Evidence map›Paper›PMID 30117738›Full record

ArticleJournal of medicinal chemistry2018

Potent and Selective Tetrahydroisoquinoline Kappa Opioid Receptor Antagonists of Lead Compound (3 R)-7-Hydroxy- N-[(1 S)-2-methyl-1-(piperidin-1-ylmethyl)propyl]-1,2,3,4-tetrahydroisoquinoline-3-carboxamide (PDTic).

Pauline W Ondachi, Chad M Kormos, Scott P Runyon, James B Thomas, S Wayne Mascarella, Ann M Decker, Hernán A Navarro, Timothy R Fennell, Rodney W Snyder, F Ivy Carroll

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Journal of medicinal chemistry, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 6 papers.

0numbers the graph read from it
0cells of the map it votes in
6citing 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

6 citing papers in PubMed.

  1. Article
  2. The Magic Methyl and Its Tricks in Drug Discovery and Development.Pharmaceuticals (Basel, Switzerland) · 2023
    Review
  3. Article
  4. Article
  5. Review
  6. 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

10 authors.

Pauline W OndachiResearch Triangle Institute , P.O. Box 12194, Research Triangle Park , North Carolina 27709-2194 , United States.
Chad M KormosResearch Triangle Institute , P.O. Box 12194, Research Triangle Park , North Carolina 27709-2194 , United States.ORCID 0000-0002-9394-2317
Scott P RunyonResearch Triangle Institute , P.O. Box 12194, Research Triangle Park , North Carolina 27709-2194 , United States.
James B ThomasResearch Triangle Institute , P.O. Box 12194, Research Triangle Park , North Carolina 27709-2194 , United States.
S Wayne MascarellaResearch Triangle Institute , P.O. Box 12194, Research Triangle Park , North Carolina 27709-2194 , United States.ORCID 0000-0003-0092-8178
Ann M DeckerResearch Triangle Institute , P.O. Box 12194, Research Triangle Park , North Carolina 27709-2194 , United States.
Hernán A NavarroResearch Triangle Institute , P.O. Box 12194, Research Triangle Park , North Carolina 27709-2194 , United States.
Timothy R FennellResearch Triangle Institute , P.O. Box 12194, Research Triangle Park , North Carolina 27709-2194 , United States.
Rodney W SnyderResearch Triangle Institute , P.O. Box 12194, Research Triangle Park , North Carolina 27709-2194 , United States.
F Ivy CarrollResearch Triangle Institute , P.O. Box 12194, Research Triangle Park , North Carolina 27709-2194 , United States.ORCID 0000-0001-9510-765X

Funding

Selective Opioid Antagonists as Medications for Drug AbuseR01DA009045 · NIDA · RESEARCH TRIANGLE INSTITUTE · PI CARROLL, FRANK IVY · 1994 to 2014
$5.6M
NIDA NIH HHS R01 DA009045
6 · The paper itself

Abstract

Past studies have shown that it has been difficult to discover and develop potent and selective κ opioid receptor antagonists, particularly compounds having potential for clinical development. In this study, we present a structure-activity relationship (SAR) study of a recently discovered new class of tetrahydroisoquinoline κ opioid receptor antagonists which led to (3 R)-7-hydroxy- N-{(1 S)-2-methyl-1-[(-4-methylpiperidine-1-yl)methyl]propyl}-1,2,3,4-tetrahydroisoquinoline-3-carboxamide (12) (4-Me-PDTic). Compound 12 had a K

Indexed as

AnimalsBrainCHO CellsCricetulusGuanosine 5'-O-(3-Thiotriphosphate)HumansMaleNarcotic AntagonistsRadioligand AssayRats, Sprague-DawleyReceptors, Opioid, deltaReceptors, Opioid, kappaReceptors, Opioid, muStructure-Activity RelationshipTetrahydroisoquinolines1,2,3,4-tetrahydroisoquinolineGuanosine 5'-O-(3-Thiotriphosphate)Narcotic AntagonistsReceptors, Opioid, deltaReceptors, Opioid, kappaReceptors, Opioid, muTetrahydroisoquinolines

Identifiers

PMID30117738
PMCPMC6692079

What OpenQuestion holds

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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.