Skip to main content
. Author manuscript; available in PMC: 2010 May 14.
Published in final edited form as: Bioorg Med Chem Lett. 2009 Jan 23;19(13):3686–3692. doi: 10.1016/j.bmcl.2009.01.057

Figure 3. Effect of PDE inhibition on β2AR regulated PKA activities in vivo.

Figure 3

Bioluminescence in A-C was detected from stable β2AR-HEK293 (see reference 19) cells transiently transfected with the PKA reporter Reg-F[1]:Cat-F[2]2 (from three independent experiments). (A) Effect of combinations of pretreatment with the selective β2AR-antagonist 20 (1 μM) and treatment with 1 (100 μM; 30 min) or 19 (1 μM, 30 min) on the on the association of Reg-F[1]:Cat-F[2] (mean ± s.d. from independent triplicates). (B) Concentration dependent effect of 18, 10 and a related triazolothiadiazine that possesses no PDE4 inhibition on the association of Reg-F[1]:Cat-F[2] (30 min, mean ± s.d. from independent triplicates). Percentage of PKA activation is normalized based upon 20 (1 μM) pretreated cells. (C) Real-time kinetics (normalized on the control experiment = pretreatment with 1 μM 20) of Reg-F[1]:Cat-F[2] dissociation in response to 10 treatment (10 μM, four independent samples).