β1-Adrenergic receptor agonists, also known as beta-1 agonists, are a class of drugs that bind selectively to the β1-adrenergic receptor. As a result, they act more selectively upon the heart. β-Adrenoceptors typically bind to norepinephrine release by sympathetic adrenergic nerves and to circulating epinephrine. The effect of β-adrenoceptors is cardiac stimulation, such as increased heart rate, heart contractility, heart conduction velocity, and heart relaxation.

Examples

Examples include: Norepinephrine reuptake inhibitors, like atomoxetine, methylphenidate, and cocaine, as well as norepinephrine releasing agents, like amphetamine, ephedrine, pseudoephedrine, and phenylpropanolamine, indirectly activate β1-adrenergic receptors (as well as other adrenergic receptors) by increasing norepinephrine and/or epinephrine levels. As a result, they can be referred to as indirectly acting sympathomimetics.