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. 2020 Sep 17;179(14):3529–3541. doi: 10.1111/bph.15248

TABLE 1.

Agonist ligands with activity at GPR84

Compound name Reported potency (EC50) Model system (in vitro, ex vivo) Comment References
Orthosteric
Decanoic acid (C10)

Human:

0.8–20.0 μM b

4.5–25.1 μM a

48 mM a

‐Recombinant system

‐RAW264.7 cells

‐Mouse bone marrow‐derived macrophages

‐Mouse primary cultured microglia

‐3T3‐L1 adipocytes

Wang et al., 2006

Nagasaki et al., 2012

Suzuki et al., 2013

Southern et al., 2013

Nikaido et al., 2015

Pillaiyar et al., 2017

Wei, Tokizane, Konishi, Yu, & Kiyama, 2017

Al Mahmud et al., 2017

Recio et al., 2018

Puengel et al., 2020

Lucy et al., 2019

Embelin

Human:

89–200 nM b

0.63 μM a

0.4 μM c

Mouse:

220 nM b

‐Recombinant system

‐Human monocyte‐derived macrophages

‐Mouse peritoneal macrophages

‐Human blood‐derived neutrophils

‐Mouse blood‐derived neutrophils

‐Mouse primary cultured microglia

‐Human monocyte

‐Rat neutrophils

Hakak, Unett, Gatlin, & Liaw, 2007

Southern et al., 2013

Al Mahmud et al., 2017

Wei et al., 2017

Pillaiyar et al., 2017

Gaidarov et al., 2018

Puengel et al., 2020

6‐OAU

Human:

14–438 nM b

1.74–11 μM c

512 nM a

‐Recombinant system

‐Mouse primary cultured microglia

‐Bone marrow‐derived macrophages

‐Human peripheral polymorphonuclear leukocyte

‐U937 cells differentiated into macrophage‐like cells

‐Human monocytes

Suzuki et al., 2013

Liu et al., 2016

Zhang, Yang, Li, & Xie, 2016

Wei et al., 2017

Recio et al., 2018

Lucy et al., 2019

PSB‐1584

Human:

5 nM b

3.2 nM c

‐Recombinant system Tritium‐labelled form of this compound is available ([3H]PSB‐1584) d

Pillaiyar et al., 2018

Köse et al., 2020

2‐HTP

(Compound 1 or ZQ‐16)

Human:

1–144 nM b

0.79–28.8 nM a

597 nM c

Mouse:

30.2 nM a

‐Recombinant system

‐THP‐1 monocytes

‐RAW264.7 cells

‐Mouse bone marrow‐derived neutrophils

‐Human blood‐derived neutrophils

‐Human monocytes

‐Human monocyte‐derived macrophages

‐Mouse bone marrow‐derived macrophages

Zhang et al., 2016

Liu et al., 2016

Al Mahmud et al., 2017

Sundqvist et al., 2018

Mancini et al., 2019

Lucy et al., 2019

DL‐175

Human:

33 nM b

‐Recombinant system

‐Mouse bone marrow‐derived macrophages

‐U937 cells differentiated into macrophage‐like cells

‐Human monocytes

Displays bias agonism for Gi‐protein signalling pathway over arrestin recruitment compared with 6‐OAU Lucy et al., 2019
Allosteric
DIM

Human:

0.25–1.25 μM b

0.5–1 μM a

5.9 mM a

Mouse:

4.26 μM a

‐Recombinant system

‐RAW264.7 cells

PSB‐15160 and PSB‐16671 are DIM analogues that display bias compared with DIM towards Gi‐mediated adenylyl cyclase inhibition over arrestin recruitment e

Wang et al., 2006

Nikaido et al., 2015

Zhang et al., 2016

Al Mahmud et al., 2017

Pillaiyar et al., 2017

Mancini et al., 2019

Note: Note comments in the text about reported potency values and potential issues of receptor reserve.

a

Potency values were generated using [35S]GTPγS assay.

b

Potency values were generated using cAMP assay.

c

Potency values were generated using β‐arrestin recruitment assay.

d

Köse et al. (2020).

e

Pillaiyar et al. (2017) and Mancini et al. (2019).