2021
DOI: 10.3390/ph14111185
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The Cholecystokinin Type 2 Receptor, a Pharmacological Target for Pain Management

Abstract: Over the past decades, accumulating evidence has demonstrated a pivotal role of cholecystokinin type 2 receptor (CCK2R) in pain modulation. The established role of CCK2R activation in directly facilitating nociception has led to the development of several CCK2R antagonists, which have been shown to successfully alleviate pain in several rodent models of pain. However, the outcomes of clinical trials are more modest since they have not demonstrated the expected biological effect obtained in animals. Such discor… Show more

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Cited by 11 publications
(9 citation statements)
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“…Among them, GRIA1 and GRIA4 , which encode subunits of AMPA-type glutamate ionotropic receptors, provided genetic evidence of a link between RLS and glutamate receptor function. Another interesting candidate is CCKBR , which encodes the predominant cholecystokinin receptor in the brain 14 , 15 . Our prioritization algorithm also listed SLC40A1 , which had already been identified in the discovery stage of a previous study but had failed to replicate 4 .…”
Section: Resultsmentioning
confidence: 99%
“…Among them, GRIA1 and GRIA4 , which encode subunits of AMPA-type glutamate ionotropic receptors, provided genetic evidence of a link between RLS and glutamate receptor function. Another interesting candidate is CCKBR , which encodes the predominant cholecystokinin receptor in the brain 14 , 15 . Our prioritization algorithm also listed SLC40A1 , which had already been identified in the discovery stage of a previous study but had failed to replicate 4 .…”
Section: Resultsmentioning
confidence: 99%
“…The phospholipase C (PLC)/inositol triphosphate (IP3) pathway can mediate neuronal apoptosis in brain tissue and play a neuroprotective role. PLCβ can be activated by G protein-coupled receptors, hydrolyzing phosphatidylinositol-4,5-bisphosphate (PIP2) into diacylglycerol (DAG) and inositol trisphosphate (IP3) [61]. DAG and IP3 are important second messengers that can activate protein kinase C, release calcium ions, and regulate cell apoptosis, as well as modulate the physiological effects of neuronal growth, differentiation, and survival [62].…”
Section: Discussionmentioning
confidence: 99%
“…Recently, heterodimerization of opioid and CCK receptors subsequent to CCK octapeptide binding was demonstrated. This interaction was identified as the basis of the inhibition of opioid signal transduction and the antagonism of morphine analgesia ( Yang et al, 2018 ; Bernard et al, 2021 ). CCK antagonists enhance the analgesic efficacy of endogenous opioids in animal models of pain ( Inoue, 2017 ).…”
Section: Pain: a Simplified Modelmentioning
confidence: 99%