Beta1-adrenergic agonist

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.^[1]

Examples

Examples include:

• Denopamine (selective β₁ agonist)^[2][3]
• Dobutamine (β₁>β₂ agonist)
• Xamoterol (β₁ partial agonist)
• Epinephrine (non-selective)
• Norepinephrine (non-selective)
• Isoprenaline (non-selective)

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.^[4] As a result, they can be referred to as indirectly acting sympathomimetics.^[4]