PNU-120596 is a potent and selective positive allosteric α7 neuronal nicotinic acetylcholine receptors modulator with an EC50 of 0.2 μM. PNU-120596 has no detectable effect on α4β2, α3β4 and α9α10 receptors. Discovered in a high-throughput screen, PNU-120596 enhanced agonist-evoked calcium flux mediated by an engineered variant of the human α7 nAChR. Electrophysiology studies demonstrated that PNU-120596 increased peak agonist-evoked currents mediated by wild-type receptors and also proved a pronounced prolongation of the triggered response in the continued presence of agonist.
| Cell Experiment | |
|---|---|
| Cell lines | SH-SY5Y-α7 cells |
| Preparation method | SH-SY5Y-α7 cells are plated on 96-well plates at a density of 15,000 cells per well (100 μL of 1.5 × 105 cells per mL) in complete growth medium and placed into a 37 °C incubator for 20 to 24 hours. Complete growth medium then is replaced with experimental medium alone ("PNU-120596 free") or containing appropriate concentrations of PNU-120596 and returns to the 37 °C ncubator for 20 to 24 hours. The medium is then replaced with fresh experimental medium and 20 μL per well MTS solution and returned to the 37 °C incubator for 3 hours, after which the plate is read on a microplate spectrophotometer at an absorbance of 490 nm. For all data analysis, data are normalized to untreated compound-free wells (100% cell viability) and a background absorbance taken from wells containing experimental medium and MTS solution. |
| Concentrations | 3-10 μM |
| Incubation time | 24 hours |
| Animal Experiment | |
|---|---|
| Animal models | male Sprague Dawley rats (weighing 250–300 g) |
| Formulation | PNU-120596 is dissolved in 5% DMSO and 5% Solutol in PBS. |
| Dosages | 1 mg/kg |
| Administration | PNU-120596 is intravenously administrated 5 minutes before auditory gating measurements. |
| Molecular Weight | 311.72 |
| Formula | C13H14ClN3O4 |
| CAS Number | 501925-31-1 |
| Form | Solid |
| Solubility (25°C) | DMSO 60 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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