PE22–28 ye mun ye?

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Fɛn minnu bɛ di nin siti in kan, olu dabɔra ɲininiw dɔrɔn kama in vitro. Sɛgɛsɛgɛli in vitro (latinkan na: *in glass*, o kɔrɔ ye gilasi minɛnw na) bɛ kɛ hadamaden farikolo kɔkan. Nin fura ninnu tɛ furaw ye, Ameriki dumuniko ni furako ɲɛmɔgɔso (FDA) ma sɔn u ma, wa u man kan ka kɛ ka furakɛli bana, bana walima bana si bali, k’a furakɛ, walima k’a furakɛ. A dagalen don kosɛbɛ sariya fɛ ka nin fɛn ninnu don hadamaden walima bagan farikolo la cogo o cogo.

PE22–28 ka ɲɛfɔli kunbaba

PE22–28 ye asidi aminiki 7 pepitiri ye min dilannen don ka da ɲininiw kan minnu kɛra Spadin kan (PE 12–28). Hakiliɲagami, hakilibana min bɛ diɲɛ jamanaden 20% ɲɔgɔn minɛ, o bɛ furakɛ sisan ni degun furaw ye minnu bɛ tɔɔrɔ ni ko dɔw ye i n’a fɔ wale daminɛni kɔfɛ ani kɔlɔlɔ jugumanw. Spadin ɲɛfɔlen don i n’a fɔ pepitiri kɔnɔna na, degun fura bɛ min na, o bɛ TREK-1 sira datugu kɛrɛnkɛrɛnnenya la, nka a baara bɛ tunun lɛri 7 kɔnɔ a tali kɔfɛ. Walasa ka Spadin sabatili n’a ka ɲɛnamaya kɛcogo ɲɛ in vivo, ɲininikɛlaw ye a ɲɔgɔnnaw ni a bɔlenw sɛgɛsɛgɛ, ka Spadin ka joli tiɲɛnifɛnw sɛgɛsɛgɛ, ka laban ka PE22-28 dilan.

Jaa 1 Spadin-analog kɛrɛnkɛrɛnnenya la. (A–D) PE 22-28 kɛra pepitiri ciden ye walasa ka spadin-analogw kɛrɛnkɛrɛnnenya sɛgɛsɛgɛ ni K2P sira tɔw ye, TREK-2 (A), TRAAK (B), TRESK (C), ani TASK-1 (D).

PE22-28 ka wale

A nɔ bɛ TREK-1 kanalw kan

In vitro kalan minnu kɛra ni patch-clamp fɛɛrɛ ye hTREK-1/HEK selilɛriw kan, olu y’a jira ko PE22-28 bɛ kɛrɛnkɛrɛnnenya ni ɲɔgɔndɛmɛ ɲuman jira TREK-1 siraw la ni i y’a suma ni Spadin ye. Kunnafoni kɛrɛnkɛrɛnnenw b’a jira ko PE22-28 ka IC5 ye 0,12 nM ye, ka sɔrɔ Spadin ta ye 40–60 nM ye. O kɔrɔ ye ko o cogo kelenw na, PE22-28 bɛ se ka baara kɛ TREK-1 sira kan ka ɲɛ ni a hakɛ dɔgɔyara, o la, a bɛ a ka ɲɛnamaya kɛcogo jira ka ɲɛ. Nin ɲinini in y’a jira fana ko o cogoya kelenw na, fɛn caman b’a la ka fɛn caman sɛmɛntiya PE22-28 N- walima C-terminus la, olu bɛ se ka TREK-1 kanal baara sabati walima k’a ban k’a sɔrɔ u ma nɔ bila a ni TREK-1 kanal ka jɛɲɔgɔnya la. Nin sariyasun kɛrɛnkɛrɛnnen in min bɛ kanali baara ni a ni ɲɔgɔn cɛ, o bɛ taamasiyɛn nafamaw di walasa ka ɲinini wɛrɛw kɛ a ka baarakɛcogo n’a furakɛlicogo kan.

Degun furaw nɔ minnu bɛ sɔrɔ in vivo

Taamacogo misali tiɲɛni : Degun kɛcogo misaliw la i n’a fɔ nakɔko sɛgɛsɛgɛli fanga la, PE22-28 n’a bɔlenw ka degun furaw dafara. Sogo minnu furakɛra ni Spadin analoziw ye (PE22-28 fana sen bɛ o la) ye dɔ bɔ kosɛbɛ lamagabaliya waati la. Lamaga-lamagali waati ye degun-ko ɲɔgɔnna kɛcogo jiralan nafama ye sosow la, waajibiya-sɛgɛsɛgɛli waati la, wa ni jiginni waati dɔgɔyara, o b’a jira ko degun-ko-taamacogo dɔgɔyara, o b’a jira ko PE22-28 bɛ ni degun fura ye. Balocogo sɛgɛsɛgɛli min kɛra ni fɛn kuraw bali ye, furakɛli kuntaalajan tile 4 kɔfɛ, PE22-28 ye dɔ bɔ kosɛbɛ sosow ka dumunikɛminɛnw dun waati la. Dumuni sɛgɛsɛgɛli min bɛ kɛ ni fɛn kura ye, o ye fɛɛrɛ ye min bɛ kɛ ka sosow ka dumuni nege jateminɛ sigida kura kɔnɔ. Ni latɛmɛ waati surunyara, o b’a jira ko jɔrɔnanko ni degun bɛ tali kɛ ɲɔgɔn na, o bɛ dɔgɔya sosow la, o bɛ PE22-28 ka degun furaw nɔw sinsin ka taa a fɛ.

A nɔ minnu bɛ sɔrɔ farikolojidɛsɛ ni sinankunya la : Furakɛli tile 4 dɔrɔn kɔfɛ, PE22-28 n’a ɲɔgɔnnaw ye farikolojidɛsɛ bila mɔgɔ la, ni G/A-PE22-28 ye nɔba jira kɛrɛnkɛrɛnnenya la. Senfagabana jɔyɔrɔ ka bon degun ni furakɛli jaabi banakisɛ sɔrɔli la, wa senfagabana kura bɔli bɛ dɛmɛ ka senfagabana baara ni dusukunnataw cogoya ɲɛ. Sogow ka kɔkolo senkɔniw na, PE22-28 n’a bɔlenw fana ye sinankunya fanga bonya, i n’a fɔ a bɛ suman cogo min na ni PSD-95 jiracogo hakɛ caya ye. PSD-95 ye farikolojɔlifɛn ye min bɛ tali kɛ sinankunya kɔfɛ yɔrɔ dense la, wa a jiracogo hakɛ cayalenba b’a jira ko sinankunya jɔli ni a baara bɛ bonya, o bɛ kunnafonidi nɔgɔya senfagabana ni senfagabana sɛrɛkiliw cɛ, o min nafa ka bon kosɛbɛ degun taamasiɲɛw ɲɛnabɔli la.

Nafa minnu bɛ sɔrɔ a kɛcogo kuntaala la : Ni i ye a suma ni Spadin ye, PE22-28 ni a ɲɔgɔnnaw ka baara kuntaala bɛ ɲɛ kosɛbɛ. Spadin bɛ bɔnɛ a ka baara la lɛri 7 a tali kɔfɛ, ka sɔrɔ PE22-28 ka baara kuntaala bɛ se ka se lɛri 23 ma. Ni a kɛcogo ka jan, o kɔrɔ ye ko a nɔfɛkow bɛ se ka mɛn farikolo la, o bɛ dɔ bɔ a tali caya la ani ka banabagatɔw ka sariya labatoli ɲɛ, o min bɛ na ni nafa nafamaw ye kɛnɛyaso furakɛli la.

PE22-28 ka baarakɛcogo

Baarakɛcogo minnu bɛ se ka kɛ degun furakɛli la : Ni an y’a jateminɛ ko PE22-28 ka baara kɛcogo ka ɲi degun furaw kɛcogo misaliw la, a ka baara kɛcogo kɛrɛnkɛrɛnnen TREK-1 sira kan, ani a nɔ ɲumanw bɛ se ka kɛ farikolojidɛsɛ furakɛli la, a bɛ kɛ fɛnɲɛnamafagalan ye min bɛ layidu ta, min bɛ se ka Spadin bila a nɔ na degun furakɛli la. PE22-28 bɔli bɛ furakɛli suguya kura di degun ma. A kɛra sira nafama ye degun furaw bɔnsɔn nataw labɛnni na. Sɛgɛsɛgɛli ni yiriwali wɛrɛw sababu fɛ, k’a fura dilanni n’a tali kɛcogo ɲumanw kɛ, a jirala ko a bɛna furakɛli suguya ɲumanw di degunbagatɔw ma.

Bununda

[1] Djillani A, Pietri M, Moreno S, ani a ɲɔgɔnnaw. Spadin Analogs surunw bɛ TREK-1 balili ɲuman jira, In Vivo sabatili ani degun furaw baara[J]. Dancɛw furakɛli la, 2017,8:643.DOI:10.3389/fphar.2017.00643.

Fɛn min bɛ sɔrɔ ɲininiw dɔrɔn kama:

PE-22-28-10mg

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