SI
SI
discoversearch

We've detected that you're using an ad content blocking browser plug-in or feature. Ads provide a critical source of revenue to the continued operation of Silicon Investor.  We ask that you disable ad blocking while on Silicon Investor in the best interests of our community.  If you are not using an ad blocker but are still receiving this message, make sure your browser's tracking protection is set to the 'standard' level.
Biotech / Medical : CVTX - CV Therapeutics, Inc.
 Public ReplyPrvt ReplyMark as Last ReadFilePrevious 10Next 10PreviousNext  
To: scaram(o)uche who wrote (363)1/2/2009 2:42:31 PM
From: Biotech Jim   of 411
 
Hello Rick and a happy and healthy new year to you! I have played around with sodium channels a bit so I can provide some comments on this work. These channels are complex in that they are large highly homologous proteins and they have regulatory subunits as well. Be careful when investigators evaluate activity of compounds in recombinant systems, as they might not have the same regulatory apparati as in the native neurons or cells. Note that it is quite difficult to evaluate selectivity against all voltage gated sodium channels, so investigators often use the major brain, cardiac and muscle forms for such studies. Note also that there are different firing rates for different neurons, and pain neurons have relatively slow firing rates (0.5 to 4 Hz). These channels have open, closed and inactive states as well.

Having said this, the work is of interest and in these biophysical they primarily focus on 1.8 and 1.7. The activity of ranolazine seems to be somewhat weak in this non-protein loaded cell system, and compounds can bind to sites in serum proteins. How about activity against the cardiac, brain and muscle forms? How about activity in the 3 major commonly used pain models?

Sorry that I do not have many answers here, but the work described is only a good start.

BJ
Report TOU ViolationShare This Post
 Public ReplyPrvt ReplyMark as Last ReadFilePrevious 10Next 10PreviousNext  

HomeMailHotSubjectMarksPeopleMarksKeepersSettings
Terms Of UseContact UsCopyright/IP PolicyPrivacy PolicyAbout UsFAQAdvertise on SI
© 2025 Knight Sac Media.  Data provided by Twelve Data, Alpha Vantage, and CityFALCON News