Endogenous opiates and behavior: 2021

RJ Bodnar - Peptides, 2023 - Elsevier
This paper is the forty-fourth consecutive installment of the annual anthological review of
research concerning the endogenous opioid system, summarizing articles published during …

[HTML][HTML] IUPHAR review: Recent progress in the development of Mu opioid receptor modulators to treat opioid use disorders

PP Pagare, R Flammia, Y Zhang - Pharmacological Research, 2024 - Elsevier
Abstract Opioid Use Disorder (OUD) can be described as intense preoccupation with using
or obtaining opioids despite the negative consequences associated with their use. As the …

Characterization of a Potential KOR/DOR Dual Agonist with No Apparent Abuse Liability via a Complementary Structure–Activity Relationship Study on Nalfurafine …

M Li, DL Stevens, M Arriaga… - ACS chemical …, 2022 - ACS Publications
Discovery of analgesics void of abuse liability is critical to battle the opioid crisis in the
United States. Among many strategies to achieve this goal, targeting more than one opioid …

Blocking potential metabolic sites on NAT to improve its safety profile while retaining the pharmacological profile

R Flammia, B Huang, PP Pagare, CMS Onge… - Bioorganic …, 2024 - Elsevier
The number of opioid-related overdose deaths and individuals that have suffered from
opioid use disorders have significantly increased over the last 30 years. FDA approved …

NCP, a dual kappa and mu opioid receptor agonist, is a potent analgesic against inflammatory pain without reinforcing or aversive properties

P Huang, CK Ho, D Cao, S Inan, SM Rawls, M Li… - … of Pharmacology and …, 2024 - ASPET
While agonists of μ (MOR) and κ (KOR) opioid receptors have analgesic effects, they
produce euphoria and dysphoria, respectively. Other side effects include respiratory …

[HTML][HTML] Conformational Plasticity Enhances the Brain Penetration of a Metabolically Stable, Dual-Functional Opioid-Peptide CycloAnt

Y Li, WE Cotham, A Eliasof, K Bland, M Walla… - International Journal of …, 2024 - mdpi.com
CycloAnt is an opioid peptide that produces potent and efficacious antinociception with
significantly reduced side effects upon systemic administration in mice. To verify its CNS …

A straightforward trifluoromethylation at the C6 position of morphinane alkaloids, their modification and evaluation of inhibition of the SARS-CoV-2 main protease

AO Finke, VI Krasnov, TV Rybalova… - Journal of Fluorine …, 2023 - Elsevier
A catalytic trifluoromethylation of stereoisomeric 6-ketomorphinans using Ruppert–Prakash
reagent and tetrabutylammonium fluoride (TBAF) was studied. 14β-Hydroxycodeinone, 4-O …

Structural Characterization of KOR Inactive and active states for 3D pharmacology and drug discovery

SA Zaidi, V Katritch - The Kappa Opioid Receptor, 2021 - Springer
The structure of the human kappa opioid receptor (KOR) in complex with the long-acting
antagonist JDTic was solved crystallographically in 2012 and, along with structures of other …