| Identification | Back Directory | [Name]
3-Thiophenecarboxylic acid, 2-[(4-chlorobenzoyl)amino]-4-ethyl-5-methyl-, methyl ester | [CAS]
544450-68-2 | [Synonyms]
COR659
3-Thiophenecarboxylic acid, 2-[(4-chlorobenzoyl)amino]-4-ethyl-5-methyl-, methyl ester | [Molecular Formula]
C16H16ClNO3S | [MDL Number]
MFCD03379002 | [MOL File]
544450-68-2.mol | [Molecular Weight]
337.82 |
| Chemical Properties | Back Directory | [storage temp. ]
4°C, away from moisture and light | [solubility ]
DMSO: 33.33 mg/mL (98.66 mM) | [form ]
Solid | [color ]
Off-white to light yellow |
| Hazard Information | Back Directory | [Uses]
COR659 is a potent and effective GABAB positive allosteric modulator (PAM). COR659 suppresses alcohol and chocolate self-administration in rats[1]. | [Biological Activity]
COR659 is a potent positive allosteric modulator (PAM) of GABAB. It alleviates drug addiction to alcohol and chocolate in rats. | [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. | [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.
It 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 of lever-responses for alcohol averaged approximately 30, 55, and 70%, in com parison 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.
| | [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. DOI:10.1007/s00213-017-4644-3
[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;155:105544. DOI:10.1007/s00213-017-4644-3
[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. DOI:10.1016/j.alcohol.2018.05.007 |
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