Rediscovery of Ceruletide, a CCK Agonist, as an Analgesic Drug

Jan M Keppel Hesselink 1, 2 1Faculty of Health, University of Witten/Herdecke, Witten, Germany; 2Department Research and Development, Institute for Neuropathic Pain, Bosch en Duin, The NetherlandsCorrespondence: Jan M Keppel Hesselink Tel +31651700527Email jan@neuropathie.nuAbstract: Ceruletide (C...

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Main Author: Keppel Hesselink JM
Format: Article
Language:English
Published: Dove Medical Press 2020-01-01
Series:Journal of Pain Research
Subjects:
Online Access:https://www.dovepress.com/rediscovery-of-ceruletide-a-cck-agonist-as-an-analgesic-drug-peer-reviewed-article-JPR
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author Keppel Hesselink JM
author_facet Keppel Hesselink JM
author_sort Keppel Hesselink JM
collection DOAJ
description Jan M Keppel Hesselink 1, 2 1Faculty of Health, University of Witten/Herdecke, Witten, Germany; 2Department Research and Development, Institute for Neuropathic Pain, Bosch en Duin, The NetherlandsCorrespondence: Jan M Keppel Hesselink Tel +31651700527Email jan@neuropathie.nuAbstract: Ceruletide (CRL) is a decapeptide, originating from the skin of a tropical frog, and is many times more potent that cholecystokinin (CCK) in a number of assays. The compound was first isolated and characterized around 50 years ago, and its analgesic properties were subsequently identified. Since the 1980s it has been available in the clinic as a parenteral solution and is used as a diagnostic tool to characterize pancreas and gall bladder malfunctions. Its analgesic properties were evaluated in a number of indications: cancer pain, burns, colic pains and migraine. Preclinically, CRL reduces pain in low microgram dose range and promotes clear and long-lasting analgesic activity in nanograms when applied centrally. CCK is amongst the most widely expressed neuropeptides in the brain. CCK-induced analgesic effects in response to persistent and inflammatory pain have recently been associated with CCK2 receptor signaling. CRL, a potent CCK agonist, might be worthwhile to rediscover as a putative analgesic drug and could represent a potential analgesic intrathecal strategy to patients with cancer-related pain.Keywords: caerulein, neuropeptide, pain, cancer, Kambo
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spelling doaj.art-47153fd3f2f042b3aea56292aecdf6f92022-12-22T01:36:44ZengDove Medical PressJournal of Pain Research1178-70902020-01-01Volume 1312313051157Rediscovery of Ceruletide, a CCK Agonist, as an Analgesic DrugKeppel Hesselink JMJan M Keppel Hesselink 1, 2 1Faculty of Health, University of Witten/Herdecke, Witten, Germany; 2Department Research and Development, Institute for Neuropathic Pain, Bosch en Duin, The NetherlandsCorrespondence: Jan M Keppel Hesselink Tel +31651700527Email jan@neuropathie.nuAbstract: Ceruletide (CRL) is a decapeptide, originating from the skin of a tropical frog, and is many times more potent that cholecystokinin (CCK) in a number of assays. The compound was first isolated and characterized around 50 years ago, and its analgesic properties were subsequently identified. Since the 1980s it has been available in the clinic as a parenteral solution and is used as a diagnostic tool to characterize pancreas and gall bladder malfunctions. Its analgesic properties were evaluated in a number of indications: cancer pain, burns, colic pains and migraine. Preclinically, CRL reduces pain in low microgram dose range and promotes clear and long-lasting analgesic activity in nanograms when applied centrally. CCK is amongst the most widely expressed neuropeptides in the brain. CCK-induced analgesic effects in response to persistent and inflammatory pain have recently been associated with CCK2 receptor signaling. CRL, a potent CCK agonist, might be worthwhile to rediscover as a putative analgesic drug and could represent a potential analgesic intrathecal strategy to patients with cancer-related pain.Keywords: caerulein, neuropeptide, pain, cancer, Kambohttps://www.dovepress.com/rediscovery-of-ceruletide-a-cck-agonist-as-an-analgesic-drug-peer-reviewed-article-JPRcaerulinneuropeptidepaincancerkambo
spellingShingle Keppel Hesselink JM
Rediscovery of Ceruletide, a CCK Agonist, as an Analgesic Drug
Journal of Pain Research
caerulin
neuropeptide
pain
cancer
kambo
title Rediscovery of Ceruletide, a CCK Agonist, as an Analgesic Drug
title_full Rediscovery of Ceruletide, a CCK Agonist, as an Analgesic Drug
title_fullStr Rediscovery of Ceruletide, a CCK Agonist, as an Analgesic Drug
title_full_unstemmed Rediscovery of Ceruletide, a CCK Agonist, as an Analgesic Drug
title_short Rediscovery of Ceruletide, a CCK Agonist, as an Analgesic Drug
title_sort rediscovery of ceruletide a cck agonist as an analgesic drug
topic caerulin
neuropeptide
pain
cancer
kambo
url https://www.dovepress.com/rediscovery-of-ceruletide-a-cck-agonist-as-an-analgesic-drug-peer-reviewed-article-JPR
work_keys_str_mv AT keppelhesselinkjm rediscoveryofceruletideacckagonistasananalgesicdrug