Evidence map›Paper›PMID 27717652›Full record

ArticleBioorganic & medicinal chemistry2016

Synthesis and evaluation of the structural elements in alkylated tetrahydroisoquinolines for binding to CNS receptors.

Edward Ofori, Xue Y Zhu, Jagan R Etukala, Barbara A Bricker, Seth Y Ablordeppey

Abstract read
In one paragraph

Article in Bioorganic & medicinal chemistry, 2016. 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. Design and discovery of a high affinity, selective and β-arrestin biased 5-HTMedicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents · 2022
    Article
  3. New dual 5-HT1A and 5-HT7 receptor ligands derived from SYA16263.European journal of medicinal chemistry · 2021
    Article
  4. Article
  5. Article
  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

5 authors.

Edward OforiDivision of Basic Pharmaceutical Sciences, Florida A&M University, College of Pharmacy and Pharmaceutical Sciences, Tallahassee, FL 32307, USA.
Xue Y ZhuDivision of Basic Pharmaceutical Sciences, Florida A&M University, College of Pharmacy and Pharmaceutical Sciences, Tallahassee, FL 32307, USA.
Jagan R EtukalaDivision of Basic Pharmaceutical Sciences, Florida A&M University, College of Pharmacy and Pharmaceutical Sciences, Tallahassee, FL 32307, USA.
Barbara A BrickerDivision of Basic Pharmaceutical Sciences, Florida A&M University, College of Pharmacy and Pharmaceutical Sciences, Tallahassee, FL 32307, USA.
Seth Y AblordeppeyDivision of Basic Pharmaceutical Sciences, Florida A&M University, College of Pharmacy and Pharmaceutical Sciences, Tallahassee, FL 32307, USA.

Funding

THE PREVENTION OF B(A)P INDUCED CELL TRANSFORMATION BY ORGANOSULFUR COMPOUNDSG12RR003020 · NCRR · FLORIDA AGRICULTURAL AND MECHANICAL UNIV · PI SOLIMAN, KARAM F.A. · 1985 to 2011
$29.7M
Recruitment and HiringG12MD007582 · NIMHD · FLORIDA AGRICULTURAL AND MECHANICAL UNIV · PI SOLIMAN, KARAM F.A. · 2012 to 2017
$16.0M
Targeted Nanocarrier Combination Based Therapy for Lung CancerP20MD006738 · NIMHD · FLORIDA AGRICULTURAL AND MECHANICAL UNIV · PI RAHMAN, SALEH MD. MAHMUDUR · 2012 to 2016
$5.6M
A New Approach for the Development of Novel Antipsychotic DrugsSC1GM116724 · NIGMS · FLORIDA AGRICULTURAL AND MECHANICAL UNIV · PI ABLORDEPPEY, SETH Y · 2016 to 2019
$1.4M
PHARMACEUTICAL RESEARCH CENTERC06RR012512 · NCRR · FLORIDA AGRICULTURAL AND MECHANICAL UNIV · PI LEWIS, HENRY · 1997 to 1997
–
NCRR NIH HHS C06 RR012512NCRR NIH HHS G12 RR003020NIGMS NIH HHS SC1 GM116724NIMHD NIH HHS G12 MD007582NIMHD NIH HHS P20 MD006738
6 · The paper itself

Abstract

Diseases of the CNS are often complex and involve multiple receptor systems and thus, the treatment options for these diseases must focus on targeting the multiple receptors implicated in the various disorders. Schizophrenia and depression are examples of such diseases and their pharmacotherapy thus depends on agents which target multiple receptors including the dopamine, serotonin and even cholinergic receptors at the same time. In our previous campaign to find multi-receptor ligands, we have identified the benzothiazole 1a as an initial lead molecule. In the current work, we have expanded the structure affinity relationship (SAFIR) of 1a resulting in the identification of a partially restrained butyrophenone 3j as a potent and selective dual 5-HT

Indexed as

Binding SitesDose-Response Relationship, DrugHumansLigandsMolecular StructureReceptor, Serotonin, 5-HT1AReceptors, SerotoninStructure-Activity RelationshipTetrahydroisoquinolinesLigandsReceptor, Serotonin, 5-HT1AReceptors, Serotoninserotonin 7 receptorTetrahydroisoquinolinesAntipsychoticCNS ligandsDual receptor ligandsMulti-receptor ligandsStructure affinity relationship

Identifiers

PMID27717652
PMCPMC5079764

What OpenQuestion holds

Textmetadata
LicenceTDM
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.