High throughput screening revealed compound 1 as a potent antagonist of the CCK(1) receptor. Evaluation of the CCK(1) SAR in a series of these diarylpyrazole antagonists was conducted in a matrix synthesis format revealing additive (Free-Wilson) and non-additive SAR. This use of additive QSAR modeling in conjunction with combinatorial libraries represents a unique approach to the evaluation of SAR interactions between the variables of any combinatorial matrix.
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Corrigendum to "Spinal CCK1 Receptors Contribute to Somatic Pain Hypersensitivity Induced by Malocclusion Via a Reciprocal Neuron-Glial Signaling Cascade" [J Pain 23 (2022) 1629-1645].
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Key Laboratory of Shaanxi Province for Craniofacial Precision Medicine Research, Research Center of Stomatology, College of Stomatology, Xi'an Jiaotong University, Xi'an, Shaanxi, China.
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Key Laboratory of Shaanxi Province for Craniofacial Precision Medicine Research, Xi'an Jiaotong University College of Stomatology, 98 West 5th Road, Xi'an, Shaanxi, 710004, China; Department of Neural and Pain Sciences, School of Dentistry, The UM Center to Advance Chronic Pain Research, University of Maryland Baltimore, 650 West Baltimore Street, Baltimore, MD, 21201, USA. Electronic address:
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
August 2024
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.
View Article and Find Full Text PDFCholecystokinin-Induced Duodenogastric Bile Reflux Increases the Severity of Indomethacin-Induced Gastric Antral Ulcers in Re-fed Mice.
Dig Dis Sci
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Greater Los Angeles Veterans Affairs Healthcare System, B114, R217, West LA VAMC, 11301 Wilshire Blvd., Los Angeles, CA, 90073, USA.
Background/aims: We examined the involvement of cholecystokinin (CCK) in the exacerbation of indomethacin (IND)-induced gastric antral ulcers by gastroparesis caused by atropine or dopamine in mice.
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.
Front Neuroendocrinol
April 2024
Second associated Hospital, Neurology Department, Shanxi Medical University, Taiyuan, Shanxi, China; Henan Academy of Innovations in Medical Science, Neurodegeneration research group, Xinzhen, Henan province, China.
Cholecystokinin (CCK) is a neuropeptide modulating digestion, glucose levels, neurotransmitters and memory. Recent studies suggest that CCK exhibits neuroprotective effects in Alzheimer's disease (AD) and Parkinson's disease (PD). Thus, we review the physiological function and therapeutic potential of CCK.
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