Table 1.
Chemicals identified as having positive allosteric modulator activity at P2X receptors.
| Drug name | Target Receptor | Predicted PAM effect (Type I, II, mixed) |
Reference |
|---|---|---|---|
| MRS2219 | P2X1 (rat) | Unknown | (Jacobson et al., 1998) |
| Gintonin | P2X1 (rat) | Unknown | (Sun-Hye et al., 2013) |
| PIP2 | P2X1 (rat) | Type I | (Bernier et al., 2008a) |
| PSB-10129 | P2X2 (rat) | Type I | (Baqi et al., 2011) |
| DHEA | P2X2 (rat) P2X2/3 (rat) |
Type II | (De Roo et al., 2003) |
| Progesterone | P2X2 (rat) | Type II | (De Roo et al., 2010) |
| Testosterone butyrate | P2X2, P2X4 |
Type II Mixed Type I/II |
(Sivcev et al., 2019) |
| Ivermectin | P2X4 (rat) P2X4 (human) P2X7 (human) |
Mixed Type I/II Mixed Type I/II |
(Khakh et al., 1999) (Priel and Silberberg, 2004) (Nörenberg et al., 2012) |
| Abamectin | P2X4 (rat) | Unknown | (Asatryan et al., 2014) |
| Selamectin | P2X4 (rat) | Unknown | (Asatryan et al., 2014) |
| Moxidectin | P2X4 | Unknown | (Huynh et al., 2017) |
| Cibacron blue | P2X4 (rat) | Unknown | (Miller et al., 1998) |
| Alfaxolone | P2X4 (rat) | Unknown | (Codocedo et al., 2009) |
| Allopregnanolone | P2X4 (rat) | Unknown | (Codocedo et al., 2009) |
| THDOC | P2X4 (rat) | Unknown | (Codocedo et al., 2009) |
| Ginsenoside CK | P2X7 (human), P2X7 (mouse) P2X4 (human) |
Mixed Type I/II Mixed Type I/II Mixed Type I/II |
(Helliwell et al., 2015) (Bidula et al., 2019a) (Dhuna et al., 2019) |
| Ginsenoside Rd | P2X7, P2X4 |
Unknown Unknown |
(Helliwell et al., 2015) (Dhuna et al., 2019) |
| Clemastine | P2X7 (human) | Type II | (Norenberg et al., 2011) |
| Tenidap | P2X7 (mouse) | Mixed Type I/II | (Sanz et al., 1998) |
| Polymyxin B | P2X7 | Mixed Type I/II | (Ferrari et al., 2004) |
| Garcinolic acid | P2X7 (human) | Unknown | (Fischer et al., 2014) |
| Agelastine | P2X7 (human) | Unknown | (Fischer et al., 2014) |
| GW791343 | P2X7 (rat) | Mixed Type I/II | (Michel et al., 2008a) |
A Type I positive allosteric modulator (PAM) effect increases efficacy whereas a Type II PAM effect increases sensitivity to agonist seen as a left-ward shift in the concentration response curve. A mixed Type I/II PAM effect represents both features.