Neuropathic pain is originated from different alterations of the nervous system. The difficulty of treatment strongly impairs quality of life of affected people. It is associated with severe, chronic sensory disturbances characterized by spontaneous pain, increased responsiveness to painful stimuli and pain perceived in response to normally non-noxious stimuli. The underlying mechanisms are complex and involve both peripheral and central nervous components.The noradrenergic system plays a pivotal role in the control of pain since its widespread distribution in the "pain matrix" representing a valuable therapeutic target. This review focused on the α2 adrenoceptor subtype modulation as strategy for neuropathic pain relief. Drugs acting as direct α2 adrenoceptor agonists (clonidine and dexmedetomidine) were analyzed as well as the indirect α2 adrenoceptor modulators. The overview included norepinephrine reuptake inhibitors (reboxetine, maprotiline), serotonin/norepinephrine reuptake inhibitors (venlafaxine, milnacipran, amitriptyline, duloxetine, bicifadine) and the compounds characterized by a double pharmacodynamic mechanism combining the norepinephrine reuptake inhibition and the µ opioid agonist profile (tramadol and tapentadol). A summary of recent compounds was illustrated.

α2 Adrenoceptor: a Target for Neuropathic Pain Treatment / Di Cesare Mannelli, Lorenzo; Micheli, Laura; Crocetti, Letizia; Giovannoni, Maria Paola; Vergelli, Claudia; Ghelardini, Carla. - In: MINI-REVIEWS IN MEDICINAL CHEMISTRY. - ISSN 1875-5607. - STAMPA. - 16:(2017), pp. 95-107. [10.2174/13895575166661606090655 35]

α2 Adrenoceptor: a Target for Neuropathic Pain Treatment

DI CESARE MANNELLI, LORENZO;MICHELI, LAURA;CROCETTI, LETIZIA;GIOVANNONI, MARIA PAOLA;VERGELLI, CLAUDIA;GHELARDINI, CARLA
2017

Abstract

Neuropathic pain is originated from different alterations of the nervous system. The difficulty of treatment strongly impairs quality of life of affected people. It is associated with severe, chronic sensory disturbances characterized by spontaneous pain, increased responsiveness to painful stimuli and pain perceived in response to normally non-noxious stimuli. The underlying mechanisms are complex and involve both peripheral and central nervous components.The noradrenergic system plays a pivotal role in the control of pain since its widespread distribution in the "pain matrix" representing a valuable therapeutic target. This review focused on the α2 adrenoceptor subtype modulation as strategy for neuropathic pain relief. Drugs acting as direct α2 adrenoceptor agonists (clonidine and dexmedetomidine) were analyzed as well as the indirect α2 adrenoceptor modulators. The overview included norepinephrine reuptake inhibitors (reboxetine, maprotiline), serotonin/norepinephrine reuptake inhibitors (venlafaxine, milnacipran, amitriptyline, duloxetine, bicifadine) and the compounds characterized by a double pharmacodynamic mechanism combining the norepinephrine reuptake inhibition and the µ opioid agonist profile (tramadol and tapentadol). A summary of recent compounds was illustrated.
2017
16
95
107
Di Cesare Mannelli, Lorenzo; Micheli, Laura; Crocetti, Letizia; Giovannoni, Maria Paola; Vergelli, Claudia; Ghelardini, Carla
File in questo prodotto:
File Dimensione Formato  
Di Cesare Mannelli-MS-MRMC 2016.pdf

accesso aperto

Tipologia: Pdf editoriale (Version of record)
Licenza: Tutti i diritti riservati
Dimensione 1.07 MB
Formato Adobe PDF
1.07 MB Adobe PDF

I documenti in FLORE sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.

Utilizza questo identificatore per citare o creare un link a questa risorsa: https://hdl.handle.net/2158/1060645
Citazioni
  • ???jsp.display-item.citation.pmc??? ND
  • Scopus 33
  • ???jsp.display-item.citation.isi??? 29
social impact