Skip to main content
. Author manuscript; available in PMC: 2018 Feb 1.
Published in final edited form as: Neuropharmacology. 2016 Sep 20;113(Pt A):82–88. doi: 10.1016/j.neuropharm.2016.09.018

Table 1. Published selectivity of PKA/EPAC activators and inhibitors.

from cell culture assays. The volume:conc (concentration) values listed in column 1 were concentration and volume used for intrathecal injections in the present in-vivo study.

Drug (volume:conc) EPAC Ka PKA Ka PKA Ki EPAC Ki
6-Bnz-cAMPa (10μL:100μM) NSa 2.7μM - -
8-pCPT-2′-O-Me-cAMPa (10μL:100μM) 1.8μM 190μM - -
Rp-8-Br-cAMPa (10μL:1mM) - - 8.5μM NSi
ESI-05b (10μL:2M) - - NSi 0.43μM
Ka

concentration for half of maximum cAMP induced response

Ki

concentration for inhibition of half maximum cAMP induced response

NSa

non-significant activating effect; ≥100 fold Ka difference

NSi

non-significant inhibitory effect; ≥100 fold Ki difference