Pregabalin ma aha GABAA ama GABAB agonist.
Pregabalin waa gabapentinoid wuxuuna u dhaqmaa isagoo joojinaya kanaalada kaalshiyamka qaarkood. Gaar ahaan waa isku-xidhka kaaliyaha α2δ-subnit-ka ee kanaalada kaalshiyamka-ku-tiirsanaanta qaarkood (VDCCs), oo markaa u dhaqma sidii horjooge α2δ-hoosaadka-ka kooban VDCCs. Waxaa jira laba qaybood oo ah α2δ-ku-xidhitaan daroogo, α2δ-1 iyo α2δ-2, iyo pregabalin waxay muujinaysaa xidhiidh la mid ah (iyo markaa la'aanta xulashada u dhaxaysa) labadan goobood. Pregabalin waa mid door ah iyada oo ku xidhan qaybta α2δ VDCC. In kasta oo xaqiiqda ah in pregabalin uu yahay analoogga GABA, kuma xidhna soo-dhoweeyayaasha GABA, uma beddelo GABA ama GABA agonist receptor kale oo ku jira 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 waxaa laga yaabaa inay leedahay 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 ugu 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), oo waxay ku jiraan dareeraha cerebrospinal ee bini'aadamka ee uruurinta micromolar (tusaale, 12.9 μM L-leucine, 4.8 μM L-isoleucine). Waxaa la soo jeediyay 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 qiyaasta micromolar hoose, iyo tartanka loogu talagalay isku-xidhka asiidhyada L-amino acids ayaa la sheegay inay u badan tahay inay mas'uul ka yihiin khilaafkan.

Pregabalin waxaa la ogaaday in uu leeyahay 6-laab xidhiidh ka sarreeya kan gabapentin ee α2δ qayb-hoosaad ka kooban VDCC-yada 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-dhaqaajinta bini'aadamka α2δ-1 subunit (Ki = 32 nM iyo 40 nM, siday u kala horreeyaan). Si kastaba ha ahaatee, 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.