Phosphodiesterases 3 and 4 Differentially Regulate the Funny Current, If, in Mouse Sinoatrial Node Myocytes
Related Experiment Video
Updated: Feb 23, 2026

Methods for the Isolation, Culture, and Functional Characterization of Sinoatrial Node Myocytes from Adult Mice
Published on: October 23, 2016
Joshua R St Clair1, Eric D Larson1, Emily J Sharpe1
1Department of Physiology and Biophysics, University of Colorado School of Medicine, Aurora, CO 80045, USA.
Abstract:
Cardiac pacemaking, at rest and during the sympathetic fight-or-flight response, depends on cAMP (3',5'-cyclic adenosine monophosphate) signaling in sinoatrial node myocytes (SAMs). The cardiac "funny current" (If) is among the cAMP-sensitive effectors that drive pacemaking in SAMs. If is produced by hyperpolarization-activated, cyclic nucleotide-sensitive (HCN) channels. Voltage-dependent gating of HCN channels is potentiated by cAMP, which acts either by binding directly to the channels or by activating the cAMP-dependent protein kinase (PKA), which phosphorylates them. PKA activity is required for signaling between β adrenergic receptors (βARs) and HCN channels in SAMs but the mechanism that constrains cAMP signaling to a PKA-dependent pathway is unknown. Phosphodiesterases (PDEs) hydrolyze cAMP and form cAMP signaling domains in other types of cardiomyocytes. Here we examine the role of PDEs in regulation of If in SAMs. If was recorded in whole-cell voltage-clamp experiments from acutely-isolated mouse SAMs in the absence or presence of PDE and PKA inhibitors, and before and after βAR stimulation. General PDE inhibition caused a PKA-independent depolarizing shift in the midpoint activation voltage (V1/2) of If at rest and removed the requirement for PKA in βAR-to-HCN signaling. PDE4 inhibition produced a similar PKA-independent depolarizing shift in the V1/2 of If at rest, but did not remove the requirement for PKA in βAR-to-HCN signaling. PDE3 inhibition produced PKA-dependent changes in If both at rest and in response to βAR stimulation. Our results suggest that PDE3 and PDE4 isoforms create distinct cAMP signaling domains that differentially constrain access of cAMP to HCN channels and establish the requirement for PKA in signaling between βARs and HCN channels in SAMs.
Insights
Phosphodiesterases (PDEs) regulate cardiac funny current (If) in sinoatrial node myocytes. PDE3 and PDE4 create distinct cAMP signaling domains, influencing PKA-dependent pathways essential for heart rate regulation.
Area of Science:
- Cardiovascular Physiology
- Molecular Cardiology
- Cellular Electrophysiology
Background:
- Cardiac pacemaking relies on cAMP signaling in sinoatrial node myocytes (SAMs).
- The cardiac funny current (If), carried by HCN channels, is a key cAMP-sensitive effector in SAMs.
- cAMP potentiates HCN channel gating via direct binding or PKA phosphorylation, but the mechanism constraining this signaling is unclear.
Purpose of the Study:
- To investigate the role of phosphodiesterases (PDEs) in regulating If in SAMs.
- To elucidate how PDE isoforms differentially control cAMP signaling and PKA dependence in SAMs.
Main Methods:
- Whole-cell voltage-clamp recordings of If in acutely-isolated mouse SAMs.
- Pharmacological inhibition of PDEs and PKA.
- Stimulation of β adrenergic receptors (βARs) to assess signaling pathways.
Main Results:
- General PDE inhibition induced a PKA-independent shift in If activation and removed PKA requirement for βAR-HCN signaling.
- PDE4 inhibition caused a similar PKA-independent shift at rest but retained PKA requirement for βAR signaling.
- PDE3 inhibition resulted in PKA-dependent If changes both at rest and upon βAR stimulation.
Conclusions:
- PDE3 and PDE4 isoforms establish distinct cAMP signaling domains within SAMs.
- These domains differentially regulate cAMP access to HCN channels, thereby controlling the PKA dependence of βAR-mediated signaling and heart rate regulation.
More Related Videos
Related Concept Videos
G-Protein Gated Ion Channels
Sensory...
Electrophysiology of Normal Cardiac Rhythm
Transducer Mechanism: Enzyme-Linked Receptors
Major types that are helpful drug targets include:
ATP Driven Pumps III: V-type Pumps
The peripheral or cytosolic V1 domain with eight subunits is involved in ATP hydrolysis. The integral or transmembrane V0 domain containing at least five subunits...

