Endomorphins: promising endogenous opioid peptides for the development of novel analgesics

ZH Gu, B Wang, ZZ Kou, Y Bai, T Chen, YL Dong, H Li… - Neurosignals, 2018 - karger.com
Endomorphin-1 (EM1) and endomorphin-2 (EM2) are two … underlying the analgesic effects
of the EMs in the spinal level can be … agonists endomorphins 1 and 2 have novel hypotensive …

Antiallodynic effects of endomorphin-1 and endomorphin-2 in the spared nerve injury model of neuropathic pain in mice

C Wang, D Yang, B Yuan, T Qiu - Anesthesia & Analgesia, 2017 - journals.lww.com
… In addition, the antiallodynic activities of peripheral … and antibodies against endogenous
opioid peptides were … μ 2 -opioid receptor subtypes are localized in the spinal cord …

Strategies to improve bioavailability and in vivo efficacy of the endogenous opioid peptides endomorphin-1 and endomorphin-2

R De Marco, A Janecka - Current Topics in Medicinal …, 2016 - ingentaconnect.com
… their agonist activities and opioid receptor specificities [51]. … quinolyl, cyclohexyl, and 2adamantyl
exhibited MOP receptor … were capable of intensifying opioid-mediated analgesia [90]. …

Exploiting endogenous opioids: Lessons learned from endomorphin 2 in the female rat

AR Gintzler, NJ Liu, EM Storman, MW Wessendorf - Peptides, 2019 - Elsevier
… of endogenous mechanism that suppress and facilitate spinalanalgesic effects of some
endogenous opioid peptides and the … to MOR, spinal dynorphin and KOR activities are also …

Innovative opioid peptides and biased agonism: novel avenues for more effective and safer analgesics to treat chronic pain

A Bedini, S Spampinato - Current Medicinal Chemistry, 2018 - ingentaconnect.com
… advantages and drawbacks of using endomorphin-1 (23) or … Endomorphin-1 (EM-1) and
-2 (EM-2) are endogenous, MOR… and at spinal levels [65], and displays an analgesic potency …

Contribution of the μ opioid receptor and enkephalin to the antinociceptive actions of endomorphin-1 analogs with unnatural amino acid modifications in the spinal …

J Zhou, L Zhao, S Wei, Y Wang, X Zhang, M Ma… - Peptides, 2021 - Elsevier
… release of endogenous opioid peptides. … analgesia compared to the parent peptide
endomorphin-1. Multiple antagonists and antibodies were used to explore the mechanisms of action

Novel endomorphin analogs are more potent and longer-lasting analgesics in neuropathic, inflammatory, postoperative, and visceral pain relative to morphine

AK Feehan, J Morgenweck, X Zhang… - The Journal of …, 2017 - Elsevier
… potency and longer duration of action relative to morphine. … that are based on the structures
of endogenous EM-1 and EM-… of pain state and test method, and 2) that morphine, but not …

Endomorphin-2 analogs with C-terminal esterification display potent antinociceptive effects in the formalin pain test in mice

S Wang, Y Zhang, X Liu, X Guo, X Wang, F Han… - Peptides, 2024 - Elsevier
… In 1997, two neuropeptide ligands named endomorphin-1 (EM… potent antinociceptive activities
in acute pain at the spinal and … the involvement of release of endogenous opioid peptides. …

Structure-constrained endomorphin analogs display differential antinociceptive mechanisms in mice after spinal administration

Y Wang, J Zhou, X Liu, L Zhao, Z Wang, X Zhang… - Peptides, 2017 - Elsevier
… In the present study, we further examined their spinal analgesia … antibodies against
endogenous opioid peptides were used to … Analogs 3 and 4 were less potent than analogs 1 and 2

The spinal anti-allodynic effects of endomorphin analogs with C-terminal hydrazide modification in neuropathic pain model

Y Zhang, W Yang, X Wang, M Wang, Y Zhang, N Gu… - Peptides, 2020 - Elsevier
… that intrathecal (it) administration of endomorphin-1 (EM-1), … and restored the antinociception
at 1.5 and 2 h. Nevertheless, EM… Opioid peptides are expected as effective analgesics in the …