Biphalin, a synthetic opioid octapeptide with a palindromic sequence has high analgesic activity. Biphalin displays a strong affinity for μ and δ-opioid receptors, and a significant to κ-receptor. The paper reports the synthesis of novel analogs of biphalin containing β(3)-homo-amino acid residues at the 4,4' positions and a hydrazine or 1,2-phenylenediamine linker. The potency and selectivity of the peptides were evaluated by a competitive receptor-binding assay in rat brain homogenate using [(3)H]DAMGO (a μ ligand) and [(3)H]DELT (a δ ligand). Analogs with β(3)-h-p-NO2Phe in positions 4 and 4' are the most active compounds. Selectivity depends on the degree of freedom between the two pharmacophore moieties. Analogs with a hydrazine linker show noticeable binding selectivity to μ receptors (IC50(μ)=0.72nM; IC50(δ)=4.66nM), while the peptides with a 1,2-phenylenediamine linker show slight δ selectivity (IC50(μ)=10.97nM; IC50(δ)=1.99nM). Tyr-d-Ala-Gly-β(3)-h-p-NO2PheNHNH-β(3)-h-p-NO2Phe (1) and (Tyr-d-Ala-Gly-β(3)-h-p-NO2PheNH)2 (2) produced greater antinociceptive effect compared to morphine after i.t. administration.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.peptides.2015.02.004 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Synergistic Improvement of Narrow Bandgap PbS Quantum Dot Solar Cells through Surface Ligand Engineering, Near-Infrared Spectral Matching, and Enhanced Electrode Transparency.
ACS Appl Mater Interfaces
January 2025
CSIR-National Chemical Laboratory, Dr. Homi Bhabha Road, Pune 411008, India.
The tunability of the energy bandgap in the near-infrared (NIR) range uniquely positions colloidal lead sulfide (PbS) quantum dots (QDs) as a versatile material to enhance the performance of existing perovskite and silicon solar cells in tandem architectures. The desired narrow bandgap (NBG) PbS QDs exhibit polar (111) and nonpolar (100) terminal facets, making effective surface passivation through ligand engineering highly challenging. Despite recent breakthroughs in surface ligand engineering, NBG PbS QDs suffer from uncontrolled agglomeration in solid films, leading to increased energy disorder and trap formation.
View Article and Find Full Text PDFExperiences of Oral Corticosteroid Use and Adverse Effects: A National Cross-Sectional Survey of People with Asthma.
Patient Prefer Adherence
January 2025
Respiratory Research@Alfred, Monash University, Melbourne, VIC, Australia.
Purpose: Oral corticosteroids (OCS) are an effective treatment for severe uncontrolled asthma or asthma exacerbations, but frequent bursts or long-term use carry serious and sometimes irreversible adverse effects, or complications such as adrenal insufficiency upon discontinuation. Our aim was to survey people with asthma on their experiences of, and attitudes towards, using OCS.
Patients And Methods: This study was a national descriptive cross-sectional survey of people with asthma in Australia.
Density Functional Theory Investigation of 2D Phase Separated Graphene/Hexagonal Boron Nitride Monolayers; Band Gap, Band Edge Positions, and Photo Activity.
J Phys Chem C Nanomater Interfaces
January 2025
Institute de Quimica Computacional i Catálisi, Universitat de Girona, Girona 17003 Spain.
Creating sustainable and stable semiconductors for energy conversion via catalysis, such as water splitting and carbon dioxide reduction, is a major challenge in modern materials chemistry, propelled by the limited and dwindling reserves of platinum group metals. Two-dimensional hexagonal borocarbonitride (h-BCN) is a metal-free alternative and ternary semiconductor, possessing tunable electronic properties between that of hexagonal boron nitride (h-BN) and graphene, and has attracted significant attention as a nonmetallic catalyst for a host of technologically relevant chemical reactions. Herein, we use density functional theory to investigate the stability and optoelectronic properties of phase-separated monolayer h-BCN structures, varying carbon concentration and domain size.
View Article and Find Full Text PDFTrends in Research Productivity Among Residents Applying For United States Orthopedic Foot and Ankle Fellowships.
Iowa Orthop J
January 2025
The Penn State Milton S. Hershey Medical Center, Hershey, Pennsylvania, USA.
Background: Little empirical research has been done on factors evaluated in the fellowship matching process, this study intends to evaluate the impact of research productivity.
Objective: The purpose of this study is to identify research trends and characterize the academic profiles of recent Foot and Ankle (F&A) fellows in the United States when they applied for fellowship.
Methods: The American Orthopedic F&A Society website was used to identify accepted fellows between the years 2017-2023.
Coronal Malalignment Is Infrequently Present in Patients With Aseptic Tibial Loosening.
Iowa Orthop J
January 2025
Vanderbilt University Medical Center, Nashville, Tennessee, USA.
Background: Coronal lower extremity malalignment and improper implant position have been described as risk factors for aseptic tibial loosening following primary total knee arthroplasty (TKA). However, several prior studies have shown no association between alignment and implant loosening. Meanwhile, there is increasing interest in kinematic alignment.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!