As heart failure (HF) is a devastating health problem worldwide, a better understanding
and the development of more effective therapeutic approaches are required. HF is characterized by
sympathetic system activation which stimulates α- and β-adrenoceptors (ARs). The exposure of the
cardiovascular system to the increased locally released and circulating levels of catecholamines leads to a
well-described downregulation and desensitization of β-ARs. However, information on the role of α-AR
is limited. We have performed a systematic literature review examining the role of both cardiac and
vascular α1-ARs in HF using 5 databases for our search. All three α1-AR subtypes (α1A, α1B and α1D) are
expressed in human and animal hearts and blood vessels in a tissue-dependent manner. We summarize
the changes observed in HF regarding the density, signaling and responses of α1-ARs. Conflicting
findings arise from different studies concerning the influence that HF has on α1-AR expression and
function; in contrast to β-ARs there is no consistent evidence for down-regulation or desensitization of
cardiac or vascular α1-ARs. Whether α1-ARs are a therapeutic target in HF remains a matter of debate