Table 3.

Small molecules that target nAChRs containing α7, α9, or α10 subunits, mechanism of action, and pharmacological effects.

Ligand	Receptor Target	Mechanism of Action	Pharmacological Effect	Ref.
Choline	α7 α9α10	agonist partial agonist	Decreased TNF-α release from mouse macrophages; inhibition of IL-1β from primary human monocytes.	[21,98]
CDP-choline	α7	agonist	Reduced oxaliplatin-induced neuropathic pain in mice; reversal of CCI-induced mechanical hyperalgesia in mice; decreased mechanical hyperalgesia and paw edema in carrageenan-induced inflammatory pain.	[100–102]
Phosphocholine	α9α10	agonist	Inhibition of IL-1β from human U937 monocytes, monocytic THP-1, THP-1 derived M1-like macrophages, primary monocytes, and PBMCs.	[21,22]
pCF3 diEPP	α9α10	partial agonist	Inhibition of TNF-α, IL-1β, and Il-6 release from whole human blood cultures; reduced IL-1β release from PBMCs, monocytic THP-1, THP-1 derived M1-like macrophages, and primary monocytes.	[97]

CDP-choline; cytidine-5′-diphosphate choline; PBMCs, peripheral blood mononuclear cells.