Evidence map›Paper›PMID 26005521›Full record

ArticleACS medicinal chemistry letters2015

Antagonism/Agonism modulation to build novel antihypertensives selectively triggering i1-imidazoline receptor activation.

Fabio Del Bello, Valentina Bargelli, Carlo Cifani, Paola Gratteri, Carla Bazzicalupi, Eleonora Diamanti, Mario Giannella, Valerio Mammoli, Rosanna Matucci, Maria Vittoria Micioni Di Bonaventura and 3 more

Open access · greenAbstract read
In one paragraph

Article in ACS medicinal chemistry letters, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 6 papers.

0numbers the graph read from it
0cells of the map it votes in
6citing papers in PubMed
1.1field-weighted citation impact, top 22% 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

6 citing papers in PubMed, 13 citations in OpenAlex.

  1. Review
  2. Discovery of (3-Phenylcarbamoyl-3,4-dihydro-2Journal of medicinal chemistry · 2025
    Article
  3. The Use of the Selective Imidazoline INeurotherapeutics : the journal of the American Society for Experimental NeuroTherapeutics · 2020
    Article
  4. Combined Interactions with IACS medicinal chemistry letters · 2016
    Article
  5. Article
  6. 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

13 authors at 2 institutions in 1 country.

Fabio Del BelloSchool of Pharmacy, Medicinal Chemistry Unit, University of Camerino , Via S. Agostino 1, 62032 Camerino, Italy.
Valentina BargelliDepartment NEUROFARBA, Preclinical and Clinical Pharmacology, University of Firenze , Viale Pieraccini 6, 50139 Firenze, Italy.
Carlo CifaniSchool of Pharmacy, Pharmacology Unit, University of Camerino , Via Madonna delle Carceri 9, 62032 Camerino, Italy.
Paola GratteriDepartment NEUROFARBA, Pharmaceutical and Nutraceutical Section and Laboratory of Molecular Modeling Cheminformatics & QSAR, University of Firenze , via Ugo Schiff 6, 50019 Sesto Fiorentino, Firenze, Italy.
Carla BazzicalupiDepartment of Chemistry Ugo Schiff, University of Firenze , Via della Lastruccia 3, 50019 Sesto Fiorentino, Italy.
Eleonora DiamantiSchool of Pharmacy, Medicinal Chemistry Unit, University of Camerino , Via S. Agostino 1, 62032 Camerino, Italy.
Mario GiannellaSchool of Pharmacy, Medicinal Chemistry Unit, University of Camerino , Via S. Agostino 1, 62032 Camerino, Italy.
Valerio MammoliSchool of Pharmacy, Medicinal Chemistry Unit, University of Camerino , Via S. Agostino 1, 62032 Camerino, Italy.
Rosanna MatucciDepartment NEUROFARBA, Preclinical and Clinical Pharmacology, University of Firenze , Viale Pieraccini 6, 50139 Firenze, Italy.
Maria Vittoria Micioni Di BonaventuraSchool of Pharmacy, Pharmacology Unit, University of Camerino , Via Madonna delle Carceri 9, 62032 Camerino, Italy.
Alessandro PiergentiliSchool of Pharmacy, Medicinal Chemistry Unit, University of Camerino , Via S. Agostino 1, 62032 Camerino, Italy.
Wilma QuagliaSchool of Pharmacy, Medicinal Chemistry Unit, University of Camerino , Via S. Agostino 1, 62032 Camerino, Italy.
Maria PiginiSchool of Pharmacy, Medicinal Chemistry Unit, University of Camerino , Via S. Agostino 1, 62032 Camerino, Italy.
Università di Camerino · ITUniversity of Florence · IT

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Pharmacological studies have suggested that I1-imidazoline receptors are involved in the regulation of cardiovascular function and that selective I1-agonists, devoid of the side effects associated with the common hypotensive α2-adrenoreceptor agonists, might be considered as a second generation of centrally acting antihypertensives. Therefore, in the present study, inspired by the antihypertensive behavior of our selective I1-agonist 4, we designed, prepared, and studied the novel analogues 5-9. A selective I1-profile, associated with significant hemodinamic effects, was displayed by 5, 8, and 9. Interestingly, the highest potency and longest lasting activity displayed by 8 (carbomethyline) suggested that van der Waals interactions, promoted by the ortho methyl decoration of its aromatic moiety, are particularly advantageous. In addition, in analogy to what was noted for (S)-(+)-4, the observation that only (S)-(+)-8 displayed significant hemodynamic effects unequivocally confirmed the stereospecific nature of the I1 proteins.

Indexed as

antihypertensive agentsbradicardic agentscarbomethylineI1-agonistsimidazoline compoundsstereoselectivity

Identifiers

PMID26005521
PMCPMC4434467
OpenAlexW2328650076

What OpenQuestion holds

Textmetadata
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.