Evidence map›Paper›PMID 26751410›Full record

ArticleJournal of neuroendocrinology2016

Carbetocin is a Functional Selective Gq Agonist That Does Not Promote Oxytocin Receptor Recycling After Inducing β-Arrestin-Independent Internalisation.

I Passoni, M Leonzino, V Gigliucci, B Chini, M Busnelli

Open access · hybridAbstract read
In one paragraph

Article in Journal of neuroendocrinology, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 23 papers.

0numbers the graph read from it
0cells of the map it votes in
23citing papers in PubMed
6.4field-weighted citation impact, top 4% 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

23 citing papers in PubMed, 68 citations in OpenAlex.

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  16. Alcohol and oxytocin: Scrutinizing the relationship.Neuroscience and biobehavioral reviews · 2021
    Review
  17. Review
  18. Review
  19. Article
  20. The New Frontier in Oxytocin Physiology: The Oxytonic Contraction.International journal of molecular sciences · 2020
    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

5 authors at 2 institutions in 1 country.

I PassoniDepartment of Medical Biotechnology and Translational Medicine, Università degli Studi di Milano, Milan, Italy.
M LeonzinoCNR, Institute of Neuroscience, Milan, Italy.
V GigliucciCNR, Institute of Neuroscience, Milan, Italy.
B ChiniCNR, Institute of Neuroscience, Milan, Italy.
M BusnelliDepartment of Medical Biotechnology and Translational Medicine, Università degli Studi di Milano, Milan, Italy.
Neuroscience Institute · ITUniversity of Milan · IT

Funding

Telethon GGP12207
6 · The paper itself

Abstract

Carbetocin, a long-acting oxytocin analogue, has been reported to elicit interesting and peculiar behavioural effects. The present study investigated the molecular pharmacology of carbetocin, aiming to better understand the molecular basis of its action in the brain. Using bioluminescence resonance energy transfer biosensors, we characterised the effects of carbetocin on the three human oxytocin/vasopressin receptors expressed in the nervous system: the oxytocin receptor (OXTR) and the vasopressin V1a (V1aR) and V1b (V1bR) receptors. Our results indicate that (i) carbetocin activates the OXTR but not the V1aR and V1bR at which it may act as an antagonist; (ii) carbetocin selectively activates only the OXTR/Gq pathway displaying a strong functional selectivity; (iii) carbetocin is a partial agonist at the OXTR/Gq coupling; (iv) carbetocin promotes OXTR internalisation via a previously unreported β-arrestin-independent pathway; and (v) carbetocin does not induce OXTR recycling to the plasma membrane. Altogether, these molecular pharmacology features identify carbetocin as a substantially different analogue compared to the endogenous oxytocin and, consequently, carbetocin is not expected to mimic oxytocin in the brain. Whether these unique features of carbetocin could be exploited therapeutically remains to be established.

Indexed as

Antidiuretic Hormone Receptor Antagonistsbeta-ArrestinsCells, CulturedEndocytosisHumansOxytocinReceptors, OxytocinReceptors, VasopressinAntidiuretic Hormone Receptor AntagonistsAVPR1A protein, humanAVPR1b protein, humanbeta-ArrestinscarbetocinOXTR protein, humanOxytocinReceptors, OxytocinReceptors, Vasopressincarbetocinoxytocin receptorreceptor recyclingvasopressin receptorβ-arrestins

Identifiers

PMID26751410
PMCPMC5021139
OpenAlexW2224382515

What OpenQuestion holds

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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.