A possible therapeutic approach for the clinical management of acute and chronic pain is polypharmacology, or the associations between two or more drugs producing biological effects on two or more different sites of action, by modulating directly or indirectly the analgesic profile and possible adverse effects. Today, considering the benefits of polypharmacology in the drug discovery process the "one-molecule multiple target" strategy has been recognized. For multitarget ligands a better analgesic activity with fewer side effects – detected in the association of drugs – coupled with favourable pharmacokinetic and pharmacodynamic characteristics have been proven. Given that the various mediators involved in the circuit of pain represent potential targets for different pharmacological interventions, multitarget ligands possessing opioid-opioid or non-opioid-opioid mechanisms of action are potential drug candidates for the management of various pain conditions. Low propensity to induce side effects was reported for multitarget ligands, able to act simultaneously on multiple opioid receptors subtypes. In particular, an improved analgesic profile associated with a reduced tolerance-inducing capability was found in mixed MOR (mu-opioid receptor)-DOR (delta-opioid receptor)ligands. In this context, the benzomorphan-based compound LP1 belongs to the class of multitarget ligand. In this manuscript the pharmacological fingerprint of LP1 as suitable drug candidate in pain relief is described.
|Titolo:||The Benzomorphan-Based Compound LP1 as Suitable Candidate for Pain Management|
|Data di pubblicazione:||2016|
|Appare nelle tipologie:||1.1 Articolo in rivista|