beta-1 adrenergic receptors: nootropics and compounds | sci-wiki

Atenolol

Atenolol is a beta-1 selective beta blocker, a cardiovascular drug that blocks the beta-1 adrenergic receptors of the heart. It is used to treat high blood pressure, angina, and certain irregular heart rhythms, and historically after heart attacks. Developed by Imperial Chemical Industries in the 1970s, it is water-soluble and crosses into the brain poorly, which tends to limit central nervous system side effects; many guidelines no longer list it as a first-choice treatment for uncomplicated high blood pressure.

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Beta-Blocker

Bisoprolol

Bisoprolol is a highly beta-1 selective adrenergic receptor antagonist, among the most cardioselective of the beta-blockers, taken once daily for hypertension, angina, certain arrhythmias and chronic heart failure. Its strong preference for cardiac beta-1 over pulmonary beta-2 receptors improves tolerability and permits cautious use even in many patients with coexisting airway disease. In the landmark CIBIS-II trial it reduced all-cause mortality and sudden cardiac death in stable heart failure with reduced ejection fraction, and the later CIBIS-III trial showed that beginning treatment with bisoprolol before an ACE inhibitor is a viable strategy. Individual-patient meta-analyses confirm the survival benefit of beta-blockade in patients in sinus rhythm while indicating attenuated benefit when atrial fibrillation coexists; bisoprolol appears on the World Health Organization list of essential medicines.

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Beta-Blocker

Metoprolol

Metoprolol is a cardioselective beta-1 adrenergic antagonist that slows heart rate and reduces myocardial contractility and workload, lowering blood pressure and cardiac oxygen demand. It is among the most rigorously validated beta-blockers: the MERIT-HF trial demonstrated a significant mortality reduction in chronic heart failure, and, as a lipophilic agent, it reduces sudden cardiac death after myocardial infarction, an effect linked to central penetration and preservation of vagal tone. Its limits are equally well documented; the large POISE trial showed that routine perioperative use lowered myocardial infarction but increased stroke and total mortality, tempering enthusiasm for prophylactic beta-blockade. It is also effective for migraine prevention, and its metabolism by the polymorphic enzyme CYP2D6 contributes to marked interindividual variability now addressed by pharmacogenetic guidelines. It is available as the immediate-release tartrate and extended-release succinate salts.

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Beta-Blocker

Metoprolol Succinate

Metoprolol succinate is the extended-release salt form of the cardioselective beta-1 blocker metoprolol, sold under the brand name Toprol-XL. Formulated to release slowly for once-daily dosing, it produces steady round-the-clock blockade of beta-1 adrenergic receptors, slowing the heart and lowering blood pressure. It is used for high blood pressure, angina, and, notably, chronic heart failure, where extended-release metoprolol has been shown to improve survival; it is distinguished from the immediate-release tartrate salt, and the two are not interchangeable.

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