3-Thiophenecarboxylic acid, 2-[(4-chlorobenzoyl)amino]-4-ethyl-5-methyl-, methyl ester
- CAS No.
- 544450-68-2
- Chemical Name:
- 3-Thiophenecarboxylic acid, 2-[(4-chlorobenzoyl)amino]-4-ethyl-5-methyl-, methyl ester
- Synonyms
- COR659;COR659, 10 mM in DMSO;Methyl 2-(4-chlorobenzamido)-4-ethyl-5-methylthiophene-3-carboxylate;3-Thiophenecarboxylic acid, 2-[(4-chlorobenzoyl)amino]-4-ethyl-5-methyl-, methyl ester;COR 659,Gamma-aminobutyric acid Receptor,sucrose,inhibit,chocolate,γ-Aminobutyric acid Receptor,GABA Receptor,COR-659,Inhibitor,COR659,alcohol
- CBNumber:
- CB48090818
- Molecular Formula:
- C16H16ClNO3S
- Molecular Weight:
- 337.82
- MDL Number:
- MFCD03379002
- MOL File:
- 544450-68-2.mol
3-Thiophenecarboxylic acid, 2-[(4-chlorobenzoyl)amino]-4-ethyl-5-methyl-, methyl ester price
Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
---|---|---|---|---|---|---|---|
ChemScene | CS-0137045 | COR659 99.94% | 544450-68-2 | 5mg | $300 | 2021-12-16 | Buy |
ChemScene | CS-0137045 | COR659 99.94% | 544450-68-2 | 10mg | $500 | 2021-12-16 | Buy |
ChemScene | CS-0137045 | COR659 99.94% | 544450-68-2 | 25mg | $950 | 2021-12-16 | Buy |
ChemScene | CS-0137045 | COR659 99.94% | 544450-68-2 | 50mg | $1550 | 2021-12-16 | Buy |
ChemScene | CS-0137045 | COR659 99.94% | 544450-68-2 | 100mg | $2350 | 2021-12-16 | Buy |
3-Thiophenecarboxylic acid, 2-[(4-chlorobenzoyl)amino]-4-ethyl-5-methyl-, methyl ester Chemical Properties,Uses,Production
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
3-Thiophenecarboxylic acid, 2-[(4-chlorobenzoyl)amino]-4-ethyl-5-methyl-, methyl ester Preparation Products And Raw materials
Raw materials
Preparation Products
3-Thiophenecarboxylic acid, 2-[(4-chlorobenzoyl)amino]-4-ethyl-5-methyl-, methyl ester Suppliers
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TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 32268 | 58 |
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