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Related Concept Videos

Adrenergic Agonists: Direct-Acting Agents01:30

Adrenergic Agonists: Direct-Acting Agents

Drugs that mimic the action of endogenous catecholamines like noradrenaline and adrenaline are called adrenergic agonists or sympathomimetics. Based on their mechanism of action, sympathomimetics can be classified as direct-, indirect-, or mixed-acting sympathomimetics. Direct-acting adrenergic agonists activate adrenoceptors without affecting presynaptic neurons, making them independent of neuronal catecholamine-depleting agents like reserpine and guanethidine.
These agents can be classified...
Adrenergic Agonists: Mixed-Action Agents01:28

Adrenergic Agonists: Mixed-Action Agents

Mixed-action adrenergic agonists, like ephedrine and pseudoephedrine, directly and indirectly affect adrenergic receptors. These agents stimulate adrenoceptors and indirectly release stored neurotransmitters, amplifying the adrenergic response.
Ephedrine and pseudoephedrine lack a catecholamine group, making them less susceptible to degradation by metabolic enzymes. They have increased oral bioavailability and lipophilicity, resulting in a longer duration of action. Their response is reduced by...
Adrenergic Agonists: Chemistry and Structure-Activity Relationship01:16

Adrenergic Agonists: Chemistry and Structure-Activity Relationship

Adrenergic agonists' structure-activity relationship (SAR) determines their selectivity and efficacy. These agonists comprise a phenylethylamine moiety with an aromatic ring and an ethylamine side chain.
Aromatic ring substitutions: Substituting the aromatic ring with –OH groups at positions 3 and 4 yields catecholamines (e.g., epinephrine), which have a high affinity for adrenoceptors. Hydrogen bonding between –OH groups and receptors enhances adrenergic activity.
Separation of the aromatic...
Adrenergic Antagonists: Chemistry and Classification of ɑ-Receptor Blockers01:17

Adrenergic Antagonists: Chemistry and Classification of ɑ-Receptor Blockers

Adrenergic antagonists, or sympatholytics, inhibit adrenoceptor activation driven by catecholamines or agonists. Based on their adrenoceptor specificity, adrenergic blockers can be categorized into two primary groups: α-adrenergic blockers (α-blockers) and β-adrenergic blockers (β-blockers). α-blockers interact with α1 and α2 subtypes of α-adrenoceptors.
Nonselective α-blockers: Nonselective α-blockers contain haloalkylamine or imidazoline moieties. Phenoxybenzamine, with a haloalkylamine...
Adrenergic Antagonists: Pharmacological Actions of ɑ-Receptor Blockers01:22

Adrenergic Antagonists: Pharmacological Actions of ɑ-Receptor Blockers

α-Adrenergic antagonists, known as α-blockers, exert their effects by inhibiting α-adrenoceptors, leading to specific physiological actions. α1-blockers and α2-blockers have distinct pharmacological actions and therapeutic applications.
α1-blockers: These drugs inhibit α1-adrenoceptors on smooth muscle cells, resulting in vasodilation. This vasodilation lowers blood pressure, making α1-blockers valuable in treating hypertension. Additionally, α1-blockers effectively address urinary obstruction...
Adrenergic Antagonists: ɑ and β-Receptor Blockers01:31

Adrenergic Antagonists: ɑ and β-Receptor Blockers

Third-generation β-blockers, such as labetalol and carvedilol, represent a significant advancement in managing cardiovascular conditions. Unlike conventional β-blockers, which can induce peripheral vasoconstriction, third-generation drugs block α1 adrenoceptors. This promotes vasodilation through several mechanisms, such as increased nitric oxide production, inhibition of calcium ion entry, opening of potassium ion channels, and antioxidant action. Labetalol, for instance, is clinically...

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Lignans isolated from valerian: identification and characterization of a new olivil derivative with partial agonistic

Britta Schumacher1, Silke Scholle, Josef Hölzl

  • 1Pharmaceutical Institute Poppelsdorf, University of Bonn, Germany.

Journal of Natural Products
|October 26, 2002
PubMed
Summary

Valerian root extract contains novel lignans, including a unique adenosine receptor agonist. These compounds may contribute to valerian

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Green Synthesis, Characterization, Encapsulation, and Measurement of the Release Potential of Novel Alkali Lignin Micro-/Submicron Particles
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Green Synthesis, Characterization, Encapsulation, and Measurement of the Release Potential of Novel Alkali Lignin Micro-/Submicron Particles

Published on: March 1, 2024

Area of Science:

  • Phytochemistry
  • Pharmacology
  • Natural Products Chemistry

Background:

  • Valeriana officinalis (valerian) is a medicinal plant with a long history of use.
  • Lignans are a class of phenolic compounds found in plants, known for diverse biological activities.
  • Understanding the chemical constituents of valerian is crucial for elucidating its pharmacological effects.

Purpose of the Study:

  • To identify and characterize lignans from Valeriana officinalis root extract.
  • To investigate the potential pharmacological activity of these lignans by examining their binding affinities at central nervous system receptors.
  • To explore the contribution of identified lignans to the overall medicinal properties of valerian.

Main Methods:

  • Methanolic extraction of Valeriana officinalis roots.
  • Isolation and structural elucidation of lignan compounds using chromatographic and spectroscopic techniques.
  • Radioligand binding assays to assess the affinity of lignans for GABA(A), benzodiazepine, 5-HT(1A), adenosine A(1), and A(2A) receptors.

Main Results:

  • Identified eight lignans, including two novel natural products: 4'-O-beta-D-glucosyl-9-O-(6' '-deoxysaccharosyl)olivil (4) and berchemol-4'-O-beta-D-glucoside (5).
  • Compound 4 demonstrated partial agonistic activity at rat and human A(1) adenosine receptors with affinity in the low micromolar to submicromolar range.
  • This study identified the first non-nucleoside adenosine receptor agonist (lignan 4) structurally unrelated to adenosine.

Conclusions:

  • The lignan profile of Valeriana officinalis root extract has been further characterized, revealing new natural compounds.
  • Novel lignan 4 exhibits significant activity at adenosine A(1) receptors, suggesting a potential mechanism for valerian's effects.
  • These findings contribute to the understanding of valerian's phytochemistry and pharmacology, particularly concerning its interaction with the central nervous system.