Tapentadol Hcl;CAS NO 850222-41-2/175591-09-0
Product Name:Tapentadol Hcl
Agonism of the MOR is a common strategy for moderate to severe pain intervention. Opioid drugs, such as morphine, that modulate this receptor have demonstrated efficacy in acute situations; however, chronic conditions, particularly those of neuropathic or inflammatory etiology, suffer from inadequate pain management with this treatment. With a narrow therapeutic window, traditional MOR agonists flirt with side effects at optimal analgesia, and prolonged use increases the potential for physical dependency. Since extensive efforts to design activators of MOR have failed to dissociate the undesirable adverse effects from the analgesic properties, the focus has been on enhancing the analgesic efficacy through a dual mechanism of action. Tapentadol hydrochloride brings this concept to fruition; MOR agonism is coupled with noradrenaline reuptake inhibition in a combinatory contribution to analgesia. Compared to morphine, it is about 50-fold less potent for MOR (Ki = 100 nM for tapentadol versus 2 nM for morphine). The Ki for inhibition of noradrenaline reuptake was 500 nM while reuptake of serotonin was only weakly inhibited (Ki = 2.5μM). Despite its lower affinity for MOR, the dual mechanism has provided an efficacious profile in both acute and chronic conditions with fewer side effects.
A novel, centrally acting oral analgesic with a dual mode of action that has demonstrated efficacy in preclinical and clinical models of pain relief.
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Last Update : Jul 14, 2020
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