Pregabalin ntabwo ari GABAA cyangwa GABAB reseptor agonist.
Pregabalin ni gabapentinoid kandi ikora mukubuza imiyoboro ya calcium.By'umwihariko ni ligand ya site ya auxiliary α2δ subunit ya sisitemu zimwe na zimwe ziterwa na calcium ya calcium (VDCCs), bityo ikora nka inhibitor ya α2δ subunit irimo VDCCs.Hano hari 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 α2δ VDCC subunit.Nuburyo pregabalin ari analogue ya GABA, ntabwo ihuza na reseptor ya GABA, ntabwo ihinduka GABA cyangwa indi reseptor agonist ya GABA muri vivo, kandi ntabwo ihindura ubwikorezi bwa GABA cyangwa metabolism.Nyamara, pregabalin yasanze itanga ubwiyongere bukabije bwubwonko bwerekana ubwonko bwa L-glutamic acide decarboxylase (GAD), enzyme ishinzwe guhuza GABA, bityo rero ikaba ishobora kugira ingaruka zitaziguye GABAergic mukwongera urwego rwa GABA mubwonko.Kugeza ubu nta kimenyetso cyerekana ko ingaruka za pregabalin zahujwe nuburyo ubwo aribwo bwose uretse kubuza α2δ irimo VDCC.Ukurikije, kubuza α2δ-1 irimo VDCCs na pregabalin bigaragara ko ari yo nyirabayazana wa anticonvulsant, analgesic, na anxiolytic.
Endogenous α-amino acide L-leucine na L-isoleucine, bisa neza na pregabalin hamwe nizindi gabapentinoide mu miterere yimiti, bigaragara ko ari ligande ya α2δ VDCC subunit ifitanye isano na gabapentinoide (urugero, IC50 = 71 nM kuri L- isoleucine), kandi biboneka mumazi yubwonko bwabantu kuri micromolar concentration (urugero, 12.9 μM kuri L-leucine, 4.8 μM kuri L-isoleucine).Byashimangiwe ko bashobora kuba ligande ya endogenous ya subunit kandi ko bashobora guhangana ningaruka 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 guhatanira guhuza na acide endogenous L-amino byavuzwe ko bishoboka ko ari yo nyirabayazana.

Pregabalin wasangaga afite inshuro 6 kurenza 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.