Evidence map›Paper›PMID 28105279›Full record

ArticleACS medicinal chemistry letters2017

Nanoconjugated NAP as a Potent and Periphery Selective Mu Opioid Receptor Modulator To Treat Opioid-Induced Constipation.

Guoyan G Xu, Olga Yu Zolotarskaya, Dwight A Williams, Yunyun Yuan, Dana E Selley, William L Dewey, Hamid I Akbarali, Hu Yang, Yan Zhang

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in ACS medicinal chemistry letters, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 2 papers.

0numbers the graph read from it
0cells of the map it votes in
2citing papers in PubMed
0.5field-weighted citation impact, top 29% of its field
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

2 citing papers in PubMed, 5 citations in OpenAlex.

  1. Trial
  2. Nanotherapeutics for Alleviating Anesthesia-Associated Complications.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2024
    Review
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

9 authors at 1 institution in 1 country.

Guoyan G XuDepartment of Medicinal Chemistry, Virginia Commonwealth University , 800 E Leigh Street, Richmond, Virginia 23298, United States.
Olga Yu ZolotarskayaDepartment of Chemical and Life Science Engineering, Virginia Commonwealth University , 401 West Main Street, Richmond, Virginia 23284, United States.
Dwight A WilliamsDepartment of Medicinal Chemistry, Virginia Commonwealth University, 800 E Leigh Street, Richmond, Virginia 23298, United States; Department of Pharmacology and Toxicology, Virginia Commonwealth University, 410 North 12th Street, Richmond, Virginia 23298, United States.
Yunyun YuanDepartment of Medicinal Chemistry, Virginia Commonwealth University , 800 E Leigh Street, Richmond, Virginia 23298, United States.
Dana E SelleyDepartment of Pharmacology and Toxicology, Virginia Commonwealth University , 410 North 12th Street, Richmond, Virginia 23298, United States.
William L DeweyDepartment of Pharmacology and Toxicology, Virginia Commonwealth University , 410 North 12th Street, Richmond, Virginia 23298, United States.
Hamid I AkbaraliDepartment of Pharmacology and Toxicology, Virginia Commonwealth University , 410 North 12th Street, Richmond, Virginia 23298, United States.
Hu YangDepartment of Chemical and Life Science Engineering, Virginia Commonwealth University, 401 West Main Street, Richmond, Virginia 23284, United States; Department of Pharmaceutics, Virginia Commonwealth University, 410 N 12th Street, Richmond, Virginia 23298, United States; Massey Cancer Center, Virginia Commonwealth University, 401 College Street, Richmond, Virginia 23298, United States.
Yan ZhangDepartment of Medicinal Chemistry, Virginia Commonwealth University, 800 E Leigh Street, Richmond, Virginia 23298, United States; Massey Cancer Center, Virginia Commonwealth University, 401 College Street, Richmond, Virginia 23298, United States.
Virginia Commonwealth University · US

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Opioids are the mainstay for cancer and noncancer pain management. However, their use is often associated with multiple adverse effects. Among them, the most common and persistent one is probably opioid-induced constipation (OIC). Periphery selective opioid antagonists may alleviate the symptoms of OIC without compromising the analgesic effects of opioids. Recently our laboratories have identified one novel lead compound, 17-cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6β-[(4'-pyridyl)acetamido]morphinan (NAP), as a peripherally selective mu opioid receptor ligand carrying subnanomolar affinity to the mu opioid receptor and over 100-folds of selectivity over both the delta and kappa opioid receptors, with reasonable oral availability and half-life, and potential to treat OIC. Nanoparticle-based drug delivery systems are now widely considered due to their technological advantages such as good stability, high carrier capacity, low therapeutic side effects, etc. Herein we report nanoparticle supported NAP as a potential candidate for OIC treatment with improved peripheral selectivity over the original lead compound NAP.

Indexed as

Mu opioid receptor antagonistnanoconjugateNAPOpioid-induced constipationPeriphery selective

Identifiers

PMID28105279
PMCPMC5238486
OpenAlexW2551489686

What OpenQuestion holds

Textmetadata
Read underepoch 390

Registered trials

None linked

Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.