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. Author manuscript; available in PMC: 2021 Jul 1.
Published in final edited form as: Pharmacol Ther. 2020 Mar 19;211:107529. doi: 10.1016/j.pharmthera.2020.107529

Table 5 —

GPCRs that are potential targets for pharmacotherapy in sepsis

Endogenous target Pharmacothe rapy Anticipated effects
Adenosine receptors A2A receptor blockade Immune stimulation and mitigation of inflammation
A3 receptor activation
Adrenoceptors β-adrenoceptor stimulation Modification of cytokine expression profile of immune cells
Complement receptors C3aR1 modulation Re-establishment of vascular endothelial barrier
C5aR1 modulation
Chemokine receptors ACKR2 activation Blockade of cytokine storm during hyper-inflammatory phase of sepsis
CCR2 blockade
CCR5 activation
CX3CR1 stimulation
Coagulation cascade PAR1 modulation Restoration of physiologic endothelial function
Cannabinoid receptors CB1 and CB2 receptor modulation Alleviation of sepsis-induced multi-organ dysfunction
Endothelin receptors ETA receptor blockade and ETB1 receptor stimulation Restoration of mitochondrial oxidative phosphorylation and alleviation of sepsis-induced hypoperfusion
LPI receptor LPI1 receptor blockade Reconstitution of the blood-gut barrier
Sphingosine-1-phosphate S1P1 receptor stimulation Re-establishment of vascular endothelial barrier
Melatonin receptors MT1 and MT2 receptor stimulation Normalization of pineal gland-immune axis
Resolvin receptors FPR2 and DRV2 receptor stimulation Enhancing bacterial clearance and promoting resolution of inflammation
Ghrelin receptor GHS-R stimulation Immune stimulation and mitigation of inflammation
Hydroxycarboxylic acid receptors HCAR2 stimulation Reconstitution of the blood-gut barrier and intestinal microbiome
Urotensin II receptors Urotensin II receptor blockade Alleviation of sepsis-induced multi-organ dysfunction

ACKR2 = Atypical chemokine receptor 2; C3aR1 = complement protein 3a receptor 1; C5aR1 = complement protein 5a receptor 1; CB = cannabinoid; CCR = CC-chemokine receptor; CX3CR = CX3C chemokine receptor; DRV2 = D-series resolvin 2 receptor; ET = endothelin; FPR = formylpeptide receptor; GHS-R = growth hormone secretagogue receptor; GPCR = G protein-coupled receptor; HCAR = hydroxycarboxylic acid receptor; LPI = lysophosphatidylinositol; MT = melatonin; PAR = protease-activated receptor; S1P = sphingosine-1-phosphate.