Pregabalin haisi GABAA kana GABAB receptor agonist.
Pregabalin inonzi gabapentinoid uye inoshanda nekudzivisa mamwe ma calcium channels. Kunyanya iyo ligand yemubatsiri α2δ subunit saiti yemamwe voltage-inotsamira karusiyamu migero (VDCCs), uye nekudaro inoshanda senge inhibitor ye α2δ subunit-ine VDCCs. Kune maviri zvinodhaka-anosunga α2δ subunits, α2δ-1 uye α2δ-2, uye pregabalin inoratidza hukama hwakafanana hwe (uye nekudaro kushaikwa kwekusarudza pakati) aya masayiti maviri. Pregabalin inosarudza mukusunga kwayo kune α2δ VDCC subunit. Pasinei nokuti pregabalin inonzi GABA analogue, haisungiri kuGABA receptors, haishanduki kuva GABA kana imwe GABA receptor agonist in vivo, uye haigadziri zvakananga GABA kutakura kana metabolism. Nekudaro, pregabalin yakawanikwa ichigadzira kuwedzera-kunoenderana nedosi mukutaura kwehuropi hweL-glutamic acid decarboxylase (GAD), iyo enzyme ine basa rekugadzira GABA, uye nekudaro inogona kuve neimwe isina kunanga GABAergic mhedzisiro nekuwedzera GABA mazinga muuropi. Ikozvino hapana humbowo hwekuti mhedzisiro ye pregabalin inopindirana neimwe nzira kunze kwekuvharirwa kwe α2δ-ine VDCCs. Maererano, inhibition ye α2δ-1-ine VDCCs ne pregabalin inoratidzika kuva inokonzera anticonvulsant, analgesic, uye anxiolytic madhara.
Iyo endogenous α-amino acids L-leucine uye L-isoleucine, iyo yakafanana nepregabalin uye imwe gabapentinoids mumakemikari chimiro, inoratidzika ligands eiyo α2δ VDCC subunit ine hukama hwakafanana neiyo gabapentinoids (semuenzaniso, IC50 = 71 nM yeL- isoleucine), uye iripo mumunhu cerebrospinal fluid pa micromolar kuisa pfungwa (semuenzaniso, 12.9 μM yeL-leucine, 4.8 μM yeL-isoleucine). Izvo zvave zvichitemerwa kuti vanogona kunge vari endogenous ligands ye subunit uye kuti vanogona kukwikwidza kupikisa mhedzisiro ye gabapentinoids. Zvinoenderana, nepo gabapentinoids senge pregabalin uye gabapentin iine nanomolar affinities yeiyo α2δ subunit, masimba avo mu vivo ari mune yakaderera micromolar renji, uye makwikwi ekusunga ne endogenous L-amino acids anonzi anogona kunge ari kukonzera kusawirirana uku.

Pregabalin yakawanikwa iine 6-yakapetwa yakakwirira hukama kupfuura gabapentin ye α2δ subunit-ine VDCCs mune imwe chidzidzo. Nekudaro, imwe ongororo yakawana kuti pregabalin negabapentin vaive nehukama hwakafanana hwea2δ-1 subunit yemunhu (Ki = 32 nM uye 40 nM, zvichiteerana). Chero zvazvingava, pregabalin inosvika 2 kusvika ku4 nguva yakawanda kupfuura gabapentin seanalgesic uye, mumhuka, inoratidzika kuva 3 kusvika ku10 nguva yakawanda kupfuura gabapentin se anticonvulsant.