A novel orvinol analog, BU08028, as a safe opioid analgesic without abuse liability in primates

H Ding, PW Czoty, N Kiguchi… - Proceedings of the …, 2016 - National Acad Sciences
Despite the critical need, no previous research has substantiated safe opioid analgesics
without abuse liability in primates. Recent advances in medicinal chemistry have led to the …

A bifunctional nociceptin and mu opioid receptor agonist is analgesic without opioid side effects in nonhuman primates

H Ding, N Kiguchi, D Yasuda, PR Daga… - Science translational …, 2018 - science.org
Misuse of prescription opioids, opioid addiction, and overdose underscore the urgent need
for developing addiction-free effective medications for treating severe pain. Mu opioid …

The therapeutic potential of nociceptin/orphanin FQ receptor agonists as analgesics without abuse liability

AP Lin, MC Ko - ACS chemical neuroscience, 2013 - ACS Publications
Although mu opioid (MOP) receptor agonists are the most commonly used analgesics for the
treatment of moderate to severe pain in the clinic, the side effects of MOP agonists such as …

The first universal opioid ligand,(2S)-2-[(5R, 6R, 7R, 14S)-N-cyclopropylmethyl-4, 5-epoxy-6, 14-ethano-3-hydroxy-6-methoxymorphinan-7-yl]-3, 3-dimethylpentan-2 …

TV Khroyan, WE Polgar, G Cami-Kobeci… - … of Pharmacology and …, 2011 - ASPET
Certain behavioral features of buprenorphine, including a bell-shaped curve for
antinociception and attenuation of alcohol consumption, are thought to be mediated by …

[HTML][HTML] BU10038 as a safe opioid analgesic with fewer side-effects after systemic and intrathecal administration in primates

N Kiguchi, H Ding, G Cami-Kobeci… - British journal of …, 2019 - Elsevier
Background The marked increase in mis-use of prescription opioids has greatly affected our
society. One potential solution is to develop improved analgesics which have agonist action …

Roles of μ-opioid receptors and nociceptin/orphanin FQ peptide receptors in buprenorphine-induced physiological responses in primates

CM Cremeans, E Gruley, DJ Kyle, MC Ko - Journal of Pharmacology and …, 2012 - ASPET
Buprenorphine is known as a μ-opioid peptide (MOP) receptor agonist, but its
antinociception is compromised by the activation of nociceptin/orphanin FQ peptide (NOP) …

C7β-methyl analogues of the orvinols: the discovery of kappa opioid antagonists with nociceptin/orphanin FQ peptide (NOP) receptor partial agonism and low, or zero …

JP Cueva, C Roche, M Ostovar, V Kumar… - Journal of medicinal …, 2015 - ACS Publications
Buprenorphine is a successful analgesic and treatment for opioid abuse, with both activities
relying on its partial agonist activity at mu opioid receptors. However, there is substantial …

BU08073 a buprenorphine analogue with partial agonist activity at μ‐receptors in vitro but long‐lasting opioid antagonist activity in vivo in mice

TV Khroyan, J Wu, WE Polgar… - British journal of …, 2015 - Wiley Online Library
Background and Purpose Buprenorphine is a potent analgesic with high affinity at μ, δ and κ
and moderate affinity at nociceptin opioid (NOP) receptors. Nevertheless, NOP receptor …

Therapeutic potentials of NOP and MOP receptor coactivation for the treatment of pain and opioid abuse

N Kiguchi, H Ding, MC Ko - Journal of neuroscience research, 2022 - Wiley Online Library
Following the identification of the nociceptin/orphanin FQ (N/OFQ) peptide (NOP) as an
endogenous ligand for the NOP receptor, ample evidence has revealed unique functional …

Translational value of non-human primates in opioid research

H Ding, MC Ko - Experimental neurology, 2021 - Elsevier
Preclinical opioid research using animal models not only provides mechanistic insights into
the modulation of opioid analgesia and its associated side effects, but also validates drug …