Evidence map›Paper›PMID 25601315›Full record

ReviewPharmacology & therapeutics2015

Structure and function of serotonin G protein-coupled receptors.

John D McCorvy, Bryan L Roth

Abstract readReview
In one paragraph

Review in Pharmacology & therapeutics, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 180 papers.

0numbers the graph read from it
0cells of the map it votes in
180citing papers in PubMed
12.1field-weighted citation impact, top 1% 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

180 citing papers in PubMed, 361 citations in OpenAlex.

  1. Trial
  2. Deciphering the allosteric landscape of 5-HTPharmacological reports : PR · 2026
    Article
  3. Article
  4. The working lives of neuronal 5-HTRSC chemical biology · 2026
    Review
  5. Serotonin-endocannabinoid crosstalk selectively regulates inhibitory GABAergic inputs in the medial prefrontal cortex.Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology · 2026
    Article
  6. Article
  7. Review
  8. Article
  9. Article
  10. Review
  11. Stereoselective, sex-dependent 5-HTNeuropsychopharmacology : official publication of the American College of Neuropsychopharmacology · 2026
    Article
  12. Review
  13. Article
  14. Article
  15. Article
  16. Review
  17. Review
  18. Article
  19. Article
  20. Article

120 more citing papers are in PubMed but not listed here.

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

2 authors at 1 institution in 1 country.

John D McCorvyDepartment of Pharmacology and Division of Chemical Biology and Medicinal Chemistry, University of North Carolina Chapel Hill Medical School, Chapel Hill, NC 27514, USA.
Bryan L RothDepartment of Pharmacology and Division of Chemical Biology and Medicinal Chemistry, University of North Carolina Chapel Hill Medical School, Chapel Hill, NC 27514, USA.
University of North Carolina at Chapel Hill · US

Funding

Screening CoreU19MH082441 · NIMH · UNIV OF NORTH CAROLINA CHAPEL HILL · PI CARON, MARC G., CARON, MARC G. · 2007 to 2016
$15.2M
Targeting and Trafficking of 5-HT2A Serotonin ReceptorsR01MH061887 · NIMH · UNIV OF NORTH CAROLINA CHAPEL HILL · PI ROTH, BRYAN L. · 2000 to 2014
$4.5M
DREADD2.0: AN ENHANCED CHEMOGENETIC TOOLKITU01MH105892 · NIMH · UNIV OF NORTH CAROLINA CHAPEL HILL · PI JIN, JIAN, KASH, THOMAS L. · 2014 to 2016
$3.0M
Optimizing Lead 5-HT2c Ligands for Use in the Treatment of SchizophreniaR01MH099993 · NIMH · UNIVERSITY OF ILLINOIS AT CHICAGO · PI CALDARONE, BARBARA J., ROTH, BRYAN L. · 2013 to 2016
$2.8M
NIMH NIH HHS R01 MH061887NIMH NIH HHS R01 MH099993NIMH NIH HHS U01 MH105892NIMH NIH HHS U19 MH082441
6 · The paper itself

Abstract

Serotonin receptors are prevalent throughout the nervous system and the periphery, and remain one of the most lucrative and promising drug discovery targets for disorders ranging from migraine headaches to neuropsychiatric disorders such as schizophrenia and depression. There are 14 distinct serotonin receptors, of which 13 are G protein-coupled receptors (GPCRs), which are targets for approximately 40% of the approved medicines. Recent crystallographic and biochemical evidence has provided a converging understanding of the basic structure and functional mechanics of GPCR activation. Currently, two GPCR crystal structures exist for the serotonin family, the 5-HT1B and 5-HT2B receptor, with the antimigraine and valvulopathic drug ergotamine bound. The first serotonin crystal structures not only provide the first evidence of serotonin receptor topography but also provide mechanistic explanations into functional selectivity or biased agonism. This review will detail the findings of these crystal structures from a molecular and mutagenesis perspective for driving rational drug design for novel therapeutics incorporating biased signaling.

Indexed as

Allosteric SiteAnimalsErgotamineGTP-Binding ProteinsHeart Valve DiseasesHumansMigraine DisordersModels, MolecularProtein ConformationReceptor, Serotonin, 5-HT1BReceptor, Serotonin, 5-HT2BReceptors, SerotoninSerotonin Receptor AgonistsSignal TransductionVasoconstrictor AgentsErgotamineGTP-Binding ProteinsReceptor, Serotonin, 5-HT1BReceptor, Serotonin, 5-HT2BReceptors, SerotoninSerotonin Receptor AgonistsVasoconstrictor Agents5-HT(1B)5-HT(2B)Functional selectivityGPCRSerotoninβ-Arrestin

Identifiers

PMID25601315
PMCPMC4414735
OpenAlexW2011312787

What Socratic 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 Socratic graph.