Evidence map›Paper›PMID 28395140›Full record

ArticleJournal of medicinal chemistry2017

Pyrazolopyrimidines as Potent Stimulators for Transient Receptor Potential Canonical 3/6/7 Channels.

Chunrong Qu, Mingmin Ding, Yingmin Zhu, Yungang Lu, Juan Du, Melissa Miller, Jinbin Tian, Jinmei Zhu, Jian Xu, Meng Wen and 13 more

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Journal of medicinal chemistry, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 24 papers.

0numbers the graph read from it
0cells of the map it votes in
24citing 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

24 citing papers in PubMed.

  1. Access to Pyrazolo[1,5-Organic letters · 2026
    Article
  2. Review
  3. Article
  4. Review
  5. Review
  6. Review
  7. TRPV3: Structure, Diseases and Modulators.Molecules (Basel, Switzerland) · 2023
    Review
  8. Article
  9. Ion channels alterations in the forebrain of high-fat diet fed rats.European journal of histochemistry : EJH · 2021
    Article
  10. Article
  11. Article
  12. Review
  13. Review
  14. TRPC4 as a coincident detector of GCurrent opinion in physiology · 2020
    Article
  15. Review
  16. Review
  17. Article
  18. Article
  19. Article
  20. 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

23 authors.

Chunrong QuState Key Laboratory of Virology, Key Laboratory of Combinatorial Biosynthesis and Drug Discovery (MOE) and Hubei Province Engineering and Technology Research Center for Fluorinated Pharmaceuticals, Wuhan University School of Pharmaceutical Sciences , Wuhan, Hubei Province 430071, China.
Mingmin DingState Key Laboratory of Virology, Key Laboratory of Combinatorial Biosynthesis and Drug Discovery (MOE) and Hubei Province Engineering and Technology Research Center for Fluorinated Pharmaceuticals, Wuhan University School of Pharmaceutical Sciences , Wuhan, Hubei Province 430071, China.
Yingmin ZhuDepartment of Integrative Biology and Pharmacology, McGovern Medical School, The University of Texas Health Science Center at Houston , Houston, Texas 77030, United States.
Yungang LuDepartment of Integrative Biology and Pharmacology, McGovern Medical School, The University of Texas Health Science Center at Houston , Houston, Texas 77030, United States.
Juan DuSchool of Basic Medical Sciences, Anhui Medical University , Hefei, Anhui Province 230032, China.
Melissa MillerDepartment of Neuroscience, High Throughput Biology Center and Johns Hopkins Ion Channel Center, Johns Hopkins University School of Medicine , Baltimore, Maryland 21205, United States.
Jinbin TianDepartment of Integrative Biology and Pharmacology, McGovern Medical School, The University of Texas Health Science Center at Houston , Houston, Texas 77030, United States.
Jinmei ZhuState Key Laboratory of Virology, Key Laboratory of Combinatorial Biosynthesis and Drug Discovery (MOE) and Hubei Province Engineering and Technology Research Center for Fluorinated Pharmaceuticals, Wuhan University School of Pharmaceutical Sciences , Wuhan, Hubei Province 430071, China.
Jian XuState Key Laboratory of Natural Medicines, Jiangsu Provincial Key laboratory for TCM Evaluation and Translational Development, China Pharmaceutical University , Nanjing, Jiangsu Province 211198, China.
Meng WenState Key Laboratory of Virology, Key Laboratory of Combinatorial Biosynthesis and Drug Discovery (MOE) and Hubei Province Engineering and Technology Research Center for Fluorinated Pharmaceuticals, Wuhan University School of Pharmaceutical Sciences , Wuhan, Hubei Province 430071, China.
Aga Er-BuMedical College, Tibet University , Lasa, Tibet 850000, China.
Jule WangMedical College, Tibet University , Lasa, Tibet 850000, China.
Yuling XiaoState Key Laboratory of Virology, Key Laboratory of Combinatorial Biosynthesis and Drug Discovery (MOE) and Hubei Province Engineering and Technology Research Center for Fluorinated Pharmaceuticals, Wuhan University School of Pharmaceutical Sciences , Wuhan, Hubei Province 430071, China.
Meng WuDepartment of Neuroscience, High Throughput Biology Center and Johns Hopkins Ion Channel Center, Johns Hopkins University School of Medicine , Baltimore, Maryland 21205, United States.
Owen B McManusDepartment of Neuroscience, High Throughput Biology Center and Johns Hopkins Ion Channel Center, Johns Hopkins University School of Medicine , Baltimore, Maryland 21205, United States.
Min LiDepartment of Neuroscience, High Throughput Biology Center and Johns Hopkins Ion Channel Center, Johns Hopkins University School of Medicine , Baltimore, Maryland 21205, United States.
Jilin WuThe International Scientist Working Station of Neuropharmacology, Shanghai Institute of Materia Medica, Chinese Academy of Sciences , Shanghai, 201203, China.
Huai-Rong LuoKey Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences , Kunming, Yunnan Province 650201, China.
Zhengyu CaoState Key Laboratory of Natural Medicines, Jiangsu Provincial Key laboratory for TCM Evaluation and Translational Development, China Pharmaceutical University , Nanjing, Jiangsu Province 211198, China.
Bing ShenSchool of Basic Medical Sciences, Anhui Medical University , Hefei, Anhui Province 230032, China.
Hongbo WangSchool of Pharmacy, Key Laboratory of Molecular Pharmacology and Drug Evaluation (Yantai University), Ministry of Education, Yantai University , Yantai, Shangdong Province 264005, China.
Michael X ZhuDepartment of Integrative Biology and Pharmacology, McGovern Medical School, The University of Texas Health Science Center at Houston , Houston, Texas 77030, United States.
Xuechuan HongState Key Laboratory of Virology, Key Laboratory of Combinatorial Biosynthesis and Drug Discovery (MOE) and Hubei Province Engineering and Technology Research Center for Fluorinated Pharmaceuticals, Wuhan University School of Pharmaceutical Sciences , Wuhan, Hubei Province 430071, China.ORCID 0000-0001-6834-3278

Funding

Johns Hopkins Ion Channel CenterU54MH084691 · NIMH · JOHNS HOPKINS UNIVERSITY · PI LI, MIN · 2008 to 2012
$13.9M
Training Program in Cellular and Molecular MedicineT32GM008752 · NIGMS · JOHNS HOPKINS UNIVERSITY · PI RAO, RAJINI · 2000 to 2019
$11.7M
Excitatory neurotransmission by PTX-sensitive G proteinsR01NS092377 · NINDS · UNIVERSITY OF TEXAS HLTH SCI CTR HOUSTON · PI ZHU, MICHAEL X · 2015 to 2019
$1.7M
High throughput screening of ligands of TRP channelsR21NS056942 · NINDS · OHIO STATE UNIVERSITY · PI ZHU, MICHAEL X · 2006 to 2008
$261k
NIGMS NIH HHS T32 GM008752NIMH NIH HHS U54 MH084691NINDS NIH HHS R01 NS092377NINDS NIH HHS R21 NS056942
6 · The paper itself

Abstract

Transient receptor potential canonical 3/6/7 (TRPC3/6/7) are highly homologous receptor-operated nonselective cation channels. Despite their physiological significance, very few selective and potent agonists are available for functional examination of these channels. Using a cell-based high throughput screening approach, a lead compound with the pyrazolopyrimidine skeleton was identified as a TRPC6 agonist. Synthetic schemes for the lead and its analogues were established, and structural-activity relationship studies were carried out. A series of potent and direct agonists of TRPC3/6/7 channels were identified, and among them, 4m-4p have a potency order of TRPC3 > C7 > C6, with 4n being the most potent with an EC

Indexed as

HEK293 CellsHumansPyrazolesPyrimidinesStructure-Activity RelationshipTRPC6 Cation ChannelTRPC Cation ChannelsPyrazolesPyrimidinesTRPC3 cation channelTRPC6 Cation ChannelTRPC6 protein, humanTRPC7 protein, humanTRPC Cation Channels

Identifiers

PMID28395140
PMCPMC5720685

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.