Exploration of Neuroprotective Therapy

From: Lysophospholipid receptors in neurodegeneration and neuroprotection

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]

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^* 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]