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Related Concept Videos

Direct-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship01:22

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Cholinergic agonists or cholinomimetics mimic the action of acetylcholine to stimulate the parasympathetic nervous system. They are categorized into direct-acting and indirect-acting agents. The direct-acting cholinergic drugs induce the parasympathetic response by directly binding to the muscarinic or nicotine receptors. In comparison, the indirect-acting cholinergic drugs prevent acetylcholine hydrolysis, indirectly contributing to the extended parasympathetic response.
The direct-acting...
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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.
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Indirect-Acting Cholinergic Agonists: Mechanism of Action01:18

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Indirect-acting cholinergic agonists work by interacting with an enzyme called acetylcholinesterase (AChE) in the synaptic cleft. They can be reversible or irreversible inhibitors and have different effects on the enzyme.
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Indirect-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship01:29

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Indirect-acting cholinergic agonists are agents that interact with the acetylcholinesterase enzyme in the synaptic cleft, preventing the breakdown of acetylcholine into choline and acetate. Consequently, the concentration of acetylcholine in the synaptic cleft increases. These agonists can be classified into reversible and irreversible inhibitors based on their duration of action.
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Adrenergic Agonists: Indirect-Acting Agents01:25

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Indirect-acting adrenergic agonists potentiate the effects of endogenous catecholamines through different mechanisms without directly binding to adrenoceptors.
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Direct-Acting Cholinergic Agonists: Pharmacokinetics01:31

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Direct-acting cholinergic agonists, such as synthetic choline esters and naturally occurring alkaloids, exert their effects by enhancing the actions of acetylcholine and stimulating the parasympathetic nervous system. Synthetic choline esters share structural similarities with acetylcholine. For example, they have a positively charged quaternary ammonium or onium group, contributing to their hydrophilic characteristics. As a result, they are poorly absorbed in the body through oral...
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N-Acylethanolamines Bind to SIRT6.

Minna Rahnasto-Rilla1,2, Tarja Kokkola2, Elina Jarho2

  • 1Bioanalytical Chemistry and Drug Screening Centre, Laboratory of Clinical Investigation, National Institute on Aging, National Institutes of Health, Suite 100, Biomedical Research Center, 251 Bayview Boulevard, Baltimore, MD, 21224-6825, USA.

Chembiochem : a European Journal of Chemical Biology
|November 27, 2015
PubMed
Summary
This summary is machine-generated.

N-acylethanolamines (NAEs) enhance Sirtuin 6 (SIRT6) enzyme activity, with oleoylethanolamide showing the most potent effect. Flavonoids quercetin and luteolin exhibit dual roles, inhibiting and stimulating SIRT6 activity at different concentrations.

Keywords:
enzymesethanolamidesnatural productsquercetinsirtuins

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Area of Science:

  • Biochemistry
  • Molecular Biology
  • Aging Research

Background:

  • Sirtuin 6 (SIRT6) is an NAD+-dependent histone deacetylase implicated in aging pathways.
  • SIRT6 exhibits dual enzymatic activity, deacetylating histones and hydrolyzing long-chain fatty acyl groups.
  • Fatty acids are known to modulate SIRT6 catalytic activity.

Purpose of the Study:

  • To investigate the regulatory effects of N-acylethanolamines (NAEs), quercetin, and luteolin on SIRT6 activity.
  • To determine the specific modulatory mechanisms of these compounds on SIRT6 function.

Main Methods:

  • Enzyme activity assays were performed to measure SIRT6 modulation.
  • Dose-response experiments were conducted to determine EC50 and IC50 values.
  • A series of NAEs, quercetin, and luteolin were tested for their effects on SIRT6.

Main Results:

  • NAEs significantly increased SIRT6 activity, with oleoylethanolamide being the most effective (EC50 = 3.1 µM).
  • Quercetin and luteolin displayed dual functionality, inhibiting SIRT6 at low concentrations (IC50 = 24 µM and 2 µM, respectively) and stimulating it at higher concentrations (EC50 = 990 µM and 270 µM, respectively).

Conclusions:

  • NAEs represent potent activators of SIRT6 enzymatic activity.
  • Quercetin and luteolin act as dual modulators of SIRT6, offering potential for targeted therapeutic intervention.
  • These findings expand the understanding of SIRT6 regulation by small molecules.