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Related Concept Videos

G Protein-coupled Receptors01:15

G Protein-coupled Receptors

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G Protein-Coupled Receptors or GPCRs are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to sensory stimuli such as light, odors, hormones, cytokines, or neurotransmitters.
GPCRs are also called heptahelical, 7TM, or serpentine receptors, and consist of seven (H1-H7) transmembrane alpha-helices that span the bilayer to form a cylindrical core. The transmembrane helices are connected by three extracellular loops and three...
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Adrenergic Agonists: Chemistry and Structure-Activity Relationship01:16

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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.
Separation of...
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Indirect-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship01:29

Indirect-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship

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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.
Reversible inhibitors display short to medium durations of action. Short-acting agents include simple alcohols with...
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Structure-Activity Relationships and Drug Design01:28

Structure-Activity Relationships and Drug Design

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Drug design is a dynamic field that involves discovering and developing new medications based on specific biological targets. This process heavily relies on structure-activity relationships (SAR) and quantitative structure-activity relationships (QSAR) to guide the design and optimization of efficient drugs.
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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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Cholinergic Antagonists: Chemistry and Structure-Activity Relationship01:29

Cholinergic Antagonists: Chemistry and Structure-Activity Relationship

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Cholinergic antagonists bind to cholinergic receptors and limit the effects of acetylcholine and other cholinergic agonists. Based on the specific cholinergic receptor affinity, these antagonists are classified as muscarinic or nicotinic. Anticholinergics interrupt parasympathetic innervations while sympathetic innervations remain uninterrupted. Muscarinic antagonists are also called 'muscarinic antagonists', 'antimuscarinics', or 'parasympatholytics'. Nicotinic...
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Quantitative Structure-Activity Relationship, Activity Prediction, and Molecular Dynamics of Non-nucleotide Reverse Transcriptase Inhibitors
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Thienopyrimidine Derivatives as GPR55 Receptor Antagonists: Insight into Structure-Activity Relationship.

Laura Figuerola-Asencio1, Paula Morales1, Pingwei Zhao2

  • 1Instituto de Química Médica, Consejo Superior de Investigaciones Científicas, 28006Madrid, Spain.

ACS Medicinal Chemistry Letters
|January 19, 2023
PubMed
Summary
This summary is machine-generated.

Researchers developed novel thienopyrimidine compounds targeting the G-protein coupled receptor 55 (GPR55). These potent and selective GPR55 antagonists offer new tools for exploring the receptor

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Area of Science:

  • Pharmacology
  • Medicinal Chemistry
  • Molecular Biology

Background:

  • G-protein coupled receptor 55 (GPR55) is an orphan receptor implicated in diverse pathophysiological processes.
  • A scarcity of potent and selective GPR55 ligands hinders comprehensive research into its functions.
  • Existing non-cannabinoid GPR55 ligands are limited, necessitating the development of novel chemical entities.

Purpose of the Study:

  • To synthesize and characterize novel thienopyrimidine derivatives as potential GPR55 ligands.
  • To evaluate the antagonist activity and selectivity of these compounds against GPR55.
  • To provide new chemical tools for investigating GPR55's role in biological systems.

Main Methods:

  • High-throughput screening identified ML192 as a starting point for scaffold-based drug design.
  • Synthesis of a novel series of thienopyrimidine compounds.
  • Functional assessment of GPR55 activity using beta-arrestin recruitment assays in CHO cells overexpressing human GPR55.
  • Evaluation of selectivity against CB1 and CB2 cannabinoid receptors.

Main Results:

  • Several synthesized thienopyrimidine derivatives demonstrated significant GPR55 antagonist activity.
  • The identified compounds exhibited functional efficacy in blocking GPR55 signaling.
  • Selectivity profiling confirmed reduced activity against CB1 and CB2 cannabinoid receptors.
  • The thienopyrimidine scaffold proved amenable to developing potent and selective GPR55 antagonists.

Conclusions:

  • Novel thienopyrimidine derivatives were successfully synthesized and validated as potent GPR55 antagonists.
  • These compounds represent valuable pharmacological tools for further GPR55 research.
  • The findings contribute to the development of targeted therapeutics for GPR55-mediated conditions.
  • This study expands the chemical space of known GPR55 ligands.