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E-Conference: Defining Calcium Entry Signals

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Pharmacology of SOCs and ARC

18 June 2004

Reinhold Penner

Don,

the 3,5-bistrifluoromethyl pyrazole (BTP2) compound you mentioned is very problematic. I must issue a big warning to anyone using this compound as a potent and selective inhibitor of CRAC. It isn't!!!

Unfortunately, our paper on this compound just got rejected by Science, so I can't be more specific about the mechanisms involved in its action. It is true that BTP2 will completely shut off Ca2+ influx in lymphocytes at low nanomolar concentrations, but this effect is due to an as yet unpublished mechanism... This novel mechanism is very important to consider when relying only on fura-2 measurements to assess SOC.

Sorry to be so secretive about this, but please be advised that BTP2 should not be considered a SOC inhibitor at low concentrations.

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