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LY-2940094 is a potent, selective and orally available antagonist of nociceptin receptor (NOP receptor) with Ki of 0.105 nM and Kb of 0.166 nM. LY2940094 (3, 10, or 30 mg/kg; 2-3 mL/kg; orally daily; for 4 days) dose-dependently reduces homecage ethanol self-administration in Indiana Alcohol-Preferring (P) and Marchigian Sardinian Alcohol-Preferring (msP) rats, without affecting food/water intake or locomotor activity. LY-2940094 reduces ethanol self-administration in animal models. Furthermore, LY2940094 blocked ethanol-stimulated dopamine release in response to ethanol challenge (1.1 g/kg, IP).
| Cell Experiment | |
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| Cell lines | |
| Preparation method | |
| Concentrations | |
| Incubation time | |
| Animal Experiment | |
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| Animal models | Female Alcohol-Preferring (P) rats (250-320 g); Male Marchigian Sardinian Alcohol-Preferring (msP) rats (400-450 g) |
| Formulation | dissolved in 20% Captisol in 25 mM phosphate buffer (pH 3, adjusted for L-tartaric acid salt weight) |
| Dosages | 3, 10, or 30 mg/kg; 2-3 mL/kg |
| Administration | 4 daily orally administered |
| Molecular Weight | 480.96 |
| Formula | C22H23ClF2N4O2S |
| CAS Number | 1307245-86-8 |
| Solubility (25°C) | DMSO 40 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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