[CAS NO. 544450-68-2] COR659
PRODUCTS SPECIFICATIONS [544450-68-2]
DESCRIPTION [544450-68-2]
Overview
| MDL | MFCD03379002 |
|---|---|
| Molecular Weight | 337.82 |
| Molecular Formula | C16H16ClNO3S |
| SMILES | O=C(C1=C(NC(C2=CC=C(Cl)C=C2)=O)SC(C)=C1CC)OC |
Summary
COR659 is a potent and effective GABA B positive allosteric modulator (PAM) . COR659 suppresses alcohol and chocolate self-administration in rats [1] .
In Vitro
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 [3] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
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
[1]
.
COR659 is able to suppress lever-responding for a sucrose solution in sP rats and a chocolate solution in Wistar rats
[2]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Male sP and Wistar rats [1] . |
| 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. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Solvent & Solubility
DMSO : 25 mg/mL ( 74.00 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.9602 mL | 14.8008 mL | 29.6016 mL |
| 5 mM | 0.5920 mL | 2.9602 mL | 5.9203 mL |
| 10 mM | 0.2960 mL | 1.4801 mL | 2.9602 mL |
References
- [1] Paola Maccioni, et al. Suppressing effect of COR659 on alcohol, sucrose, and chocolate self-administration in rats: involvement of the GABA B and cannabinoid CB 1 receptors. Psychopharmacology (Berl). 2017 Sep;234(17):2525-2543.
- [2] Francesca Ferlenghi, et al. The GABA B receptor positive allosteric modulator COR659: In vitro metabolism, in vivo pharmacokinetics in rats, synthesis and pharmacological characterization of metabolically protected derivatives. Eur J Pharm Sci. 2020 Dec 1
- [3] Paola Maccioni, et al. Anti-addictive properties of COR659 - Additional pharmacological evidence and comparison with a series of novel analogues. Alcohol. 2019 Mar;75:55-66.