I-Pregabalin ayikho i-GABAA okanye i-GABAB ye-receptor agonist.
I-Pregabalin yi-gabapentinoid kwaye isebenza ngokuthintela iziteshi ezithile ze-calcium. Ngokukodwa ligand yesiza esincedisayo se-α2δ yamajelo athile e-calcium axhomekeke kumbane (VDCCs), kwaye ngokwenjenjalo isebenza njenge-inhibitor ye-α2δ subunit-containing VDCCs. Kukho ii-subunits ezimbini ze-α2δ ezibophelela iziyobisi, i-α2δ-1 kunye ne-α2δ-2, kwaye i-pregabalin ibonisa ubudlelwane obufanayo (kwaye ngenxa yoko ukungabikho kokukhetha phakathi) kwezi ndawo zimbini. I-Pregabalin ikhetha ekubopheleleni kwayo kwi-subunit ye-α2δ VDCC. Nangona i-pregabalin i-analogue ye-GABA, ayibopheleli kwi-GABA receptors, ayiguquki kwi-GABA okanye enye i-GABA receptor agonist kwi-vivo, kwaye ayilungelelanisi ngokuthe ngqo ukuthutha kwe-GABA okanye imetabolism. Nangona kunjalo, i-pregabalin ifunyenwe ivelisa ukonyuka okuxhomekeke kwidosi kwinkcazo yengqondo ye-L-glutamic acid decarboxylase (GAD), i-enzyme enoxanduva lokwenza i-GABA, kwaye ngenxa yoko inokuba neziphumo ezingangqalanga ze-GABAergic ngokunyusa amanqanaba e-GABA engqondweni. Okwangoku akukho bungqina bokuba iziphumo ze-pregabalin zilawulwa yiyo nayiphi na indlela ngaphandle kokuvinjelwa kwe-α2δ-equlethe ii-VDCC. Ngokuhambelanayo, ukuvinjelwa kwe-α2δ-1-equlethe ii-VDCC nge-pregabalin kubonakala kuxanduva lwe-anticonvulsant, i-analgesic, kunye nemiphumo ye-anxiolytic.
I-alpha-amino acids engapheliyo i-L-leucine kunye ne-L-isoleucine, efana ngokusondeleyo ne-pregabalin kunye nezinye i-gabapentinoids kwisakhiwo sekhemikhali, zi-ligands ezicacileyo ze-α2δ VDCC subunit enobudlelwane obufanayo njenge-gabapentinoids (umz., IC50 = 71 nM ye-L- isoleucine), kwaye zikhona kulwelo lwe-cerebrospinal yomntu kwi-micromolar ugxininiso (umzekelo, i-12.9 μM ye-L-leucine, i-4.8 μM ye-L-isoleucine). Kuye kwachazwa ukuba banokuba yi-endogenous ligands ye-subunit kwaye banokukhuphisana nemiphumo ye-gabapentinoids. Ngokungqinelanayo, ngelixa i-gabapentinoids efana ne-pregabalin kunye ne-gabapentin zine-nanomolar affinities ye-α2δ subunit, amandla abo kwi-vivo akuluhlu oluphantsi lwe-micromolar, kwaye ukhuphiswano lokubophelela nge-endogenous L-amino acids kuthiwa lunokuba luxanduva loku mahluko.

I-Pregabalin yafunyanwa inobudlelwane obuphindwe ka-6 obuphezulu kune-gabapentin ye-α2δ equlethe ii-VDCCs eziqulathe i-subunit kwisifundo esinye. Nangona kunjalo, olunye uphononongo lwafumanisa ukuba i-pregabalin kunye ne-gabapentin zinee-affinities ezifanayo kwi-subunit yabantu α2δ-1 (Ki = 32 nM kunye ne-40 nM, ngokulandelanayo). Kwimeko nayiphi na into, i-pregabalin i-2 kumaxesha e-4 anamandla ngaphezu kwe-gabapentin njenge-analgesic kwaye, kwizilwanyana, ibonakala ngathi i-3 kumaxesha angama-10 anamandla ngaphezu kwe-gabapentin njenge-anticonvulsant.