Table 2.

Antagonists that target α9-containing nAChRs, mechanism of action, and effects in models of pain and inflammation.

Ligand	Mechanism of Action	Disease Model	Pharmacological Effects	Ref.
Vc1.1	Antagonist	CCI-induced neuropathic pain	Reduced mechanical allodynia, mechanical hyperalgesia, infiltration of immune cells; disease modifying effects.	[75, 81]
Mr1.1	Antagonist	CCI-induced neuropathic pain	Reduced mechanical hyperalgesia.	[79]
RgIA	Antagonist	CCI-induced neuropathic pain CIN	Reduced mechanical allodynia and mechanical hyperalgesia, infiltration of immune cells. Reduced mechanical hyperalgesia, cold allodynia; disease modifying effects	[81] [83, 115]
RgIA4	Antagonist	CIN	Reduced mechanical hyperalgesia and cold allodynia; disease modifying effects.	[84, 85, 116]
RgIA-5474	Antagonist	CIN	Prevention of cold allodynia induction.	[89]
RgIA-5628	Antagonist	CIN	Prevention of cold allodynia induction.	[87]
RgIA-5524	Antagonist	CIN	Prevention of cold allodynia induction.	[90]
GeXIVA	Antagonist	CCI-induced neuropathic pain CIN	Reduced mechanical hyperalgesia. Long-lasting inhibition of mechanical and cold allodynia.	[88] [91, 117]
ZZ-204 G	Antagonist	CCI-induced neuropathic pain Formalin-induced inflammatory pain	Reduced mechanical hyperalgesia Reduced inflammatory pain.	[92] [92]
ZZ1–61c	Antagonist	CIN	Reduced mechanical allodynia and mechanical hyperalgesia.	[93]

CCI, chronic constriction injury; CIN, chemotherapeutic-induced neuropathic pain.