Table 4.
Target | Concentration range (μM); (effect) | EC50/IC50 (μM) | Ki (μM) | Preparation or tissue | Assay type | Reference |
---|---|---|---|---|---|---|
ABCC1 | 0.08–50.00; (–) | 5.5 | ND | SF9/ human | ATPase/N-ethyl-maleimide-glutathione | [103] |
ABCG2 | 0.08–50.00; (–) | 7.3 | ND | ATPase/ sulfasalazine | [104] | |
Adenosine uptake | 10–3–102; (–) | 3.5 | ND | Striatal tissue synaptosome/rat | Dual-label counting [3H]-adenosine | [105] |
Adenosine uptake | 10–2–1; (–) | 0.12 | ND | EOC-20 microglia/ mouse | Scintillation counting/ [3H]-adenosine | [106] |
Anandamide uptake (AMT) | 5–50; (–)* | 22 | ND | RBL – 2H3 cells/rat | Scintillation counting/[14C]-anandamide | [19] |
1–25; (–) | 25.3 | ND | [71] | |||
Dopamine uptake | 0.5–100.0; (–)* | 16.2 | ND | Striatal tissue synaptosome/ rat | Dual-label counting/[3H]-dopamine | [105] |
0.005–10.000;(-)* | ND | ND | Hippocampus/corpus striatum/rat | [3H]-dopamine | ||
Glutamate uptake | 1–102; (–) | 43.8 | ND | Striatal tissue synaptosome/rat | Dual-label counting/[3H]-glutamate | |
Mg2+-ATPase | 1–103; (–) | ND | ND | Brain cortical vesicules/ rat | Phosphate release | [107] |
NA uptake | 0.005–10.000;(–)* | ND | ND | Hippocampus/corpus striatum/ rat | Method: Coyle and Snyder (1969)/ [3H]-NA | [108] |
Thymidine uptake | 10–2–1; (–) | 0.19 | ND | EOC-20 microglia/ mouse | Scintillation counting/ [3H]-thymidine | [106] |
Choline uptake | 0.24–240.00; (–) | 15.9 | ND | Hippocampus synaptosome/rat | Method: Whittaker et al. (1964) | [109] |
AMT = anandamide membrane transporter; Mg2+-ATPase = magnesium-activated adenosine triphosphatase; NA = noradrenaline; ND = not described; (+) = stimulation; (–) = inhibition
*Estimated from plots in cited paper