Evidence map›Paper›PMID 28603600›Full record

ArticleMedChemComm2017

Synthesis and pharmacological evaluation of novel selective MOR agonist 6β-pyridinyl amidomorphines exhibiting long-lasting antinociception.

Ákos Urai, András Váradi, Levente Szőcs, Balázs Komjáti, Valerie Le Rouzic, Amanda Hunkele, Gavril W Pasternak, Susruta Majumdar, Sándor Hosztafi

Abstract read
In one paragraph

Article in MedChemComm, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 4 papers.

0numbers the graph read from it
0cells of the map it votes in
4citing papers in PubMed
–field-weighted citation impact
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

4 citing papers in PubMed.

  1. Article
  2. Review
  3. Review
  4. Article
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.

Ákos UraiDepartment of Pharmaceutical Chemistry, Semmelweis University, Hőgyes E. u. 9., Budapest H-1092, Hungary.
András VáradiMolecular Pharmacology and Chemistry Program and Department of Neurology, Memorial Sloan Kettering Cancer Center, 1275 York Ave., New York, NY 10065, USA.
Levente SzőcsDepartment of Pharmaceutical Chemistry, Semmelweis University, Hőgyes E. u. 9., Budapest H-1092, Hungary.
Balázs KomjátiDepartment of Organic Chemistry and Technology, Budapest University of Technology and Economics, Szent Gellért tér 4, Budapest 1111, Hungary.
Valerie Le RouzicMolecular Pharmacology and Chemistry Program and Department of Neurology, Memorial Sloan Kettering Cancer Center, 1275 York Ave., New York, NY 10065, USA.
Amanda HunkeleMolecular Pharmacology and Chemistry Program and Department of Neurology, Memorial Sloan Kettering Cancer Center, 1275 York Ave., New York, NY 10065, USA.
Gavril W PasternakMolecular Pharmacology and Chemistry Program and Department of Neurology, Memorial Sloan Kettering Cancer Center, 1275 York Ave., New York, NY 10065, USA.
Susruta MajumdarMolecular Pharmacology and Chemistry Program and Department of Neurology, Memorial Sloan Kettering Cancer Center, 1275 York Ave., New York, NY 10065, USA.
Sándor HosztafiDepartment of Pharmaceutical Chemistry, Semmelweis University, Hőgyes E. u. 9., Budapest H-1092, Hungary.

Funding

X-RAY CRYSTALLOGRAPHYP30CA008748 · NCI · SLOAN-KETTERING INSTITUTE FOR CANCER RES · PI Hongbiao Carl Lekaye · 1985 to 2026
$347.4M
Synthesis &Pharmacology of Novel Opiates and SystemsR01DA006241 · NIDA · SLOAN-KETTERING INSTITUTE FOR CANCER RES · PI PAN, YING-XIAN · 1990 to 2018
$6.4M
PHARMACOLOGY OF OPIOID RECEPTOR SUBTYPESR01DA007242 · NIDA · SLOAN-KETTERING INSTITUTE FOR CANCER RES · PI PAN, YING-XIAN · 1991 to 2022
$6.0M
PHARMACOLOGY OF OPIOID RECEPTOR SUBTYPESR37DA007242 · NIDA · SLOAN-KETTERING INSTITUTE FOR CANCER RES · PI PASTERNAK, GAVRIL W · 1996 to 2004
$1.5M
Analgesics targeting truncated 6transmembrane exon 11 variants of MOR-1 (6TM-E11)R33DA034106 · NIDA · SLOAN-KETTERING INST CAN RESEARCH · PI MAJUMDAR, SUSRUTA · 2014 to 2015
$596k
Analgesics targeting truncated 6transmembrane exon 11 variants of MOR-1 (6TM-E11)R21DA034106 · NIDA · SLOAN-KETTERING INST CAN RESEARCH · PI MAJUMDAR, SUSRUTA · 2012 to 2013
$443k
NCI NIH HHS P30 CA008748NIDA NIH HHS R01 DA006241NIDA NIH HHS R01 DA007242NIDA NIH HHS R21 DA034106NIDA NIH HHS R33 DA034106NIDA NIH HHS R37 DA007242
6 · The paper itself

Abstract

It was previously reported that 6β-aminomorphinan derivatives show high affinity for opiate receptors. Novel 6β-heteroarylamidomorphinanes were designed based on the MOR selective antagonist NAP. The 6β-aminomorphinanes were prepared with stereoselective Mitsunobu reaction and subsequently acylated with nicotinic acid and isonicotinic acid chloride hydrochlorides. The receptor binding and efficacy were determined

Identifiers

PMID28603600
PMCPMC5464418

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Registered trials

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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.