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The β-blockers are an immensely important class of drugs due to their high prevalence of use. The discovery of β-blockers reaches back to more than 100 years ago, when early investigators came up with the idea that catecholamines were binding selectively to receptor-like structures and that this was the cause of their pharmacological actions. [3]
Propranolol may cause harmful effects for the baby if taken during pregnancy; [7] however, its use during breastfeeding is generally considered to be safe. [8] It is a non-selective beta blocker which works by blocking β-adrenergic receptors. [2] Propranolol was patented in 1962 and approved for medical use in 1964. [9]
Bisoprolol, sold under the brand name Zebeta among others, is a beta blocker which is selective for the beta-1 receptor [7] and used for cardiovascular diseases, [7] including tachyarrhythmias, high blood pressure, angina, and heart failure. [7] [8] It is taken by mouth. [7]
The Cleveland Clinic classified beta blockers into two categories, cardioselective and nonselective, according to its website. The latter is for medicines that block the B1 receptors found in the ...
Dichloroisoprenaline (DCI), also known as dichloroisoproterenol, was the first beta blocker ever to be developed. It is non-selective for the β 1 -adrenergic and β 2 -adrenergic receptors . DCI has low potency and acts as a partial agonist / antagonist at these receptors .
Beta blockers vary in their lipophilicity (fat solubility) and in turn in their ability to cross the blood–brain barrier and exert effects in the central nervous system. [76] Beta blockers with greater blood–brain barrier permeability can have both neuropsychiatric therapeutic benefits and side effects, as well as adverse cognitive effects ...
Labetalol is often classified as a beta blocker with low lipophilicity and hence lower potential for crossing the blood–brain barrier and blood–placenta barrier. [ 17 ] [ 29 ] [ 30 ] This in turn may result in fewer effects in the central nervous system as well as a lower risk of neuropsychiatric side effects. [ 17 ]
Pronethalol (also known as nethalide or compound 38,174; trade name Alderlin) was an early non-selective beta blocker clinical candidate. It was the first beta blocker to be developed by James Black and associates at Imperial Chemical Industries, and the first to enter clinical use, in November 1963.