The nociceptin/Orphanin FQ (N/OFQ) peptide (NOP) receptor is a G protein-coupled receptor with a high degree of structural homology (~ 60%) to the classical opioid receptors μ, δ and κ. The interaction between NOPand its endogenous agonist N/OFQ plays a key role in pain transmission, among other biological functions. Therefore, this system opened a new option for the treatment of acute and chronic pain possibly by generating drugs with a lower side effect profile.The confirmed affinity towards NOP receptor of the α2 adrenergic and 5-HT1A partial agonist spiroxatrine (Ki= 127 nM) has led us to the synthesis of a series of novel and optimized analogs based upon the spiropiperidinecore, in order to perform preliminarySAR studies.
Synthesis, structural characterization and pharmacological evaluation of spiroxatrine analogs as potential nociceptin/orphanin FQ receptor ligands / Corrado, Sandra; Battisti, Umberto; Sorbi, Claudia; Malfacini, Davide; Calò, Girolamo; Brasili, Livio; Tait, Annalisa. - ELETTRONICO. - -:(2012), pp. 66-66. (Intervento presentato al convegno Paul Ehrlich MedChem Euro-PhD Network tenutosi a Lubiana nel 9th - 11th September 2012).
Synthesis, structural characterization and pharmacological evaluation of spiroxatrine analogs as potential nociceptin/orphanin FQ receptor ligands
SORBI, Claudia;BRASILI, Livio;TAIT, Annalisa
2012
Abstract
The nociceptin/Orphanin FQ (N/OFQ) peptide (NOP) receptor is a G protein-coupled receptor with a high degree of structural homology (~ 60%) to the classical opioid receptors μ, δ and κ. The interaction between NOPand its endogenous agonist N/OFQ plays a key role in pain transmission, among other biological functions. Therefore, this system opened a new option for the treatment of acute and chronic pain possibly by generating drugs with a lower side effect profile.The confirmed affinity towards NOP receptor of the α2 adrenergic and 5-HT1A partial agonist spiroxatrine (Ki= 127 nM) has led us to the synthesis of a series of novel and optimized analogs based upon the spiropiperidinecore, in order to perform preliminarySAR studies.
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