phospholipase c inhibitors

John Arne R|ttingen j.a.rottingen at basalmed.uio.no
Tue Aug 1 10:26:10 EST 1995


In article <3uh5g8$19n at cville-srv.wam.umd.edu>, nedens at wam.umd.edu (Neile Kay Edens) says:
>
>has anyone ever tried using the phospholipase c inhibitor u73122,
>sold by biomol, in adipocytes?  i've gotten bizarre effects on glucose
>metabolism.  i'dlike to know if others have had the same experience,
>or have found other inhibitors that work well.
>

I have used U73122 in Madin Darby canine kidney cells when i measure cytosolic
free calcium by fura-2. 

I manage to inhibit the signal, but I see a gradual increase in the calcium
level indicating some unspecific effects. Other investigators have also found
unspecific effects of U73122. Willems et al (Eur J Physiol 1994; 427:233) 
found that U73122 could induce Ca2+ oscillations, Alter et al (Life Sciences 
1994; 54:107 say that U73122 does not specifically inhibit PLC, and Vickers
(J Pharmacol Exp Therapeu 1993; 266: 1156) says that U73122 affects the 
equilibria between the phosphoinositides.

I would recommend that you do a search in Medline to see if any other reports 
on unspesific effects have been published. Please, inform us if you find any.

Finally!
Every specific inhibitor gets less and less specific from the day it is released
until noone will use it anymore.




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