Table 5.
Esmethadone affinities for NMDARs and additional binding sites
| Target | Concentration | % Inhibition | Species |
|---|---|---|---|
| Calcium channel L-type, benzothiazepine | 10 µM | 81 | Rat |
| Calcium channel L-type, phenylalkylamine | 10 µM | 81 | Rat |
| Glutamate, NMDA, phencyclidine | 10 µM | 73 | Rat |
| Histamine H1 | 10 µM | 72 | Human |
| Muscarinic M5 | 10 µM | 72 | Human |
| Muscarinic, oxotremorine-M | 10 µM | 52 | Rat |
| µ-Opioid receptor (PO3, MOP) | 10 µM | 90 | Human |
| Serotonin (5-hydroxytryptamine) 5-HT2C | 10 µM | 89 | Human |
| Serotonin (5-hydroxytryptamine) 5-HT5A | 10 µM | 70 | Human |
| Serotonin (5-hydroxytryptamine) 5-HT7 | 10 µM | 66 | Human |
| Sigma σ1 | 10 µM | 85 | Human |
| Sodium channel, site 2 | 10 µM | 69 | Rat |
| Serotonin transporter (5-hydroxytryptamine) | 10 µM | 73 | Human (SERT) |
The activity of esmethadone was determined in radioligand binding assays through Eurofins Discovery Services (Relmada data on file). Results are presented as the percent inhibition of specific binding activity. Values listed above met criteria for significance (≥ 50% inhibition or stimulation)