Binding Site | % Inhibition4-a | Binding Site | % Inhibition4-a |
---|---|---|---|
Adenosine A1 | −2.8 | Imidazoline (I2) | 63.8 |
Adenosine A2 | −41.6 | K+ ATP channel | |
Adrenergic | Central | −0.9 | |
α1 (nonselective) | 32.5 | Peripheral | −60.9 |
α2 (nonselective) | 75.1 | Cholinergic | |
β1 | −2.1 | M1 | 11.4 |
β2 | −17.9 | M2 | −7.6 |
Benzodiazepine | M3 | 11.4 | |
Central | −20.0 | Nicotine(CNS) | −3.7 |
Peripheral | −14.5 | Na+ channel | 28.1 |
Ca2+ channel (L) | 0.3 | Opioid | |
Dopaminergic | μ | −6.5 | |
D1 | −13.0 | κ | −13.1 |
D2 | 14.5 | δ | −9.2 |
Endothelin | Serotonergic | ||
ETA | −2.2 | 5-HT1 (nonselective) | 5.4 |
ETB | −6.7 | 5-HT1A | 51.3 |
Glutamate | 1.8 | 5-HT1B | −4.0 |
NMDA | −36.2 | 5-HT1D | 23.4 |
AMPA | −25.1 | 5-HT2A | 0.0 |
Kainate | −38.2 | 5-HT2C | 5.7 |
γ-Aminobutyric acid | −32.8 | 5-HT3 | 6.4 |
↵4-a Total and nonspecific binding as well as the percentage of inhibition by GT-2227 (1 μM) for the given receptor/ion channel were determined. Values represent the mean of triplicate determinations in a single experiment.