Receptor | Ligand | % Inhibition |
---|---|---|
Angiotensin AT1 | [3H]Losartan | −11 |
Bradykinin B2 | [3H]Bradykinin | −8 |
Cholecystokinin A | [3H]L-364,718 | −3 |
Cholecystokinin B | [3H]CCK-8 | −18 |
Dopamine D3 | [3H]Spiperone | −6 |
Dopamine D2,4 | [3H]Spiperone | 13 |
Galanin | [125I]Galanin | −16 |
Histamine H3 | [3H]NAMH | 15 |
Kainate | [3H]Kainate | 9 |
Leukotriene B4 | [3H]LTB4 | 21 |
Muscarinic M1 | [3H]Pirenzipine | −1 |
Muscarinic M2 | [3H]NMS | −13 |
Muscarinic M4 | [3H]NMS | −4 |
Neurokinin NK1 | [3H]Substance P | 11 |
Neuropeptide Y2 | [3H]NPY | −16 |
Nicotinic (CNS) | [3H]Cytisine | 5 |
N-Methyl-d-aspartic acid | [3H]CGS-19755 | 22 |
Phencyclidine | [3H]TCP | −17 |
Platelet-activating factor | [3H]PAF | 28 |
Serotonin 5-HT1A | [3H]8-OH-DPAT | −11 |
Serotonin 5-HT3 | [3H]GR-65630 | 0 |
Sigma ς1 | [3H]Pentazocine | 12 |
Sodium channel-2 | [3H]Batrachotoxinin | 8 |
Thromboxane A2 | [3H]SQ-29,548 | −13 |
Thyrotropin-releasing hormone | [3H](Me)TRH | 20 |
Vasoactive intestinal polypeptide | [125I]VIP | 8 |
Enzyme | Source | % Inhibition |
Calcineurin | Rat brain | −4 |
Calpain | Human erythrocyte | 18 |
EGF tyrosine kinase | Human recombinant | −15 |
Nitric oxide synthase (constitutive) | Rat cerebellum | 2 |
Nitric oxide synthase (inducible) | RAW 264.7 cells | 5 |
Protein kinase C α2-a | Rat brain | −4 |
Protein kinase C β2-a | Rat brain | 7 |
↵2-a Concentration of T-0201 was 50 μM.