High-throughput screening revealed compound 1 as a potent antagonist of the CCK(1) receptor. Here, we disclose the synthesis of combinatorial libraries by solid-phase synthesis on Kenner 'safety catch' resin. Additive QSAR models were used to determine a lack of consistent additive SAR within the matrix.
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| http://dx.doi.org/10.1016/j.bmcl.2005.09.041 | DOI Listing |
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Article Synopsis
- * A study on mice exposed to chronic stress revealed that they exhibited anxiety, depression-like behaviors, and long-lasting widespread pain across multiple body regions.
- * The research identified an increase in cholecystokinin (CCK) receptor expression in the spinal cord after stress, suggesting that targeting these receptors could lead to new treatments for chronic primary pain.
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Eur J Pharm Sci
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School of Chemistry & Materials Science, Jiangsu Normal University, Xuzhou 221116, PR China.
The combined use of gastrointestinal hormones for treating metabolic diseases is gaining increasing attention. The potential of developing novel dual agonists targeting both cholecystokinin 1 (CCK-1) receptor and glucagon-like peptide 1 (GLP-1) receptor to improve the treatment of type 2 diabetes and obesity have not been fully explored. In this investigation, we reported a series of novel GLP-1/CCK-1 receptor co-agonists constructed by linking the C-terminus of a GLP-1 receptor agonist (bullfrog GLP-1) to the N-terminus of a CCK-1 receptor selective agonist NN9056.
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Greater Los Angeles Veterans Affairs Healthcare System, B114, R217, West LA VAMC, 11301 Wilshire Blvd., Los Angeles, CA, 90073, USA.
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Methods: Male mice were fed for 2 h (re-feeding) following a 22-h fast. Indomethacin (IND; 10 mg/kg, s.
Cholecystokinin (CCK): a neuromodulator with therapeutic potential in Alzheimer's and Parkinson's disease.
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