disorders of alcohol consumption (AUD) is
the most common form of drug abuse. The development of tolerance to repeated
AUD contains lead alcohol, alcohol withdrawal syndrome (AWS), physical and
psychological dependence, to control the loss of excessive alcohol consumption
capacity. Currently there is no effective therapeutic agents for AUD without
significant side effects. Dihydromyricetin (EHD, 1 mg / kg, ip injection), a
flavonoid component of herbal medicines, counteracts acute alcohol (EtOH)
noise, and withdrawal symptoms in rats, including tolerance, increased anxiety
and seizure susceptibility; DHM significantly reduces the consumption of EtOH
rats intermittent voluntary EtOH intake paradigm. GABA (speed) are important
goals of acute and chronic EtOH actions on the brain. At the cellular level DHM
(1 uM) antagonizes induced potentiation EtOH-acute BARs GABA and EtOH exposure
/ induced weaning GABAAR plasticity, including changes in the reactivity of the
extracellular GABAARs and postsynaptic acute EtOH, and especially, increases in
-unity GABAAR α4 expression in the hippocampus and neurons in culture.
anti-alcohol effects DHM behavior and neurons of the central nervous system
have been stymied by flumazenil (10 mg / kg in vivo, in vitro 10 uM), the
benzodiazepine (BZ) antagonist. DHM competitive inhibited the site BZ [3H]
flunitrazepam binding (IC50, 4.36 uM), suggesting a DHM interaction with EtOH
comprises the BZ sites GABAARs. In summary, we found an anti-alcohol effect DHM
animal models and determines an important molecular target and cellular
mechanism of EHD counteract alcohol intoxication and dependence. We have shown
the pharmacological properties of DHM are in line with expectations of a
successful medical treatment AUD to reason; So DHM is a therapeutic candidate.
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