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@ARTICLE{Torre:283125,
author = {Torre, Eleonora and Faure, Mélanie and Bidaud, Isabelle
and Baudot, Matthias and Gaillardon, Marvin and Pereira de
Vasconcelos, Walma and Laarioui, Sihame and Talssi, Leïla
and Engeland, Birgit and Reiken, Steven and Saponaro, Andrea
and Chen, Bi-Xing and Moroni, Anna and D'Souza, Alicia and
Isbrandt, Dirk and Marks, Andrew R and Marx, Steven O and
Mesirca, Pietro and Mangoni, Matteo E},
title = {{L}-{T}ype {C}av1.3 and {HCN} {C}hannels {M}ediate {H}eart
{R}ate {A}cceleration by {C}atecholamines.},
journal = {Circulation research},
volume = {138},
number = {1},
issn = {0009-7330},
address = {New York, NY},
publisher = {Assoc.},
reportid = {DZNE-2026-00021},
pages = {e327497},
year = {2026},
abstract = {The ionic mechanism by which catecholamines increase the
heart rate is incompletely understood. In this study, we
have assessed the roles of sinoatrial node L-type Cav1.3
(α1D) Ca2+ channels, phosphorylation of L-type channel
regulatory partner protein Rad (Ras-related RGK GTP-binding
protein), and cAMP-dependent regulation of
hyperpolarization-activated HCN (hyperpolarization-activated
cyclic nucleotide-gated) channels.We studied β-adrenergic
regulation of heart rate and sinoatrial pacemaker activity
in mice lacking Cav1.3 channels and in mice expressing
dihydropyridine-insensitive L-type Cav1.2 channels alone or
concomitantly expressing cAMP-insensitive HCN4 subunits in a
heart-specific and time-controlled manner. We also studied
the chronotropic response to sympathomimetics of sinoatrial
pacemaker myocytes under conditions of specific inhibition
of cAMP-dependent regulation of HCN4 by the cyclic
dinucleotide cyclic di-(3',5')-GMP and ablation of PKA
(protein kinase A)-dependent phosphorylation of Rad.Mutant
mice with knockout of Cav1.3 and cAMP-insensitive HCN4
subunits in the heart lacked diurnal variation in heart rate
and failed to increase their heart rate after administration
of catecholamines or during physical activity. Selective
pharmacological inhibition of Cav1.3 prevented the
enhancement of pacemaker activity by sympathomimetics or by
direct activation of adenylate cyclase, as well as by
phosphodiesterase inhibitors, when cAMP-dependent regulation
of HCN was simultaneously silenced. Upregulation of Cav1.3
and HCN-mediated funny current (If) accounted for the total
change in diastolic current on activation of
β-adrenoceptors, explaining the loss of chronotropic effect
of catecholamines. Preventing PKA phosphorylation of Rad
abrogated the chronotropic response to sympathomimetics of
intact hearts under HCN blockade, or in pacemaker myocytes
on preventing cAMP-dependent regulation of HCN4,
respectively.PKA phosphorylation of Rad, which disinhibits
Cav1.3 channels and cAMP-dependent activation of HCN
channels, are key effectors in β-adrenergic regulation of
cardiac pacemaker activity and can sustain positive
chronotropic effects independently. These findings on
Rad-mediated regulation of Cav1.3 and HCN channels unravel
the ionic mechanisms underlying the catecholaminergic
acceleration of the heart rate.},
keywords = {Animals / Hyperpolarization-Activated Cyclic
Nucleotide-Gated Channels: metabolism /
Hyperpolarization-Activated Cyclic Nucleotide-Gated
Channels: genetics / Heart Rate: drug effects / Heart Rate:
physiology / Mice / Calcium Channels, L-Type: genetics /
Calcium Channels, L-Type: metabolism / Calcium Channels,
L-Type: deficiency / Calcium Channels, L-Type: physiology /
Phosphorylation / Catecholamines: pharmacology /
Catecholamines: metabolism / Sinoatrial Node: drug effects /
Sinoatrial Node: metabolism / Sinoatrial Node: physiology /
Sinoatrial Node: cytology / Mice, Knockout / Cyclic
AMP-Dependent Protein Kinases: metabolism / Cyclic AMP:
metabolism / Myocytes, Cardiac: drug effects / Myocytes,
Cardiac: metabolism / Mice, Inbred C57BL / Male / Muscle
Proteins: metabolism / Adrenergic beta-Agonists:
pharmacology / ras Proteins / catecholamines (Other) / heart
rate (Other) / phosphorylation (Other) / sinoatrial node
(Other) / sympathomimetics (Other) /
Hyperpolarization-Activated Cyclic Nucleotide-Gated Channels
(NLM Chemicals) / Calcium Channels, L-Type (NLM Chemicals) /
Catecholamines (NLM Chemicals) / Cyclic AMP-Dependent
Protein Kinases (NLM Chemicals) / Cyclic AMP (NLM Chemicals)
/ Hcn4 protein, mouse (NLM Chemicals) / Rrad protein, mouse
(NLM Chemicals) / Muscle Proteins (NLM Chemicals) /
Adrenergic beta-Agonists (NLM Chemicals) / ras Proteins (NLM
Chemicals)},
cin = {AG Isbrandt},
ddc = {610},
cid = {I:(DE-2719)1011003},
pnm = {351 - Brain Function (POF4-351)},
pid = {G:(DE-HGF)POF4-351},
typ = {PUB:(DE-HGF)16},
pubmed = {pmid:41342134},
pmc = {pmc:PMC12757128},
doi = {10.1161/CIRCRESAHA.125.327497},
url = {https://pub.dzne.de/record/283125},
}