Engineered endomorphin-2 gene: A novel therapy for improving morphine reinstatement in CPP model of rats by using deficient adenovirus as the vector

X Wang, Y Liu, X Wu, Y Zhang, RR Pan, W Yu… - … and biophysical research …, 2019 - Elsevier
… As an endogenous agonist for MOR, endomorphin-2 (EM2) is of high affinity and high … [22,23]
or to keep the release of EM2 by genetic engineering approach [24]. In our study, we …

An engineered endomorphin-2 gene for morphine withdrawal syndrome

F Wu, Y He, H Di, Y Sun, R Pan, W Yu, R Liu - PloS one, 2016 - journals.plos.org
… sequences of EM2 limit the possibility of engineering through transgene methods. In the
present study, we bypassed these obstacles by engineering a complex of gene for EM2 and a …

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 and endomorphin-2 are present in mammalian immune tissues. J … tolerance
to endomorphin-1 and endomorphin-2 given intraventricularly in the rat. Eur J Pharmacol …

Endomorphin-2 analogs with C-terminal esterification produce potent systemic antinociception with reduced tolerance and gastrointestinal side effects

C Wang, T Qiu, D Yang, B Yuan, F Han, L Li, N Gu - Neuropharmacology, 2017 - Elsevier
… In the present study, the pharmacological activities of C-terminal esterified endomorphin-2
(EM-2) analogs 1–3 were characterized by in vitro metabolic stability and octanol/buffer …

[PDF][PDF] A Brief Survey on Recent Endomorphin-1 and Endomorphin-2 Analogues

R De Marco - J Biochem Chem Sci, 2017 - researchgate.net
… In this review is reported a brief collection of recently published modified endomorphins,
for which the potentiality as painkiller was clearly demonstrated in vitro and in vivo. Selected …

MEL-N16: a series of novel endomorphin analogs with good analgesic activity and a favorable side effect profile

X Liu, L Zhao, Y Wang, J Zhou, D Wang… - ACS chemical …, 2017 - ACS Publications
Endomorphins are among the most active endogenous … a series of novel endomorphin
analogs with multiple site … the activity of synthesized endomorphin analogs toward opioid …

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
Previously, we have investigated three C-terminal esterified endomorphin-2 (EM-2) analogs
EM-2-Me, EM-2-Et and EM-2-Bu with methyl, ethyl and tert-butyl ester modifications, …

Novel endomorphin analogues CEMR‐1 and CEMR‐2 produce potent and long‐lasting antinociception with a favourable side effect profile at the spinal level

Y Zhang, S Wang, X Guo, X Liu, X Wang… - British Journal of …, 2024 - Wiley Online Library
Novel endomorphin analogs CEMR‐1 and CEMR‐2 produce potent and long‐lasting
antinociception with a favorable side effect p Page 1 This article has been accepted for publication …

Constraining endomorphin-1 by β, α-hybrid dipeptide/heterocycle scaffolds: identification of a novel κ-opioid receptor selective partial agonist

R De Marco, A Bedini, S Spampinato… - Journal of Medicinal …, 2018 - ACS Publications
… Herein we present the expedient synthesis of endomorphin-1 analogues containing
stereoisomeric β 2 -homo-Freidinger lactam-like scaffolds ([Amo 2 ]EM), and we discuss opioid …

Dilemma of addiction and respiratory depression in the treatment of pain: a prototypical endomorphin as a new approach

L Webster, WK Schmidt - Pain Medicine, 2020 - academic.oup.com
… the prototypical MOR-selective endomorphin-1 analog CYT-1010 and to compare what is
known about the clinical potential of MOR-selective endomorphins with traditional opioids for …