 | |
| Names | |
|---|---|
| Preferred IUPAC name 4-(2-{[2-Hydroxy-3-(3-methylphenoxy)propyl]amino}ethoxy)benzamide | |
| Identifiers | |
3D model (JSmol) | |
| ChemSpider | |
| ECHA InfoCard | 100.048.877 |
PubChem CID | |
| UNII | |
CompTox Dashboard (EPA) | |
| |
| |
| Properties | |
| C19H24N2O4 | |
| Molar mass | 344.411 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 | |
Tolamolol is a beta adrenergic receptor antagonist. [1]
Beta blockers, also spelled β-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.
Propranolol, sold under the brand name Inderal among others, is a medication of the beta blocker class. It is used to treat high blood pressure, a number of types of irregular heart rate, thyrotoxicosis, capillary hemangiomas, performance anxiety, and essential tremors, as well to prevent migraine headaches, and to prevent further heart problems in those with angina or previous heart attacks. It can be taken by mouth or by injection into a vein. The formulation that is taken by mouth comes in short-acting and long-acting versions. Propranolol appears in the blood after 30 minutes and has a maximum effect between 60 and 90 minutes when taken by mouth.
In pharmacology, an inverse agonist is a drug that binds to the same receptor as an agonist but induces a pharmacological response opposite to that of the agonist.
Tachykinin peptides are one of the largest families of neuropeptides, found from amphibians to mammals. They were so named due to their ability to rapidly induce contraction of gut tissue. The tachykinin family is characterized by a common C-terminal sequence, Phe-X-Gly-Leu-Met-NH2, where X is either an Aromatic or an Aliphatic amino acid. The genes that produce tachykinins encode precursor proteins called preprotachykinins, which are chopped apart into smaller peptides by posttranslational proteolytic processing. The genes also code for multiple splice forms that are made up of different sets of peptides.
Bisoprolol, marketed under the tradename Concor among others, is a beta blocker medication most commonly used for heart diseases. This specifically includes high blood pressure, chest pain from not enough blood flow to the heart, and heart failure. It is taken by mouth.
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.
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.
A sympatholytic drug is a medication that opposes the downstream effects of postganglionic nerve firing in effector organs innervated by the sympathetic nervous system (SNS). They are indicated for various functions; for example, they may be used as antihypertensives. They are also used to treat anxiety, such as generalized anxiety disorder, panic disorder and PTSD.
Cyanopindolol is a drug related to pindolol which acts as both a β1 adrenoceptor antagonist and a 5-HT1A receptor antagonist. Its radiolabelled derivative iodocyanopindolol has been widely used in mapping the distribution of beta adrenoreceptors in the body.
Iodocyanopindolol (INN) is a drug related to pindolol which acts as both a β1 adrenoreceptor antagonist and a 5-HT1A receptor antagonist. Its 125I radiolabelled derivative has been widely used in mapping the distribution of beta adrenoreceptors in the body.
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.
ZK-93426 (ethyl-5-isopropoxy-4-methyl-beta-carboline-3-carboxylate) is a drug from the beta-carboline family. It acts as a weak partial inverse agonist of benzodiazepine receptors, meaning that it causes the opposite effects to the benzodiazepine class of drugs and has anxiogenic properties, although unlike most benzodiazepine antagonists it is not a convulsant and actually has weak anticonvulsant effects. In human tests it produced alertness, restlessness and feelings of apprehension, and reversed the effect of the benzodiazepine lormetazepam. It was also shown to produce nootropic effects and increased release of acetylcholine.
Isamoltane (CGP-361A) is a drug used in scientific research. It acts as an antagonist at the β-adrenergic, 5-HT1A, and 5-HT1B receptors. It has about five times the potency for the 5-HT1B receptor over the 5-HT1A receptor. It has anxiolytic effects in rodents.
(–)-2β-Carbomethoxy-3β-(4-bromophenyl)tropane is a semi-synthetic alkaloid in the phenyltropane group of psychostimulant compounds. First publicized in the 1990s, it has not been used enough to have gained a fully established profile. RTI-51 can be expected to have properties lying somewhere in between RTI-31 and RTI-55. Importantly it has a ratio of monoamine reuptake inhibition of D > S > N which is an unusual balance of effects not produced by other commonly used compounds. It has been used in its 76Br radiolabelled form to map the distribution of dopamine transporters in the brain.
Brefonalol is a beta-adrenergic antagonist that reduces heart frequency and blood pressure and dilates blood vessels. It has been studied in around 1990, but is not known to be marketed as of 2021.
Falintolol is a beta-adrenergic receptor antagonist.
Sulfinalol is a beta adrenergic receptor antagonist.
Hydroxycarteolol is a beta blocker and metabolite of carteolol.
Beclometasone/formoterol/glycopyrronium, sold under the brand name Trimbow among others, is an inhalable fixed-dose combination medication for the treatment of chronic obstructive pulmonary disease (COPD). It contains beclometasone dipropionate, formoterol fumarate dihydrate, and glycopyrronium bromide.
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