Bufuralol

Last updated
Bufuralol
Bufuralol.svg
Names
Preferred IUPAC name
2-(tert-Butylamino)-1-(7-ethyl-1-benzofuran-2-yl)ethan-1-ol
Other names
2-(tert-Butylamino)-1-(7-ethylbenzofuran-2-yl)ethan-1-ol
2-(tert-Butylamino)-1-(7-ethyl-1-benzofuran-2-yl)ethanol
Identifiers
3D model (JSmol)
ChEMBL
ChemSpider
ECHA InfoCard 100.053.720
PubChem CID
UNII
Properties
C16H23NO2
Molar mass 261.365 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

Bufuralol is a potent beta-adrenoceptor antagonist with partial agonist activity. [1] It is metabolized by CYP2D6. [2]

Partial agonist

In pharmacology, partial agonists are drugs that bind to and activate a given receptor, but have only partial efficacy at the receptor relative to a full agonist. They may also be considered ligands which display both agonistic and antagonistic effects—when both a full agonist and partial agonist are present, the partial agonist actually acts as a competitive antagonist, competing with the full agonist for receptor occupancy and producing a net decrease in the receptor activation observed with the full agonist alone. Clinically, partial agonists can be used to activate receptors to give a desired submaximal response when inadequate amounts of the endogenous ligand are present, or they can reduce the overstimulation of receptors when excess amounts of the endogenous ligand are present.

CYP2D6 protein-coding gene in the species Homo sapiens

Cytochrome P450 2D6 (CYP2D6) is an enzyme that in humans is encoded by the CYP2D6 gene. CYP2D6 is primarily expressed in the liver. It is also highly expressed in areas of the central nervous system, including the substantia nigra.

Most beta blockers are aryloxypropanolamine-based. In this rare exception, the benzofuran oxygen is part of a ring instead of derived from the epichlorohydrin precursor.

Beta blocker class of medications that are particularly used to manage cardiac arrhythmias, and to protect the heart from a second heart attack after a first heart attack

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Epichlorohydrin chemical compound

Epichlorohydrin is an organochlorine compound and an epoxide. Despite its name, it is not a halohydrin. It is a colorless liquid with a pungent, garlic-like odor, moderately soluble in water, but miscible with most polar organic solvents. It is a chiral molecule generally existing as a racemic mixture of right-handed and left-handed enantiomers. Epichlorohydrin is a highly reactive electrophilic compound and is used in the production of glycerol, plastics, epoxy glues and resins, and elastomers.

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Weak interaction the fundamental interaction responsible for beta decay and nuclear fission

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Propranolol beta blocker drug

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Interaction kind of action that occurs as two or more objects have an effect upon one another

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Tazobactam chemical compound

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Isoprenaline chemical compound

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Dicloxacillin chemical compound

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Nebivolol chemical compound

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Cefoxitin chemical compound

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Loreclezole chemical compound

Loreclezole is a sedative and an anticonvulsant which acts as a GABAA receptor positive allosteric modulator. The binding site of loreclezole has been shown experimentally to be shared by valerenic acid, an extract of the root of the valerian plant. Structurally, loreclezole is a triazole derivative. In animal seizure models, loreclezole is protective against pentylenetetrazol seizures but is less active in the maximal electroshock test. In addition, at low, nontoxic doses, the drug has anti-absence activity in a genetic model of generalized absence epilepsy. Consequently, loreclezole has a profile of activity similar to that of benzodiazepines. A potential benzodiazepine-like interaction with GABA receptors is suggested by the observation that the anticonvulsant effects of loreclezole can be reversed by benzodiazepine receptor inverse agonists. The benzodiazepine antagonist flumazenil, however, fails to alter the anticonvulsant activity of loreclezole, indicating that loreclezole is not a benzodiazepine receptor agonist. Using native rat and cloned human GABA-A receptors, loreclezole strongly potentiated GABA-activated chloride current. However, activity of the drug did not require the presence of the γ-subunit and was not blocked by flumazenil, confirming that loreclezole does not interact with the benzodiazepine recognition site.

ZK-93426 chemical compound

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Adimolol (MEN-935) is antihypertensive agent which acts as a non-selective α1-, α2-, and β-adrenergic receptor antagonist.

Levomethadone chemical compound

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Bunitrolol chemical compound

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Butidrine chemical compound

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Ceftolozane/tazobactam Antibiotic

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References

  1. Pringle, TH; Francis, RJ; East, PB; Shanks, RG (1986). "Pharmacodynamic and pharmacokinetic studies on bufuralol in man". British Journal of Clinical Pharmacology. 22 (5): 527–34. doi:10.1111/j.1365-2125.1986.tb02931.x. PMC   1401192 . PMID   2878678.
  2. Flockhart DA (2007). "Drug Interactions: Cytochrome P450 Drug Interaction Table". Indiana University School of Medicine. Retrieved on July 2011