Literature DB >> 19886609

Might adrenergic alpha2C-agonists/alpha2A-antagonists become novel therapeutic tools for pain treatment with morphine?

Claudia Cardinaletti1, Laura Mattioli, Francesca Ghelfi, Fabio Del Bello, Mario Giannella, Ariana Bruzzone, Hervé Paris, Marina Perfumi, Alessandro Piergentili, Wilma Quaglia, Maria Pigini.   

Abstract

The imidazoline nucleus linked in position 2 via an oxyethylene bridge to a phenyl ring carrying an ortho substituent of moderate steric bulk provided alpha(2)-adrenergic (AR) ligands endowed with significant alpha(2C)-agonism/alpha(2A)-antagonism. Similar behavior was displayed by cirazoline (12). For their positive morphine analgesia modulation (due to alpha(2C)-AR stimulation) and sedation overcoming (due to alpha(2A)-AR antagonism), 8 and 11 might be useful as adjuvant agents in the management of pain with morphine.

Entities:  

Mesh：

Substances：

Year:  2009        PMID： 19886609     DOI： 10.1021/jm901262f

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  6 in total

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

Authors:  Fabio Del Bello; Valentina Bargelli; Carlo Cifani; Paola Gratteri; Carla Bazzicalupi; Eleonora Diamanti; Mario Giannella; Valerio Mammoli; Rosanna Matucci; Maria Vittoria Micioni Di Bonaventura; Alessandro Piergentili; Wilma Quaglia; Maria Pigini
Journal:  ACS Med Chem Lett       Date:  2015-04-03       Impact factor: 4.345

2.  Exploring multitarget interactions to reduce opiate withdrawal syndrome and psychiatric comorbidity.

Authors:  Fabio Del Bello; Eleonora Diamanti; Mario Giannella; Valerio Mammoli; Laura Mattioli; Federica Titomanlio; Alessandro Piergentili; Wilma Quaglia; Marco Lanza; Chiara Sabatini; Gianfranco Caselli; Elena Poggesi; Maria Pigini
Journal:  ACS Med Chem Lett       Date:  2013-07-22       Impact factor: 4.345

3.  Low Doses of Allyphenyline and Cyclomethyline, Effective against Morphine Dependence, Elicit an Antidepressant-like Effect.

Authors:  Fabio Del Bello; Eleonora Diamanti; Mario Giannella; Valerio Mammoli; Carla Marchioro; Laura Mattioli; Federica Titomanlio; Alessandro Piergentili; Wilma Quaglia; Giovanni Benedetti; Maurizio Varrone; Maria Pigini
Journal:  ACS Med Chem Lett       Date:  2012-06-08       Impact factor: 4.345

4.  Dual Alpha2C/5HT1A Receptor Agonist Allyphenyline Induces Gastroprotection and Inhibits Fundic and Colonic Contractility.

Authors:  Zoltán S Zádori; Ágnes Fehér; Viktória E Tóth; Mahmoud Al-Khrasani; László Köles; Szabina Sipos; Fabio Del Bello; Maria Pigini; Klára Gyires
Journal:  Dig Dis Sci       Date:  2016-02-10       Impact factor: 3.199

5.  A Novel Class of Dopamine D4 Receptor Ligands Bearing an Imidazoline Nucleus.

Authors:  Valerio Mammoli; Alessandro Bonifazi; Diego Dal Ben; Mario Giannella; Gianfabio Giorgioni; Alessandro Piergentili; Maria Pigini; Wilma Quaglia; Ajiroghene Thomas; Amy H Newman; Sergi Ferré; Marta Sanchez-Soto; Thomas M Keck; Fabio Del Bello
Journal:  ChemMedChem       Date:  2016-03-15       Impact factor: 3.466

6.  The Use of the Selective Imidazoline I1 Receptor Agonist Carbophenyline as a Strategy for Neuropathic Pain Relief: Preclinical Evaluation in a Mouse Model of Oxaliplatin-Induced Neurotoxicity.

Authors:  Laura Micheli; Lorenzo Di Cesare Mannelli; Fabio Del Bello; Mario Giannella; Alessandro Piergentili; Wilma Quaglia; Donatello Carrino; Alessandra Pacini; Carla Ghelardini
Journal:  Neurotherapeutics       Date:  2020-07       Impact factor: 6.088
  6 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.