Many different receptors and ion channels that regulate ion currents are involved in the control of the cardiovascular system (CVS). The functioning of the CVS occurs with the involvement of the processes of nervous and humoral regulation; in both cases, acetylcholine receptors of different families and subtypes as well as of different localization take part in these processes. It was demonstrated that acetylcholine receptors are directly located on the cell membranes of the heart and blood vessels; and this review considers the regulation of CVS functions with the involvement of only those acetylcholine receptors that are located in the tissue of the heart and blood vessels. In general, both muscarinic and nicotinic acetylcholine receptors are widely present in the tissues of the CVS. At the same time, muscarinic acetylcholine receptors are generally involved in the regulation of vascular tone and contractility of the heart, while nicotinic acetylcholine receptors are mainly involved in the regulation of a number of important pathophysiological processes directly affecting the functioning of the CVS. The regulation of the functioning of acetylcholine receptors can be considered as an addition to the existing methods of treating CVS diseases, including such diseases as atherosclerosis and heart failure. The use of blockers and activators of acetylcholine receptors for the study and/or treatment of pathological conditions of CVS is discussed.