Pregabalin ntabwo ari GABAA cyangwa GABAB reseptor agonist.
Pregabalin ni gabapentinoid kandi ikora mukubuza imiyoboro ya calcium. By'umwihariko ni ligand ya site yubufasha α2δ subunit yumurongo wa calcium zimwe na zimwe ziterwa na calcium ya calcium (VDCCs), bityo ikora nkibuza α2δ subunit irimo VDCCs. Hariho ibiyobyabwenge bibiri bihuza α2δ subunits, α2δ-1 na α2δ-2, na pregabalin byerekana isano isa na (bityo rero kubura guhitamo hagati yizi mbuga zombi. Pregabalin iratoranya muguhuza kwayo α2δ VDCC subunit. Nuburyo pregabalin ari analogue ya GABA, ntabwo ihuza na reseptors ya GABA, ntabwo ihinduka GABA cyangwa indi reseptor ya GABA agonist muri vivo, kandi ntabwo ihindura byimazeyo transport ya GABA cyangwa metabolism. Nyamara, pregabalin yasanze itanga ubwiyongere bukabije bwubwonko bwerekana ubwonko bwa L-glutamic acide decarboxylase (GAD), enzyme ishinzwe guhuza GABA, bityo ikaba ishobora kugira ingaruka zimwe na zimwe za GABAergic zitaziguye mukongera urugero rwa GABA mubwonko. Kugeza ubu nta kimenyetso cyerekana ko ingaruka za pregabalin zahujwe nuburyo ubwo aribwo bwose uretse kubuza α2δ zirimo VDCC. Ukurikije, kubuza α2δ-1 irimo VDCCs na pregabalin bigaragara ko ari yo nyirabayazana w'ingaruka zayo za anticonvulsant, analgesic, na anxiolytique.
Endogenous α-amino acide L-leucine na L-isoleucine, bisa neza na pregabalin hamwe nizindi gabapentinoide mu miterere yimiti, ni ligande ya α2δ VDCC subunit ifitanye isano na gabapentinoide (urugero, IC50 = 71 nM kuri L- isoleucine), kandi biboneka mumazi ya cerebrospinal fluid yabantu kuri micromolar concentration (urugero, 12.9 μM kuri L-leucine, 4.8 μM kuri L-isoleucine). Byagaragaye ko bishobora kuba ligande ya endogenous ligands ya subunit kandi ko bashobora guhatanira kurwanya ingaruka za gabapentinoide. Ukurikije, mugihe gabapentinoide nka pregabalin na gabapentin bifite isano ya nanomolar kuri α2δ subunit, imbaraga zabo muri vivo ziri murwego rwa micromolar nkeya, kandi amarushanwa yo guhuza na acide endogenous L-amino bivugwa ko ashobora kuba nyirabayazana w'iri tandukaniro.

Pregabalin wasangaga afite inshuro 6 hejuru ya gabapentin kuri α2δ subunit irimo VDCCs mubushakashatsi bumwe. Ariko, ubundi bushakashatsi bwerekanye ko pregabalin na gabapentin bafitanye isano isa na recombinant yumuntu α2δ-1 subunit (Ki = 32 nM na 40 nM). Ibyo ari byo byose, pregabalin ikubye inshuro 2 kugeza kuri 4 kurusha gabapentin nka analgesic kandi, mu nyamaswa, bigaragara ko ifite imbaraga inshuro 3 kugeza 10 kurenza gabapentin nka anticonvulsant.