Opioid addiction is often characterized as a chronic relapsing condition due to the severe somatic and behavioral signs, associated with depressive disorders, triggered by opiate withdrawal. Since prolonged abstinence remains a major challenge, our interest has been addressed to such objective. Exploring multitarget interactions, the present investigation suggests that 3 or its (S)-enantiomer and 4, endowed with effective alpha(2C)-AR agonism/alpha(2A)-AR antagonism/5-HT1A-R agonism, or 7 and 9-11 producing efficacious alpha(2C)-AR agonism/alpha(2A)-AR antagonism/I-2-IBS interaction might represent novel multifunctional tools potentially useful for reducing withdrawal syndrome and associated depression. Such agents, lacking in sedative side effects due to their alpha(2A)-AR antagonism, might afford an improvement over current therapies with clonidine-like drugs.
Del Bello, F., Diamanti, E., Giannella, M., Mammoli, V., Mattioli, L., Titomanlio, F., et al. (2013). Exploring multitarget interactions to reduce opiate withdrawal syndrome and psychiatric comorbidity. ACS MEDICINAL CHEMISTRY LETTERS, 4(9), 875-879 [10.1021/ml400232p].
Exploring multitarget interactions to reduce opiate withdrawal syndrome and psychiatric comorbidity
Diamanti, Eleonora;
2013
Abstract
Opioid addiction is often characterized as a chronic relapsing condition due to the severe somatic and behavioral signs, associated with depressive disorders, triggered by opiate withdrawal. Since prolonged abstinence remains a major challenge, our interest has been addressed to such objective. Exploring multitarget interactions, the present investigation suggests that 3 or its (S)-enantiomer and 4, endowed with effective alpha(2C)-AR agonism/alpha(2A)-AR antagonism/5-HT1A-R agonism, or 7 and 9-11 producing efficacious alpha(2C)-AR agonism/alpha(2A)-AR antagonism/I-2-IBS interaction might represent novel multifunctional tools potentially useful for reducing withdrawal syndrome and associated depression. Such agents, lacking in sedative side effects due to their alpha(2A)-AR antagonism, might afford an improvement over current therapies with clonidine-like drugs.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
