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
[edit]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]
References
[edit]- ^ Sakuma, Tsutomu; Hida, Mieko; Nambu, Yoshihiro; Osanai, Kazuhiro; Toga, Hirohisa; Takahashi, Keiji; Ohya, Nobuo; Inoue, Masao; Watanabe, Yoh (2001). "Beta1-Adrenergic Agonist Is a Potent Stimulator of Alveolar Fluid Clearance in Hyperoxic Rat Lungs". The Japanese Journal of Pharmacology. 85 (2): 161–166. doi:10.1254/jjp.85.161. ISSN 0021-5198. PMID 11286398.
- ^ Sakuma T, Hida M, Nambu Y, et al. (February 2001). "Beta1-adrenergic agonist is a potent stimulator of alveolar fluid clearance in hyperoxic rat lungs". Jpn. J. Pharmacol. 85 (2): 161–6. doi:10.1254/jjp.85.161. PMID 11286398.
- ^ Nishio R, Matsumori A, Shioi T, et al. (September 1998). "Denopamine, a beta1-adrenergic agonist, prolongs survival in a murine model of congestive heart failure induced by viral myocarditis: suppression of tumor necrosis factor-alpha production in the heart". J. Am. Coll. Cardiol. 32 (3): 808–15. doi:10.1016/S0735-1097(98)00314-3. hdl:2433/181223. PMID 9741531.
- ^ a b Biaggioni, I., & Robertson, D. (2018). Adrenoceptor Agonists & Sympathomimetic Drugs. Basic & Clinical Pharmacology, 14th Edition, 137–155. https://scholar.google.com/scholar?cluster=8160024720742860204
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