Table 5.
Binding affinity profile for (±)-MDMA with values for Ki reported in nM. Radioligand binding assays were performed using stably or transiently expressing cell lines (HEK, HEKT, or CHO) unless noted otherwise.
| Receptor | Radiolabeled Ligand |
Ligand Classification |
Species | Ki (nM) | Reference |
|---|---|---|---|---|---|
| 5-HT1A | 3H-8-OH-DPAT | Agonist | Human | >10,000 | 77 |
| 5-HT1A | 3H-8-OH-DPAT | Agonist | Human | 12,200 | 62 |
| 5-HT 1B | 3H-GR-125743 | Antagonist | Human | >10,000 | 77 |
| 5-HT 1D | 3H-GR-125743 | Antagonist | Human | >10,000 | 77 |
| 5-HT 1E | 3H-5-HT | Agonist | Human | >10,000 | 77 |
| 5-HT2A | 3H-Ketanserin | Antagonist | Rat | >10,000 | 77 |
| 5-HT2A | 3H-Ketanserin | Antagonist | Human | 7,800 | 62 |
| 5-HT2B | 3H-LSD | Agonist | Human | 500 | 77 |
| 5-HT2C | 3H-Mesulergine | Antagonist | Rat | >10,000 | 77 |
| 5-HT2C | 3H-Mesulergine | Antagonist | Human | >13,000 | 62 |
| 5-HT3 | 3H-Zacopride | Antagonist | Human | >10,000 | 77 |
| 5-HT5 | 3H-LSD | Agonist | Human | >10,000 | 77 |
| 5-HT6 | 3H-LSD | Agonist | Human | >10,000 | 77 |
| 5-HT7 | 3H-LSD | Agonist | Human | >10,000 | 77 |
| Alpha1A | 125I-HEAT | Antagonist | Human | >10,000 | 77 |
| Alpha1A | 3H-Prazosin | Inverse Agonist | Human | >6,000 | 62 |
| Alpha1B | 125I-HEAT | Antagonist | Human | >10,000 | 77 |
| Alpha2A | 3H-Clonidine | Agonist | Human | 2,532 | 77 |
| Alpha2A | 3H- Rauwolscine | Antagonist | Human | 15,000 | 62 |
| Alpha2B | 3H-Clonidine | Agonist | Human | 1,785 | 77 |
| Alpha2C | 3H-Clonidine | Agonist | Human | 1,123 | 77 |
| Beta1 | 125I-Pindolol | Partial Agonist | Rat | >10,000 | 77 |
| Beta2 | 125I-Pindolol | Partial Agonist | Rat | >10,000 | 77 |
| CB1 | 3H-CP-55940 | Agonist | Rat (brain) | >10,000 | 77 |
| M1 | 3H-QNB | Antagonist | Human | >10,000 | 77 |
| M2 | 3H-QNB | Antagonist | Human | >10,000 | 77 |
| M3 | 3H-QNB | Antagonist | Human | 1,851 | 77 |
| M4 | 3H-QNB | Antagonist | Human | 8,245 | 77 |
| M5 | 3H-QNB | Antagonist | Human | 6,339 | 77 |
| Nicotinic Alpha1Beta2 |
3H-Epibatidine | Agonist | Human | >10,000 | 77 |
| Nicotinic Alpha2Beta2 |
3H-Epibatidine | Agonist | Human | >10,000 | 77 |
| Nicotinic Alpha2Beta4 |
3H-Epibatidine | Agonist | Human | >10,000 | 77 |
| Nicotinic Alpha3Beta2 |
3H-Epibatidine | Agonist | Human | >10,000 | 77 |
| Nicotinic Alpha3Beta4 |
3H-Epibatidine | Agonist | Human | >10,000 | 77 |
| Nicotinic Alpha7 | 3H-Epibatidine | Agonist | Human | >10,000 | 77 |
| D1 | 3H-SCH23390 | Antagonist | Human | >10,000 | 77 |
| D1 | 3H-SCH23390 | Antagonist | Human | >13,600 | 62 |
| D2 | 3H-NMSP | Antagonist | Human | >10,000 | 77 |
| D2 | 3H-Spiperone | Antagonist | Human | 25,200 | 62 |
| D3 | 3H-NMSP | Antagonist | Human | >10,000 | 77 |
| D3 | 3H-Spiperone | Antagonist | Human | >17,700 | 62 |
| D4 | 3H-NMSP | Antagonist | Rat | >10,000 | 77 |
| D5 | 3H-SCH23390 | Antagonist | Human | >10,000 | 77 |
| GABA A | 3H-Muscimol | Agonist | Rat (forebrain) | >10,000 | 77 |
| GABA B | 3H-Baclofen | Agonist | Rat (forebrain) | >10,000 | 77 |
| NMDA | 3H-MK-801 | Antagonist | Rat (forebrain) | >10,000 | 77 |
| H1 | 3H-Pyrilamine | Antagonist | Human | 2,138 | 77 |
| H1 | 3H-Pyrilamine | Antagonist | Human | >14,400 | 62 |
| H2 | 3H-Pyrilamine | Antagonist | Human | >10,000 | 77 |
| Prostaglandin EP3 | 3H-PGE2 | Agonist | Human | >10,000 | 77 |
| Prostaglandin EP4 | 3H-PGE2 | Agonist | Human | >10,000 | 77 |
| NET | 3H-Nisoxetine | Inhibitor | Human | >10,000 | 77 |
| NET | 3H-Nisoxetine | Inhibitor | Human | 30,500 | 62 |
| DAT | 3H-GBR 12935 | Inhibitor | Human | >10,000 | 77 |
| DAT | 3H-WIN35,428 | Inhibitor | Human | 6,500 | 62 |
| SERT | 3H-Citalopram | Inhibitor | Human | >10,000 | 77 |
| SERT | 3H-Citalopram | Inhibitor | Human | 13,300 | 62 |
| TAAR1 | 3H-RO5166017 | Agonist | Rat | 370 | 62 |
| TAAR1 | 3H-RO5166017 | Agonist | Mouse | 2,400 | 62 |