Selected examples of allosteric modulators of GPCRs
| Receptor | Example Modulator(s) | References |
|---|---|---|
| Adenosine A1 | PD 81,723; PD 117,975 | Bruns and Fergus, 1990;Bhattacharya and Linden, 1995; Kollias-Baker et al., 1997; Musser et al., 1999;Kourounakis et al., 2001 |
| Adenosine A2A | Amilorides | Gao and Ijzerman, 2000 |
| Adenosine A3 | VU5455 VU8504 | Gao et al., 2001 |
| Adrenoceptor α1 | Amilorides; Benzodiazepines | Waugh et al., 1999; Leppik et al., 2000 |
| Adrenoceptor α2A, α2B | Amiloride | Nunnari et al., 1987;Wilson et al., 1991; Leppik et al., 1998;Leppik and Birdsall, 2000 |
| Adrenoceptor α2D | Agmatine | Molderings et al., 2000 |
| Calcium Sensing Receptor | NPS 467; NPS 568; l-amino acids | Hammerland et al., 1998; Conigrave et al., 2000b |
| Chemokine CXCR3 | IP-10; I-TAC | Cox et al., 2001 |
| Chemokine CCR5, CXCR4 | Trichosanthin | Zhao et al., 1999 |
| Chemokine CCR1, CCR3 | UCB35625 | Sabroe et al., 2000 |
| Dopamine D1 | Zinc | Schetz and Sibley, 1997 |
| Dopamine D2 | Amilorides, zinc | Hoare and Strange, 1996; Schetz et al., 1999 |
| Endothelin ETA | Aspirin, sodium salicylate | Blandin et al., 2000; Talbodec et al., 2000 |
| GABAB | CGP7930; CGP13501 | Urwyler et al., 2001 |
| Glutamate mGluR1 | CPCCOEt, Ro 67-7476, Ro 01-6128; BAY36-7620 | Litschig et al., 1999; Carroll et al., 2001; Knoflach et al., 2001 |
| Glutamate mGluR5 | MPEP | Pagano et al., 2000;Spooren et al., 2001 |
| Muscarinic M1–M5 | Gallamine, alcuronium, brucine, dimethyl-W84 | Clark and Mitchelson, 1976;Stockton et al., 1983; Knaus et al., 1991; Proska and Tucek, 1994; Lazareno and Birdsall, 1995; Traenkle et al., 1998 |
| Neurokinin NK1 | Heparin | Knaus et al., 1991 |
| Purine P2Y1 | 2,2′-pyridylsatogen tosylate | Spedding et al., 1975; King et al., 1996 |
| Serotonin 5-HT1B/1D | 5-HT moduline | Fillion et al., 1996; Massot et al., 1998 |
| Serotonin 5-HT2A | Oleamide | Thomas et al., 1997 |
| Serotonin 5-HT7 | Oleamide | Thomas et al., 1997; Hedlund et al., 1999 |