Pregabalin tsis yog GABAA lossis GABAB receptor agonist.
Pregabalin yog gabapentinoid thiab ua los ntawm inhibiting qee cov calcium channels. Tshwj xeeb nws yog ligand ntawm lub koom haum α2δ subunit site ntawm qee qhov hluav taws xob-nyob ntawm calcium channels (VDCCs), thiab yog li ua tus inhibitor ntawm α2δ subunit-muaj VDCCs. Muaj ob hom tshuaj-binding α2δ subunits, α2δ-1 thiab α2δ-2, thiab pregabalin qhia zoo sib xws rau (thiab yog li tsis muaj kev xaiv ntawm) ob qhov chaw no. Pregabalin yog xaiv hauv nws txoj kev khi rau α2δ VDCC subunit. Txawm hais tias qhov tseeb tias pregabalin yog GABA analogue, nws tsis khi rau GABA receptors, tsis hloov mus rau GABA lossis lwm tus GABA receptor agonist hauv vivo, thiab tsis ncaj qha hloov GABA thauj lossis metabolism. Txawm li cas los xij, pregabalin tau pom los tsim cov koob tshuaj nce ntxiv hauv lub hlwb qhia ntawm L-glutamic acid decarboxylase (GAD), enzyme lub luag haujlwm rau kev sib txuas GABA, thiab yog li no tej zaum yuav muaj qee qhov cuam tshuam GABAergic los ntawm kev nce GABA qib hauv lub hlwb. Tam sim no tsis muaj pov thawj tias qhov cuam tshuam ntawm pregabalin yog kho los ntawm ib qho kev ua haujlwm uas tsis yog inhibition ntawm α2δ-muaj VDCCs. Raws li, inhibition ntawm α2δ-1-muaj VDCCs los ntawm pregabalin zoo li ua lub luag haujlwm rau nws cov tshuaj tiv thaiv kab mob, tshuaj tua kab mob, thiab kev ntxhov siab.
Cov endogenous α-amino acids L-leucine thiab L-isoleucine, uas zoo ib yam li pregabalin thiab lwm yam gabapentinoids hauv cov qauv tshuaj, yog pom tseeb ligands ntawm α2δ VDCC subunit nrog affinity zoo li gabapentinoids (xws li, IC50 = 71 nM rau L. isoleucine), thiab muaj nyob rau hauv tib neeg cerebrospinal kua ntawm micromolar concentrations (piv txwv li, 12.9 μM rau L-leucine, 4.8 μM rau L-isoleucine). Nws tau raug theorized tias lawv yuav yog cov ligands endogenous ntawm lub subunit thiab hais tias lawv yuav sib tw antagonize cov teebmeem ntawm gabapentinoids. Raws li, thaum gabapentinoids zoo li pregabalin thiab gabapentin muaj nanomolar affinities rau α2δ subunit, lawv cov potencies hauv vivo yog nyob rau hauv qis micromolar ntau yam, thiab kev sib tw rau kev khi los ntawm endogenous L-amino acids tau hais tias yuav muaj lub luag haujlwm rau qhov tsis sib xws.

Pregabalin tau pom tias muaj 6-fold ntau dua affinity dua gabapentin rau α2δ subunit-muaj VDCCs hauv ib txoj kev tshawb fawb. Txawm li cas los xij, lwm txoj kev tshawb nrhiav pom tias pregabalin thiab gabapentin muaj qhov sib xws rau tib neeg recombinant α2δ-1 subunit (Ki = 32 nM thiab 40 nM, feem). Nyob rau hauv txhua rooj plaub, pregabalin yog 2 mus rau 4 lub sij hawm ntau zog tshaj gabapentin raws li ib tug analgesic thiab, nyob rau hauv cov tsiaj, zoo li 3 mus rau 10 lub sij hawm ntau haib tshaj gabapentin raws li ib tug anticonvulsant.