This review summarizes the pharmacological potential of catecholamine signaling for the treatment of socially significant diseases such as depression, Parkinson’s disease, hypertension, etc. The catecholamines dopamine, norepinephrine and epinephrine are released as neurotransmitters in nervous system and as hormones as well. The hormone prolactostatin is known to be biochemically dopamine and is continuously secreted by hypothalamic neurons in both sexes. Norepinephrine, as the main mediator released from postganglionic endings of sympathetic neurons, activates alpha- and beta-adrenoreceptors of target cells. In adrenal medulla, norepinephrine is a precursor for epinephrine synthesis and is released in small amounts as a hormone. Both norepinephrine and epinephrine induce stress responses by generalized sympathetic “fight-or-flight” response that increases cardiac output, blood pressure and breathing. A common therapeutic approach is usage of pharmacological substances that influence the adrenergic signaling. Additionally, treatments with drugs like reserpine, desipramine, 6-hydroxydopamine and others are useful tools for studding the role of local reuptake, de novo synthesis and plasma catecholamines in the regulation of physiological processes.