| biological activity | COR659 is a potent positive allosteric regulator (PAM) of GABAB. COR659 relieves drug addiction to alcohol and chocolate in rats. |
| in vitro study | COR659 apparently exerts its effects via a composite mechanism, including positive allosteric modulation of the GABA B receptor and an action at the cannabinoid CB1 receptor. |
| in vivo study | COR659 (0, 2.5, 5 and 10 mg/kg) treatment is completely ineffective on lever-responding (FR10) for regular food pellets in food-deprived Wistar rats. COR659 is able to suppress lever-responding for a sucrose solution in sP rats and a chocolate solution in Wistar rats. Animal Model: Male SP and Wistar rats. Dosage: 0, 2.5, 5 and 10 mg/kg. Administration: Intraperitoneally (administered 30 min before the start of the self-administration, reinstatement, and locomotor activity sessions.). Result: The magnitude of the reducing effect of the compound on number oflever-responses for alcohol averaged approximately 30, 55, and 70%, in comparison to the vehicle-treated rat group, in the rat groups treated with 2.5, 5, and 10 mg/kg COR659, respectively. The magnitude of the reducing effect of COR659 on number of lever-responses for alcohol averaged approximately 20, 40, and 80%, in comparison to the vehicletreated rat group, in the rat groups treated with 2.5, 5, and 10 mg/kg COR659, respectively. |
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Animal Model:
| Male sP and Wistar rats. |
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Dosage:
| 0, 2.5, 5 and 10 mg/kg. |
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Administration:
| Intraperitoneally (administered 30 min before the start of the self-administration, reinstatement, and locomotor activity sessions.). |
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Result:
| The magnitude of the reducing effect of the compound on number oflever-responses for alcohol averaged approximately 30, 55, and 70%, in comparison to the vehicle-treated rat group, in the rat groups treated with 2.5, 5, and 10 mg/kg COR659, respectively. The magnitude of the reducing effect of COR659 on number of lever-responses for alcohol averaged approximately 20, 40, and 80%, in comparison to the vehicletreated rat group, in the rat groups treated with 2.5, 5, and 10 mg/kg COR659, respectively. |
