The Cholecystokinin Type 2 Receptor, a Pharmacological Target for Pain Management

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...

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Autores principales:	Amandine Bernard, Aurore Danigo, Sylvie Bourthoumieu, Mohamad Mroué, Alexis Desmoulière, Franck Sturtz, Amandine Rovini, Claire Demiot
Formato:	article
Lenguaje:	EN
Publicado:	MDPI AG 2021
Materias:	cholecystokinin type 2 receptor pain management antagonist rodent model clinical trial Medicine R Pharmacy and materia medica RS1-441
Acceso en línea:	https://doaj.org/article/f33ce5bb1927427ab60341e936ffe901
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spelling	oai:doaj.org-article:f33ce5bb1927427ab60341e936ffe9012021-11-25T18:40:01ZThe Cholecystokinin Type 2 Receptor, a Pharmacological Target for Pain Management10.3390/ph141111851424-8247https://doaj.org/article/f33ce5bb1927427ab60341e936ffe9012021-11-01T00:00:00Zhttps://www.mdpi.com/1424-8247/14/11/1185https://doaj.org/toc/1424-8247Over 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 discordances of results between preclinical and clinical studies suggest reconsidering our knowledge about the molecular basis of the pharmacology and functioning of CCK2R. This review focuses on the cellular localization of CCK2R specifically in the sensory nervous system and discusses in further detail the molecular mechanisms and signal transduction pathways involved in controlling pain perception. We then provide a comprehensive overview of the most successful compounds targeting CCK2R and report recent advances in pharmacological strategies used to achieve CCK2R modulation. We purposely distinguish between CCK2R benefits obtained in preclinical models and outcomes in clinical trials with different pain etiologies. Lastly, we emphasize the biological and clinical relevance of CCK2R as a promising target for the development of new treatments for pain management.Amandine BernardAurore DanigoSylvie BourthoumieuMohamad MrouéAlexis DesmoulièreFranck SturtzAmandine RoviniClaire DemiotMDPI AGarticlecholecystokinin type 2 receptorpain managementantagonistrodent modelclinical trialMedicineRPharmacy and materia medicaRS1-441ENPharmaceuticals, Vol 14, Iss 1185, p 1185 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	cholecystokinin type 2 receptor pain management antagonist rodent model clinical trial Medicine R Pharmacy and materia medica RS1-441
spellingShingle	cholecystokinin type 2 receptor pain management antagonist rodent model clinical trial Medicine R Pharmacy and materia medica RS1-441 Amandine Bernard Aurore Danigo Sylvie Bourthoumieu Mohamad Mroué Alexis Desmoulière Franck Sturtz Amandine Rovini Claire Demiot The Cholecystokinin Type 2 Receptor, a Pharmacological Target for Pain Management
description	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 discordances of results between preclinical and clinical studies suggest reconsidering our knowledge about the molecular basis of the pharmacology and functioning of CCK2R. This review focuses on the cellular localization of CCK2R specifically in the sensory nervous system and discusses in further detail the molecular mechanisms and signal transduction pathways involved in controlling pain perception. We then provide a comprehensive overview of the most successful compounds targeting CCK2R and report recent advances in pharmacological strategies used to achieve CCK2R modulation. We purposely distinguish between CCK2R benefits obtained in preclinical models and outcomes in clinical trials with different pain etiologies. Lastly, we emphasize the biological and clinical relevance of CCK2R as a promising target for the development of new treatments for pain management.
format	article
author	Amandine Bernard Aurore Danigo Sylvie Bourthoumieu Mohamad Mroué Alexis Desmoulière Franck Sturtz Amandine Rovini Claire Demiot
author_facet	Amandine Bernard Aurore Danigo Sylvie Bourthoumieu Mohamad Mroué Alexis Desmoulière Franck Sturtz Amandine Rovini Claire Demiot
author_sort	Amandine Bernard
title	The Cholecystokinin Type 2 Receptor, a Pharmacological Target for Pain Management
title_short	The Cholecystokinin Type 2 Receptor, a Pharmacological Target for Pain Management
title_full	The Cholecystokinin Type 2 Receptor, a Pharmacological Target for Pain Management
title_fullStr	The Cholecystokinin Type 2 Receptor, a Pharmacological Target for Pain Management
title_full_unstemmed	The Cholecystokinin Type 2 Receptor, a Pharmacological Target for Pain Management
title_sort	cholecystokinin type 2 receptor, a pharmacological target for pain management
publisher	MDPI AG
publishDate	2021
url	https://doaj.org/article/f33ce5bb1927427ab60341e936ffe901
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The Cholecystokinin Type 2 Receptor, a Pharmacological Target for Pain Management

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