Recent data support the evidence that some molecules can activate ORs though they lack of the protonated amine, generally regarded to as the fundamental pharmacophore. Among such unusual ligands, we discovered the agonist c[YpwFG], having a good MOR affinity (Ki 34nM), that is an effective and potent analgesic for visceral pain when administered peripherally (i.p ED50 1,25mg/kg; s.c. ED50 2,7mg/kg), and retains moderate central analgesic effects (tail-flick, 20mg/kg).
L. Gentilucci, R. de Marco, A. Tolomelli, S. Feddersen, S. Spampinato, A. Bedini, et al. (2011). A novel family of minimalist opioid peptides deprived of the classic pharmacophores. PHARMACOLOGICAL REPORTS, 63, 212-212.
A novel family of minimalist opioid peptides deprived of the classic pharmacophores
GENTILUCCI, LUCA;DE MARCO, ROSSELLA;TOLOMELLI, ALESSANDRA;SPAMPINATO, SANTI MARIO;BEDINI, ANDREA;
2011
Abstract
Recent data support the evidence that some molecules can activate ORs though they lack of the protonated amine, generally regarded to as the fundamental pharmacophore. Among such unusual ligands, we discovered the agonist c[YpwFG], having a good MOR affinity (Ki 34nM), that is an effective and potent analgesic for visceral pain when administered peripherally (i.p ED50 1,25mg/kg; s.c. ED50 2,7mg/kg), and retains moderate central analgesic effects (tail-flick, 20mg/kg).I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
