Table Info

Table 2.

Pharmacological compounds. Major pharmacological compounds used in the literature for investigation of the roles of S1P and LPA receptors

Compound	Receptor targets	Role	Reference
S1P receptor targeting agents
Fingolimod^*	S1P₁, S1P₃, S1P₄, S1P₅	Agonist (functional antagonist)	[13, 14]
SEW2871	S1P₁	Agonist	[15, 16]
W146	S1P₁	Antagonist	[17]
LPA receptor targeting agents
Ki16425	LPA₁, LPA₃	Antagonist	[18]
AM095	LPA₁	Antagonist	[19]
TCLPA5	LPA₅	Antagonist	[20]

^* Fingolimod is phosphorylated in vivo, and fingolimod-phosphate is the active agonist. Furthermore, although fingolimod is a S1P receptor agonist, it often acts as a functional antagonist by causing receptor internalization and degradation [21, 22]

Declarations

Acknowledgments

I would like to thank Dr. Daniel Stovall, Layla Herndon and Mallika Singh for critical reading of the manuscript.

Author contributions

EB: Writing—original draft, Writing—review & editing.

Conflicts of interest

The author declares no conflicts of interest.

Ethical approval

Not applicable.

Consent to participate

Not applicable.

Consent to publication

Not applicable.

Availability of data and materials

Not applicable.

Funding

E.B. was supported by the National Institute of General Medical Sciences of the National Institutes of Health [P20GM103499]. The funders had no role in study design, data collection and analysis, decision to publish, or preparation of the manuscript.

Copyright

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