Yam Code

New Paste Browse

https://www.selleckchem.com/CDK.html Lacosamide is a new-generation anticonvulsant acting on Na+ channels. Compared to the classic anticonvulsants targeting Na+ channels, lacosamide is unique in structure and in its molecular action requiring longer membrane depolarization. Selective binding to the slow inactivated state of Na+ channels was then advocated for lacosamide, although slow binding to the fast inactivated state was alternatively proposed recently. In addition, quantitative characterization of lacosamide action has been deficient. We investigated the interactions between lacosamide and Na+ channels in native mammalian neurons, and found that the apparent dissociation constant (~13.7 μM) of lacosamide to the slow inactivated state is well within the therapeutic concentration range and is much (>15-fold) lower than the dissociation constant of lacosamide to the fast inactivated state. Besides, lacosamide has extremely slow binding rates (3000 M-1sec-1) to the slow inactivated Na+ channels. Consistent with these biophysical characters, we further demonstrated that lacosamide is much more effective against the repetitive burst discharges with interburst intervals at -60 mV than -80 mV. With preponderant binding to the slow inactivation state in therapeutic concentrations and thus less propensity to affect normal discharges, lacosamide could be a drug of choice for seizure discharges characterized by relatively depolarized interburst intervals, during which more slow inactivated states could be generated and more binding of lacosamide would ensue. Traumatic brain injury (TBI) is one of the most prevalent injuries in the military with mild traumatic brain injury (mTBI) accounting for approximately 70-80 % of all TBI. TBI has been associated with diffuse and focal brain changes to structures and networks underlying cognitive-emotional processing. Although the anterior cingulate cortex (ACC) plays a critical role in emotion regulation and executive function and is

Paste Settings

Paste Title : [Optional]

Paste Folder : [Optional]

Syntax Highlighting : [Optional]

Paste Expiration : [Optional]

Paste Status : [Optional]

Password : [Optional]

Description: [Optional]

Tags: [Optional]

Encrypt Paste (?)

You are currently not logged in, this means you can not edit or delete anything you paste. Sign Up or Login

Paste Settings

Site Languages