Pregabalin ma aha GABAA ama GABAB agonist.
Pregabalin waa gabapentinoid wuxuuna u dhaqmaa isagoo joojinaya kanaalada calcium qaarkood.Gaar ahaan waa isku xidhka kaaliyaha α2δ qayb hoosaadka ee kanaalada calcium-ku-tiirsanaanta qaarkood (VDCCs), oo markaa u dhaqma sidii horjooge α2δ qayb-hoosaad-ka kooban VDCCs.Waxaa jira laba qaybood oo ah α2δ-ku-xidha daroogada, α2δ-1 iyo α2δ-2, iyo pregabalin waxay muujineysaa isku mid ahaanshaha (iyo markaa la'aanta xulashada u dhaxaysa) labadan goobood.Pregabalin waxay dooratay inay ku xidho qaybta α2δ VDCC.In kasta oo xaqiiqda ah in pregabalin uu yahay analoogga GABA, kuma xidhna soo-dhoweeyayaasha GABA, uma beddelo GABA ama GABA reseptor agonist gudaha vivo, oo si toos ah uma beddelo gaadiidka GABA ama dheef-shiid kiimikaadka.Si kastaba ha ahaatee, pregabalin ayaa la ogaaday in ay soo saarto qiyaasta ku-tiirsanaanta qiyaasta maskaxda ee muujinta maskaxda ee L-glutamic acid decarboxylase (GAD), enzyme ka masuulka ah isku-darka GABA, oo markaa waxay yeelan kartaa saameyn aan toos ahayn GABAergic iyadoo kordhinaysa heerarka GABA ee maskaxda.Hadda ma jiraan wax caddayn ah oo muujinaya in saamaynta pregabalin ay dhexdhexaadinayaan habab kasta oo aan ka ahayn xannibaadda α2δ-ka kooban VDCCs.Iyadoo la raacayo, xannibaadda α2δ-1-ka kooban VDCCs ee pregabalin waxay u muuqataa inay mas'uul ka tahay saameynteeda anticonvulsant, xanuunka xanuunka, iyo anxiolytic.
The endogenous α-amino acids L-leucine iyo L-isoleucine, kuwaas oo si dhow u eg pregabalin iyo gabapentinoids kale ee qaabdhismeedka kiimikada, waa seedaha muuqda ee α2δ VDCC hoostiisa oo la mid ah sida gabapentinoids (tusaale, IC50 = 71 nM ee L- isoleucine), waxayna ku jiraan dareeraha cerebrospinal ee bini'aadamka ee uruurinta micromolar (tusaale, 12.9 μM ee L-leucine, 4.8 μM ee L-isoleucine).Waxaa la saadaaliyay in ay noqon karaan ligands endogenous ee qaybta hoose iyo in ay si tartan ah uga soo horjeedaan saameynta gabapentinoids.Iyadoo la raacayo, halka gabapentinoids sida pregabalin iyo gabapentin ay leeyihiin namolar affinities ee qaybta α2δ, awooddooda ku jirta vivo waxay ku jiraan heerka ugu hooseeya ee micromolar, iyo tartanka loogu talagalay xidhitaanka asiidhyada L-amino acids ayaa la sheegay inay u badan tahay inay mas'uul ka yihiin khilaafkan.

Pregabalin waxaa la ogaaday in uu lahaado xidhiidh ka sarreeya 6-laab marka loo eego gabapentin ee α2δ subunit-ka kooban VDCCs hal daraasad.Si kastaba ha ahaatee, daraasad kale ayaa lagu ogaaday in pregabalin iyo gabapentin ay leeyihiin xiriir isku mid ah oo loogu talagalay dib-u-dhiska bini'aadamka α2δ-1 subunit (Ki = 32 nM iyo 40 nM, siday u kala horreeyaan).Si kastaba ha noqotee, pregabalin waa 2 ilaa 4 jeer ka awood badan gabapentin sida xanuunka xanuunka iyo, xayawaanka, waxay u muuqataa inay 3 ilaa 10 jeer ka awood badan tahay gabapentin sida anticonvulsant.