Table 2.

Pharmacological properties of P2X1 receptor modulators. EC50 or IC50 values are recorded as nM values with respect to P2X1 activity. Letters in activity column designate P2X1 receptor origin with m for mouse, r for rat and h for human

Compound	P2X1 Activity (nM)	Source	Mode of action
ATP	56 (h), 100–300 (r)	[37, 73, 108]	Agonist
α,β-meATP	200 (h), 3200 (r)	[37, 108]	Agonist
2-MeSATP	54 (h), 100 (r)	[37, 108]	Agonist
BzATP	1.8 (h), 24,200 (r)	[37, 108]	Agonist
Ap6A	1120 (h), 600–720 (r)	[37, 73, 108]	Agonist
TNP-ATP	1 (r), 6 (h)	[108–110]	Antagonist
IP5I	3.1 (r)	[74, 108, 109]	Antagonist
Suramin	851 (h), 1700 (r)	[37, 108]	Antagonist
NF449	0.05 (h), 0.28–0.29 (r)	[75, 111, 112]	Antagonist
PPADS	1820 (h), 69 (r)	[37, 109]	Antagonist
PPNDS	14 (r)	[113]	Antagonist
MRS2159	9.4 (r)	[77, 109]	Antagonist
MRS2219	5900 (r)	[81]	PAM
Aurintricarboxylic acid (ATA)	8.6 (r)	[79]	Antagonist
PSB-2001	19 (h)	[78]	Antagonist
1	236 (m)	[76, 114, 115]	Antagonist
2	14,000 (r)	[80]	Antagonist
3	602 (h)	[116]	Antagonist
4	100,000 (h)	[117]	Antagonist
5	3000 (h)	[118]	Antagonist