I-Pregabalin ayiyona i-GABAA noma i-GABAB receptor agonist.
I-Pregabalin iyi-gabapentinoid futhi isebenza ngokuvimbela iziteshi ezithile ze-calcium. Ikakhulukazi iwumgogodla wesiza se-α2δ subunit site yamashaneli e-calcium ancike ku-voltage (VDCCs), futhi ngokwenza kanjalo isebenza njengesivimbeli sama-VDCC aqukethe i-α2δ subunit. Kunama-subunits amabili e-α2δ abopha izidakamizwa, i-α2δ-1 kanye ne-α2δ-2, futhi i-pregabalin ibonisa ukuhlobana okufanayo (ngakho-ke ukuntuleka kokukhetha phakathi) kwalawa masayithi amabili. I-Pregabalin iyakhetha ekubophezeleni kwayo kuyunithi encane ye-α2δ VDCC. Naphezu kweqiniso lokuthi i-pregabalin iyi-analogue ye-GABA, ayibophezeli kuma-receptors e-GABA, ayiguquli ibe yi-GABA noma enye i-GABA receptor agonist ku-vivo, futhi ayishintshi ngokuqondile ukuthutha kwe-GABA noma i-metabolism. Kodwa-ke, i-pregabalin itholwe ikhiqiza ukwanda okuncike kumthamo ekukhulumeni kobuchopho kwe-L-glutamic acid decarboxylase (GAD), i-enzyme ebhekele ukwenziwa kwe-GABA, futhi ngenxa yalokho ingaba nemiphumela engaqondile ye-GABAergic ngokwandisa amazinga e-GABA ebuchosheni. Okwamanje abukho ubufakazi bokuthi imiphumela ye-pregabalin ilamula nganoma iyiphi indlela ngaphandle kokuvinjelwa kwama-VDCC aqukethe i-α2δ. Ngokuvumelana nalokho, ukuvinjelwa kwe-α2δ-1-aqukethe i-VDCC nge-pregabalin kubonakala kunesibopho semiphumela yayo ye-anticonvulsant, analgesic, kanye ne-anxiolytic.
Ama-alpha-amino acid e-alpha-amino acid L-leucine kanye ne-L-isoleucine, afana ngokuseduze ne-pregabalin namanye ama-gabapentinoid esakhiweni samakhemikhali, angama-ligand we-α2δ VDCC subunit enobudlelwane obufana ne-gabapentinoids (isb, IC50 = 71 nM ye-L- isoleucine), futhi zikhona oketshezini lwe-cerebrospinal yomuntu ku-micromolar ukugxila (isb, 12.9 μM ye-L-leucine, 4.8 μM ye-L-isoleucine). Kuye kwacatshangwa ukuthi zingase zibe yi-endogenous ligands ye-subunit nokuthi zingase ziphikisana nemiphumela ye-gabapentinoids ngokuncintisana. Ngokuvumelanayo, kuyilapho ama-gabapentinoid afana ne-pregabalin ne-gabapentin ane-nanomolar affinities ye-α2δ subunit, amandla awo ku-vivo akubanga eliphansi le-micromolar, futhi ukuncintisana kokubopha ngama-endogenous L-amino acids kuthiwa kungenzeka kube yimbangela yalokhu kuhluka.

I-Pregabalin itholwe inokusondelana okuphindwe izikhathi ezi-6 kune-gabapentin ye-α2δ equkethe i-subunit VDCC ocwaningweni olulodwa. Kodwa-ke, olunye ucwaningo lwathola ukuthi i-pregabalin ne-gabapentin zazinokuhlobana okufanayo kwe-subunit ehlanganisiwe ye-α2δ-1 (Ki = 32 nM kanye ne-40 nM, ngokulandelana). Kunoma yikuphi, i-pregabalin inamandla izikhathi ezi-2 kuya kwezi-4 kune-gabapentin njenge-analgesic futhi, ezilwaneni, ibonakala inamandla izikhathi ezi-3 kuya kweziyi-10 kune-gabapentin njenge-anticonvulsant.