Neuropharmacology, volume 166, pages 107678
BPR1M97, a dual mu opioid receptor/nociceptin-orphanin FQ peptide receptor agonist, produces potent antinociceptive effects with safer properties than morphine
Po-Kuan Chao
1
,
Hsiao-Wei Chang
1
,
Wan-Ting Chang
1
,
Teng-Kuang Yeh
1
,
Li Ou
1
,
Jian-Ying Chuang
2
,
John Tsu An Hsu
1
,
Pao-Luh Tao
3
,
Horace H. Hoh
4
,
Chuan Shih
1
,
Shau Hua Ueng
5, 6
,
Shiu-Hwa Yeh
5, 7
1
Institute of Biotechnology and Pharmaceutical Research, National Health Research Institutes, Miaoli County 35053, Taiwan
|
2
3
Center for Neuropsychiatric Research, National Heath Research Institutes, Zhunan, Miaoli County, 35053, Taiwan
|
4
5
Institute of Biotechnology and Pharmaceutical Research, National Health Research Institutes, Miaoli County, 35053, Taiwan
|
Publication type: Journal Article
Publication date: 2020-04-01
Journal:
Neuropharmacology
Quartile SCImago
Q1
Quartile WOS
Q1
Impact factor: 4.7
ISSN: 00283908, 18737064
Pharmacology
Cellular and Molecular Neuroscience
Abstract
There is unmet need to design an analgesic with fewer side effects for severe pain management. Although traditional opioids are the most effective painkillers, they are accompanied by severe adverse responses, such as respiratory depression, constipation symptoms, tolerance, withdrawal, and addiction. We indicated BPR1M97 as a dual mu opioid receptor (MOP)/nociceptin-orphanin FQ peptide (NOP) receptor full agonist and investigated the pharmacology of BPR1M97 in multiple animal models. In vitro studies on BPR1M97 were assessed using cyclic-adenosine monophosphate production, β-arrestin, internalization, and membrane potential assays. In vivo studies were characterized using the tail-flick, tail-clip, lung functional, heart functional, acetone drop, von Frey hair, charcoal meal, glass bead, locomotor activity, conditioned place preference (CPP) and naloxone precipitation tests. BPR1M97 elicited full agonist properties for all cell-based assays tested in MOP-expressing cells. However, it acted as a G protein-biased agonist for NOP. BPR1M97 initiated faster antinociceptive effects at 10 min after subcutaneous injection and elicited better analgesia in cancer-induced pain than morphine. Unlike morphine, BPR1M97 caused less respiratory, cardiovascular, and gastrointestinal dysfunction. In addition, BPR1M97 decreased global activity and induced less withdrawal jumping precipitated by naloxone. Thus, BPR1M97 could serve as a novel small molecule dual receptor agonist for antinociception with fewer side effects than morphine. This article is part of the Special Issue entitled ‘New Vistas in Opioid Pharmacology’.
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- We do not take into account publications without a DOI.
- Statistics recalculated only for publications connected to researchers, organizations and labs registered on the platform.
- Statistics recalculated weekly.
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Chao P. et al. BPR1M97, a dual mu opioid receptor/nociceptin-orphanin FQ peptide receptor agonist, produces potent antinociceptive effects with safer properties than morphine // Neuropharmacology. 2020. Vol. 166. p. 107678.
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Chao P., Chang H., Chang W., Yeh T., Ou L., Chuang J., Tsu An Hsu J., Tao P., Hoh H. H., Shih C., Ueng S. H., Yeh S. BPR1M97, a dual mu opioid receptor/nociceptin-orphanin FQ peptide receptor agonist, produces potent antinociceptive effects with safer properties than morphine // Neuropharmacology. 2020. Vol. 166. p. 107678.
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TY - JOUR
DO - 10.1016/j.neuropharm.2019.107678
UR - https://doi.org/10.1016/j.neuropharm.2019.107678
TI - BPR1M97, a dual mu opioid receptor/nociceptin-orphanin FQ peptide receptor agonist, produces potent antinociceptive effects with safer properties than morphine
T2 - Neuropharmacology
AU - Chao, Po-Kuan
AU - Chang, Hsiao-Wei
AU - Chang, Wan-Ting
AU - Yeh, Teng-Kuang
AU - Ou, Li
AU - Chuang, Jian-Ying
AU - Tsu An Hsu, John
AU - Tao, Pao-Luh
AU - Hoh, Horace H.
AU - Shih, Chuan
AU - Ueng, Shau Hua
AU - Yeh, Shiu-Hwa
PY - 2020
DA - 2020/04/01 00:00:00
PB - Elsevier
SP - 107678
VL - 166
SN - 0028-3908
SN - 1873-7064
ER -
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@article{2020_Chao,
author = {Po-Kuan Chao and Hsiao-Wei Chang and Wan-Ting Chang and Teng-Kuang Yeh and Li Ou and Jian-Ying Chuang and John Tsu An Hsu and Pao-Luh Tao and Horace H. Hoh and Chuan Shih and Shau Hua Ueng and Shiu-Hwa Yeh},
title = {BPR1M97, a dual mu opioid receptor/nociceptin-orphanin FQ peptide receptor agonist, produces potent antinociceptive effects with safer properties than morphine},
journal = {Neuropharmacology},
year = {2020},
volume = {166},
publisher = {Elsevier},
month = {apr},
url = {https://doi.org/10.1016/j.neuropharm.2019.107678},
pages = {107678},
doi = {10.1016/j.neuropharm.2019.107678}
}