Receptor selectivity profile of 1 μM CJ-023,423
The results are expressed as a percentage of inhibition of control specific binding (mean values; n = 2).
Receptor | Subtype Name | 1 μM CJ-023,423 | Reference Compound | IC50 |
|---|---|---|---|---|
| nM | ||||
| Adenosine | A1 (human) | — | 8-Cyclopentyl-1,3-dipropylxanthine | 7.7 |
| A2A (human) | 12 | 5′-N-Ethylcarboxamidoadenosine | 100 | |
| Adrenergic | α1 (nonselective) | — | Prazosin | 0.32 |
| α2 (nonselective) | — | Yohimbine | 59 | |
| β1 (human) | — | Atenolol | 1980 | |
| β2 (human) | — | ICI 118551 | 3.0 | |
| Dopamine | D1 (human) | — | SCH23390 | 0.86 |
| D2 (human) | — | (+)-Butaclamol | 26 | |
| D3 (human) | — | (+)-Butaclamol | 7.6 | |
| D4.4 (human) | — | Clozapine | 77 | |
| Histamine | H1, central | — | Pyrilamine | 1.2 |
| H2 | — | Cimetidine | 2310 | |
| Muscarinic | Nonselective | — | Atropine | 0.37 |
| Nicotinic | Neuronal (α-bungarotoxin-insensitive) | — | Nicotine | 12 |
| Muscle type | — | α-Bungarotoxin | 6.0 | |
| Opiate | Nonselective | — | Naloxone | 2.0 |
| Serotonin | Nonselective | — | Serotonin | 3.7 |
| Benzodiazepine | Central | — | Diazepam | 8.0 |
| Calcium channel | L-type, verapamil site | — | D600 | 17 |
| L-type, dihydropyridine site | — | Nitrendipine | 0.99 | |
| L-type, diltiazem site | — | Diltiazem | 37 | |
| N-type | — | ω-Conotoxin GVIA | 0.0054 | |
| GABA | Nonselective | — | GABA | 20 |
| Glutamate | α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid | — | l-Glutamate | 457 |
| Kainate | — | Kainic acid | 16 | |
| N-Methyl-d-aspartate | — | CGS19755 | 513 | |
| Glycine | Strychnine-insensitive | — | Glycine | 307 |
| Potassium channel | Voltage-dependent | — | α-Dendrotoxin | 1.2 |
| Ca2+-dependent | — | Apamin | 0.025 | |
| ATP-dependent | — | Glibenclamide | 2.1 | |
| Na+ channel | Site2 | — | Veratridine | 3690 |
| Cl- channel | Cl- ionophore | — | Picrotoxinin | 339 |
| Transporter | Norepinephrine (human) | 28 | Protriptyline | 11 |
| Dopamine (human) | — | GBR 12909 | 10 | |
| GABA | 20 | Nipecotic acid | 6600 | |
| Choline | — | Hemicholinium-3 | 11 | |
| 5-Hydroxytryptamine (human) | — | Imipramine | 5.0 | |
| Estradiol | Estrogen β (human) | — | 17-β-Estradiol | 52 |
| Thyroid hormone | — | T3 | 0.34 | |
| Glucocorticoid | Glucocorticoid (human) | — | Dexamethasone | 5.4 |
| Angiotensin II | AT1 (human) | 19 | Saralasin | 0.71 |
| AT2 (human) | — | Saralasin | 0.58 | |
| Vasopressin | V1α (human) | — | [d(CH2)51,Tyr (Me)2]-AVP | 1.9 |
| Leukotriene | LTB4 (human) (BLT) | 10 | LTB4 | 1.4 |
| LTD4 (human) | — | LTD4 | 7.0 | |
| Interleukin | Interleukin-6 (human) | — | Interleukin-6 | 0.085 |
| TNF-α | TNF-α (human) | — | TNF-α | 0.45 |
| Prostanoid | TP (human) | — | U44069 | 1060 |
| Platelet-activating factor | 39 | WEB2086 | 7.9 | |
| Neurokinin | NK1 (human) | — | [Sar9,Met(O2)11]-SP | 2.6 |
| NK2 (human) | — | [Nle10]-NKA(4-10) | 19 | |
|
| NK3 (human) | — | [MePhe7]-NKB | 6.5 |
—, inhibition of less than 10%.