Evidence map›Paper›PMID 34536549›Full record

ArticlePharmacological research2021

Development of a triazolobenzodiazepine-based PET probe for subtype-selective vasopressin 1A receptor imaging.

Achi Haider, Zhiwei Xiao, Xiaotian Xia, Jiahui Chen, Richard S Van, Shi Kuang, Chunyu Zhao, Jian Rong, Tuo Shao, Perla Ramesh and 5 more

Open access · greenAbstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Pharmacological research, 2021. 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
1.1field-weighted citation impact, top 21% 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

4 citing papers in PubMed, 6 citations in OpenAlex.

  1. SAR-Guided Scaffold Innovation of Selective VACS medicinal chemistry letters · 2026
    Article
  2. Discovery and evaluation of a novelActa pharmaceutica Sinica. B · 2024
    Article
  3. Article
  4. 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

15 authors at 4 institutions in 2 countries.

Achi HaiderDepartment of Radiology, Division of Nuclear Medicine and Molecular Imaging Massachusetts General Hospital and Harvard Medical School, 55 Fruit Street, Boston, MA 02114, United States.
Zhiwei XiaoDepartment of Radiology, Division of Nuclear Medicine and Molecular Imaging Massachusetts General Hospital and Harvard Medical School, 55 Fruit Street, Boston, MA 02114, United States.
Xiaotian XiaDepartment of Radiology, Division of Nuclear Medicine and Molecular Imaging Massachusetts General Hospital and Harvard Medical School, 55 Fruit Street, Boston, MA 02114, United States; Department of Nuclear Medicine, Union Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan 430022, China.
Jiahui ChenDepartment of Radiology, Division of Nuclear Medicine and Molecular Imaging Massachusetts General Hospital and Harvard Medical School, 55 Fruit Street, Boston, MA 02114, United States.
Richard S VanDepartment of Chemistry and Biochemistry, University of Oklahoma, Norman, OK 73019, United States.
Shi KuangAthinoula A. Martinos Center for Biomedical Imaging, Massachusetts General Hospital and Harvard Medical School, Boston, MA 02129, United States.
Chunyu ZhaoDepartment of Radiology, Division of Nuclear Medicine and Molecular Imaging Massachusetts General Hospital and Harvard Medical School, 55 Fruit Street, Boston, MA 02114, United States.
Jian RongDepartment of Radiology, Division of Nuclear Medicine and Molecular Imaging Massachusetts General Hospital and Harvard Medical School, 55 Fruit Street, Boston, MA 02114, United States.
Tuo ShaoDepartment of Radiology, Division of Nuclear Medicine and Molecular Imaging Massachusetts General Hospital and Harvard Medical School, 55 Fruit Street, Boston, MA 02114, United States.
Perla RameshSambi Pharma Pvt. Ltd., Hyderabad 500060, India.
Appu AravindSambi Pharma Pvt. Ltd., Hyderabad 500060, India.
Yihan ShaoDepartment of Chemistry and Biochemistry, University of Oklahoma, Norman, OK 73019, United States.
Chongzhao RanAthinoula A. Martinos Center for Biomedical Imaging, Massachusetts General Hospital and Harvard Medical School, Boston, MA 02129, United States.
Larry J YoungSilvio O. Conte Center for Oxytocin and Social Cognition, Center for Translational Social Neuroscience, Yerkes National Primate Research Center, Emory University, Atlanta, GA, United States; Department of Psychiatry and Behavioral Sciences, Emory University School of Medicine, Atlanta, GA, United Stated.
Steven H LiangDepartment of Radiology, Division of Nuclear Medicine and Molecular Imaging Massachusetts General Hospital and Harvard Medical School, 55 Fruit Street, Boston, MA 02114, United States. Electronic address: liang.steven@mgh.harvard.edu.
Harvard University · USUniversity of Oklahoma · USEmory University · USUnion Hospital · CN

Funding

Yerkes National Primate Research Center Role of type-I IFN in regulating COVID-19 induced inflammation and pathogenesisP51OD011132 · OD · EMORY UNIVERSITY · PI Joon Sup Lee · 2012 to 2026
$167.0M
The Impact of Oxytocin on the Neural Representation Social Stimuli P50MH100023 · NIMH · EMORY UNIVERSITY · PI SANCHEZ, MAR M · 2013 to 2022
$21.8M
NIH HHS P51 OD011132NIMH NIH HHS P50 MH100023
6 · The paper itself

Abstract

objectivesTo enable non-invasive real-time quantification of vasopressin 1A (V1A) receptors in peripheral organs, we sought to develop a suitable PET probe that would allow specific and selective V1A receptor imaging in vitro and in vivo.

methodsWe synthesized a high-affinity and -selectivity ligand, designated compound 17. The target structure was labeled with carbon-11 and tested for its utility as a V1A-targeted PET tracer by cell uptake studies, autoradiography, in vivo PET imaging and ex vivo biodistribution experiments.

resultsCompound 17 (PF-184563) and the respective precursor for radiolabeling were synthesized in an overall yield of 49% (over 7 steps) and 40% (over 8 steps), respectively. An inhibitory constant of 0.9 nM towards the V1A receptors was measured, while excellent selectivity over the related V1B, V2 and OT receptor (IC

conclusionWe have developed the first V1A-targeted PET ligand that is suitable for subtype-selective receptor imaging in peripheral organs including the liver, heart, pancreas and spleen. Our findings suggest that [

Indexed as

AnimalsAutoradiographyBenzodiazepinesCarbon RadioisotopesCHO CellsCricetulusFemaleLigandsLiverMaleMiceMyocardiumPancreasPositron-Emission TomographyRadiopharmaceuticalsRatsBenzodiazepinesCarbon-11Carbon RadioisotopesLigandsRadiopharmaceuticalsReceptors, VasopressinTriazolesPharmacologyPositron emission tomographyTracer developmentTriazolobenzodiazepinesVasopressin 1A receptor

Identifiers

PMID34536549
PMCPMC8581590
OpenAlexW3201616976

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.