Changes in myocardial and vascular receptors in heart failure.

Heart failure results in dramatic changes in certain neurotransmitter and hormone receptors. The majority of the changes occur in the heart and generally can be classified as regulatory phenomena that withdraw the failing heart from adrenergic stimulation. Of these, the most prominent is beta 1-receptor downregulation. Changes in vascular receptors are much less prominent and there is no direct evidence that any vascular receptor changes in heart failure. The changes that occur in myocardial receptors suggest that antiadrenergic therapy would be effective in the treatment of heart failure by removing adrenergic signaling transduced by the remaining components of the receptor pathways. Taken together, the receptor desensitization changes present in the failing heart provide a rationale for beta 1- plus beta 2-adrenergic blockade or even combined beta 1-, beta 2-alpha 1-adrenergic receptor blockade in heart failure.