Tìm theo
XP13512
Thuốc Gốc
Small Molecule
XP13512 is a patented new chemical entity internally discovered at XenoPort. It is in clinical development for the potential treatment of restless legs syndrome, or RLS, and neuropathic pain. It is a Transported Prodrug of gabapentin, a drug that has been sold by Pfizer Inc as Neurontin since 1993 and is currently sold as a generic drug by a number of companies. XP13512 is being investigated by XenoPort, Inc.
Cơ Chế Tác Dụng : XP13512 is a patented new chemical entity internally discovered at XenoPort. It is in clinical development for the potential treatment of restless legs syndrome, or RLS, and neuropathic pain. It is a Transported Prodrug of gabapentin, a drug that has been sold by Pfizer Inc as Neurontin since 1993 and is currently sold as a generic drug by a number of companies. XP13512 is being investigated by XenoPort, Inc. XP13512 is a prodrug of gabapentin. Gabapentin interacts with cortical neurons at auxillary subunits of voltage-sensitive calcium channels. It increases the synaptic concentration of GABA, enhances GABA responses at non-synaptic sites in neuronal tissues, and reduces the release of mono-amine neurotransmitters. One of the mechanisms implicated in this effect of gabapentin is the reduction of the axon excitability measured as an amplitude change of the presynaptic fibre volley (FV) in the CA1 area of the hippocampus. This is mediated through its binding to presynaptic NMDA receptors. Other studies have shown that the antihyperalgesic and antiallodynic effects of gabapentin are mediated by the descending noradrenergic system, resulting in the activation of spinal alpha2-adrenergic receptors. Gabapentin has also been shown to bind and activate the adenosine A1 receptor.
Dược Động Học :
▧ Absorption :
Absorbed following oral administration.
▧ Metabolism :
Converted to gabapentin following absorption. Gabapentin is not appreciably metabolized in humans.
Chỉ Định : For the potential treatment of restless legs syndrome, or RLS, and neuropathic pain.
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB04922
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