Direct neuronal protection by the protease-activated receptor PAR4
antagonist ML354 after experimental stroke in mice
Abstract
Background and Purpose Thrombo-inflammation is a key feature of stroke
pathophysiology and provides multiple candidate drug targets. Thrombin
exerts coagulation-independent actions via protease-activated receptors
(PAR), of which PAR1 has been implicated in stroke-associated
neuro-inflammation. The role of PAR4 in this context is less clear. This
study examined if the selective PAR4 antagonist ML354 provides
neuroprotection in experimental stroke and explored the underlying
mechanisms. Experimental Approach Mouse primary cortical neurons were
exposed to oxygen-glucose deprivation (OGD) and simulated reperfusion ±
ML354. For comparison, functional Ca2+-imaging was performed upon acute
stimulation with a PAR4 activating peptide or glutamate. Male mice
underwent sham operation or transient middle cerebral artery occlusion
(tMCAO), with ML354 or vehicle treatment beginning at recanalization. A
subset of mice received a platelet-depleting antibody. Stroke size and
functional outcome were assessed. Abundance of target genes, proteins
and cell markers was determined in cultured cells and tissues by qPCR,
immunoblotting and immunofluorescence. Key Results Stroke upregulates
PAR4 expression in cortical neurons in vitro and in vivo. OGD augments
spontaneous and PAR4-mediated neuronal activity; ML354 suppresses
OGD-induced neuronal excitotoxicity and apoptosis. ML354 applied in vivo
after tMCAO reduces infarct size, apoptotic markers, macrophage
accumulation and interleukin-1β expression. Platelet depletion did not
affect infarct size in mice with tMCAO ± ML354. Conclusions and
Implications Selective PAR4 inhibition during reperfusion improves
infarct size and neurological function after experimental stroke by
blunting neuronal excitability, apoptosis and local inflammation. PAR4
antagonists may provide additional neuroprotective benefits in patients
with acute stroke beyond their canonical antiplatelet action.