Evidence map›Paper›PMID 33202534›Full record

ReviewPharmaceuticals (Basel, Switzerland)2020

Allosteric Modulators of G Protein-Coupled Dopamine and Serotonin Receptors: A New Class of Atypical Antipsychotics.

Irene Fasciani, Francesco Petragnano, Gabriella Aloisi, Francesco Marampon, Marco Carli, Marco Scarselli, Roberto Maggio, Mario Rossi

Open access · goldAbstract readReview
In one paragraph

Review in Pharmaceuticals (Basel, Switzerland), 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.

0numbers the graph read from it
0cells of the map it votes in
16citing papers in PubMed
1.6field-weighted citation impact, top 16% 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

16 citing papers in PubMed, 25 citations in OpenAlex.

  1. Dual-Acting Vitamin BJournal of medicinal chemistry · 2026
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  9. ExploringFrontiers in fungal biology · 2023
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  11. Review
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  15. Current Developments on the Role of αFrontiers in cell and developmental biology · 2021
    Review
  16. 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

8 authors at 4 institutions in 2 countries.

Irene FascianiDepartment of Biotechnological and Applied Clinical Sciences, University of l'Aquila, 67100 L'Aquila, Italy.
Francesco PetragnanoDepartment of Biotechnological and Applied Clinical Sciences, University of l'Aquila, 67100 L'Aquila, Italy.
Gabriella AloisiDepartment of Biotechnological and Applied Clinical Sciences, University of l'Aquila, 67100 L'Aquila, Italy.
Francesco MaramponDepartment of Radiotherapy, "Sapienza" University of Rome, Policlinico Umberto I, 00161 Rome, Italy.
Marco CarliDepartment of Translational Research and New Technology in Medicine and Surgery, University of Pisa, 56126 Pisa, Italy.ORCID 0000-0003-1447-4947
Marco ScarselliDepartment of Translational Research and New Technology in Medicine and Surgery, University of Pisa, 56126 Pisa, Italy.
Roberto MaggioDepartment of Biotechnological and Applied Clinical Sciences, University of l'Aquila, 67100 L'Aquila, Italy.ORCID 0000-0003-4436-2356
Mario RossiInstitute of Molecular Cell and Systems Biology, University of Glasgow, Glasgow G12 8QQ, UK.
University of L'Aquila · ITUniversity of Pisa · ITPoliclinico Umberto I · ITUniversity of Glasgow · GB

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Schizophrenia was first described by Emil Krapelin in the 19th century as one of the major mental illnesses causing disability worldwide. Since the introduction of chlorpromazine in 1952, strategies aimed at modifying the activity of dopamine receptors have played a major role for the treatment of schizophrenia. The introduction of atypical antipsychotics with clozapine broadened the range of potential targets for the treatment of this psychiatric disease, as they also modify the activity of the serotoninergic receptors. Interestingly, all marketed drugs for schizophrenia bind to the orthosteric binding pocket of the receptor as competitive antagonists or partial agonists. In recent years, a strong effort to develop allosteric modulators as potential therapeutic agents for schizophrenia was made, mainly for the several advantages in their use. In particular, the allosteric binding sites are topographically distinct from the orthosteric pockets, and thus drugs targeting these sites have a higher degree of receptor subunit specificity. Moreover, "pure" allosteric modulators maintain the temporal and spatial fidelity of native orthosteric ligand. Furthermore, allosteric modulators have a "ceiling effect", and their modulatory effect is saturated above certain concentrations. In this review, we summarize the progresses made in the identification of allosteric drugs for dopamine and serotonin receptors, which could lead to a new generation of atypical antipsychotics with a better profile, especially in terms of reduced side effects.

Indexed as

allosteric binding sitedopamine receptorendogenous allosteric modulatornegative allosteric modulatororthosteric binding sitepositive allosteric modulatorserotonin (5-HT) receptor

Identifiers

PMID33202534
PMCPMC7696972
OpenAlexW3106530255

What OpenQuestion holds

Textmetadata
LicenceCC BY
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.