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| Names | |
|---|---|
| IUPAC name 8-[3-(tert-Butylamino)-2-hydroxypropoxy]-5-methylchromen-2-one | |
| Identifiers | |
3D model (JSmol) | |
| ChEMBL | |
| ChemSpider | |
| KEGG | |
| MeSH | C024221 |
PubChem CID | |
| UNII | |
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| Properties | |
| C17H23NO4 | |
| Molar mass | 305.374 g·mol−1 |
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa). | |
| Infobox references | |
Bucumolol is a beta-adrenergic antagonist. [1]
Beta blockers are a class of medications that are predominantly used to manage abnormal heart rhythms, and to protect the heart from a second heart attack after a first heart attack. They are also widely used to treat high blood pressure (hypertension), although they are no longer the first choice for initial treatment of most patients.
Penbutolol is a medication in the class of beta blockers, used in the treatment of high blood pressure. Penbutolol is able to bind to both beta-1 adrenergic receptors and beta-2 adrenergic receptors, thus making it a non-selective β blocker. Penbutolol is a sympathomimetic drug with properties allowing it to act as a partial agonist at β adrenergic receptors.
The beta-1 adrenergic receptor, also known as ADRB1, is a beta-adrenergic receptor, and also denotes the human gene encoding it. It is a G-protein coupled receptor associated with the Gs heterotrimeric G-protein and is expressed predominantly in cardiac tissue.
The beta-2 adrenergic receptor, also known as ADRB2, is a cell membrane-spanning beta-adrenergic receptor that interacts with (binds) epinephrine, a hormone and neurotransmitter whose signaling, via adenylate cyclase stimulation through trimeric Gs proteins, increased cAMP, and downstream L-type calcium channel interaction, mediates physiologic responses such as smooth muscle relaxation and bronchodilation.
An adrenergic antagonist is a drug that inhibits the function of adrenergic receptors. There are five adrenergic receptors, which are divided into two groups. The first group of receptors are the beta (β) adrenergic receptors. There are β1, β2, and β3 receptors. The second group contains the alpha (α) adrenoreceptors. There are only α1 and α2 receptors. Adrenergic receptors are located near the heart, kidneys, lungs, and gastrointestinal tract. There are also α-adreno receptors that are located on vascular smooth muscle.
Carazolol is a high affinity antagonist/partial inverse agonist of the β-adrenergic receptor.
The beta-3 adrenergic receptor, also known as ADRB3, is a beta-adrenergic receptor, and also denotes the human gene encoding it.
Denopamine (INN) is a cardiotonic drug which acts as a β1 adrenergic receptor agonist. It is used in the treatment of angina and may also have potential uses in the treatment of congestive heart failure and for clearing pulmonary oedema. It is marketed in Japan under the brand name Kalgut (カルグート) and available as tablets of 5 and 10 mg, and 5% fine granules.
Beta adrenergic agonists or beta agonists are medications that relax muscles of the airways, which widen the airways and result in easier breathing. They are a class of sympathomimetic agents which act upon the beta adrenoceptors. In general, pure beta-adrenergic agonists have the opposite function of beta blockers. Beta adrenoreceptor agonist ligands mimic the action of epinephrine and norepinephrine signaling in the heart, lungs, and smooth muscle tissue, with epinephrine expressing the highest affinity. The activation of β1, β2 and β3 activates the enzyme, adenylate cyclase. This, in turn, leads to the activation of the secondary messenger cyclic adenosine monophosphate (cAMP), cAMP then activates protein kinase A (PKA) which phosphorylates target proteins, ultimately inducing smooth muscle relaxation and contraction of the cardiac tissue.
Beta1-adrenergic agonists, also known as Beta1-adrenergic receptor agonists, are a class of drugs that bind selectively to the beta-1 adrenergic receptor. As a result, they act more selectively upon the heart. Beta-adrenoceptors typically bind to norepinephrine release by sympathetic adrenergic nerves and to circulating epinephrine. The effect of B-adrenoceptors is cardiac stimulation, such as increased heart rate, heart contractility, heart conduction velocity and heart relaxation.
ICI-118,551 is a selective β2 adrenergic receptor (adrenoreceptor) antagonist or beta blocker. ICI binds to the β2 subtype with at least 100 times greater affinity than β1 or β3, the two other known subtypes of the beta adrenoceptor. The compound was developed by Imperial Chemical Industries, which was acquired by AkzoNobel in 2008.
SR 59230A is a selective antagonist of the beta-3 adrenergic receptor, but was subsequently shown to also act at α1 adrenoceptors at high doses. It has been shown to block the hyperthermia produced by MDMA in animal studies.
Dihydroalprenolol (DHA) is a hydrogenated alprenolol derivative that acts as a beta-adrenergic blocker. When the extra hydrogen atoms are tritium, it is a radiolabeled form of alprenolol, which is used to label beta-adrenergic receptors for isolation.
Cloranolol (Tobanum) is a beta blocker.
Bornaprolol is a beta-adrenergic antagonist.
Cetamolol is a beta adrenergic antagonist, a b1-adrenergic blocker.
Falintolol is a beta-adrenergic receptor antagonist.
Indenolol is a beta-adrenergic blocker.
Nadoxolol is an antiarrhythmic agent, chemically related in structure to beta-adrenergic receptor blocker drugs such as propranolol.
Soquinolol is a beta adrenergic receptor antagonist.
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