ikarabella bakeng sa litlamorao tsa eona tsa anticonvulsant, analgesic le anxiolytic.
Li-ome-amino acid tsa L-leucine le L-isoleucine, tse ts'oanang hantle le pregabalin le tse ling tsa gabapentinoids tse sebopeho sa lik'hemik'hale, ke li-ligand tsa α2δ VDCC subunit e nang le kamano e tšoanang le ea gabapentinoids (mohlala, IC50 = 71 nM ea L- isoleucine), 'me li teng mokelikeli oa motho oa cerebrospinal maemong a micromolar (mohlala, 12.9 μM bakeng sa L-leucine, 4.8 μM bakeng sa L-isoleucine). Ho 'nile ha boleloa hore e kanna ea ba li-ligand tsa semmuso tsa subunit le hore ba ka qothisana lehlokoa le litlamorao tsa gabapentinoids. Ho latela, le ha gabapentinoids joalo ka pregabalin le gabapentin li na le linomine tsa nanomolar bakeng sa α2δ subunit, matla a tsona a vivo a maemong a tlase a micromolar, mme tlholisano ea ho tlama ke li-amino acid tse sa feleng ho thoe e kanna ea ikarabella bakeng sa ho se tšoane hona.

Pregabalin e fumanoe e na le kamano e phahameng makhetlo a 6 ho feta gabapentin bakeng sa li-VDCC tse nang le li-subunit tse nang le li-subcitit thutong e le 'ngoe. Leha ho le joalo, phuputso e 'ngoe e fumane hore pregabalin le gabapentin li na le liemahale tse tšoanang bakeng sa subunit ea motho e boetse e na le α2δ-1 (Ki = 32 nM le 40 nM, ka ho latellana). Boemong bofe kapa bofe, pregabalin e matla ho feta makhetlo a 2 ho isa ho a mane ho feta gabapentin joalo ka analgesic mme, liphoofolong, e bonahala e le matla ho feta makhetlo a 3 ho isa ho a 10 ho feta gabapentin joalo ka anticonvulsant.

NTHATISI

2018 GMP-2
原料药GMP证书201811(captopril ,thalidomide etc)
GMP-of-PMDA-in-Chanyoo-平成28年08月03日 Nantong-Chanyoo-Pharmatech-Co
FDA-EIR-Letter-201901

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