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Drug-Receptor Interaction: Agonist01:25

Drug-Receptor Interaction: Agonist

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Agonists are drugs that interact with specific receptors in the body to produce a biological response. When an agonist binds to a receptor, it activates or enhances the receptor's function, leading to physiological effects. The interaction between agonist drugs and receptors is crucial for their therapeutic action in various medical treatments.
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Adrenergic Agonists: Direct-Acting Agents01:30

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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.
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Endothelins (ETs) are potent vasoactive peptides critical in the human body's various physiological and pathological processes. One of the most promising therapeutic strategies for treating pulmonary arterial hypertension (PAH) involves counteracting the effects of these endothelins using a class of drugs known as endothelin receptor antagonists.
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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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Direct-Acting Cholinergic Agonists: Pharmacological Actions00:59

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Direct-acting cholinergic agonists exert their pharmacological actions by mimicking the effects of acetylcholine on postsynaptic muscarinic receptors to generate parasympathetic responses. These agents elicit a range of physiological responses, including cardiovascular effects. For example, activation of muscarinic receptors induces bradycardia, decreased cardiac output, reduced peripheral resistance, and consequent hypotension. In the eye, stimulation of M3 receptors leads to smooth muscle...
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Adrenergic Agonists: Therapeutic Classification01:18

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Adrenergic agonists can be classified based on their therapeutic uses and mechanisms of action. They serve various purposes in clinical applications.
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Related Experiment Video

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Parallel Interrogation of β-Arrestin2 Recruitment for Ligand Screening on a GPCR-Wide Scale using PRESTO-Tango Assay
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TAAR Agonists.

Zhengrong Xu1,2,3, Qian Li4,5

  • 1Collaborative Innovation Center for Brain Science, Department of Anatomy and Physiology, Shanghai Jiao Tong University School of Medicine, Shanghai, 200025, China.

Cellular and Molecular Neurobiology
|December 19, 2019
PubMed
Summary
This summary is machine-generated.

Trace amine-associated receptors (TAARs) are GPCRs that detect amines. This review covers TAAR agonists, their structures, biosynthesis, and roles in brain and olfactory systems.

Keywords:
AgonistG protein-coupled receptor (GPCR)Olfactory receptorTrace amine-associated receptor (TAAR)Trace aminesVolatile amines

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Area of Science:

  • Neuroscience
  • Biochemistry
  • Pharmacology

Background:

  • Trace amine-associated receptors (TAARs) are a conserved family of G protein-coupled receptors (GPCRs) in vertebrates.
  • TAAR1, primarily in the brain, detects trace amines and is activated by amphetamines, influencing monoaminergic systems.
  • Olfactory TAARs, found in the olfactory system, recognize volatile and water-soluble amines, including those derived from amino acids and ethological odors.

Purpose of the Study:

  • To provide a comprehensive review of trace amine-associated receptor (TAAR) agonists.
  • To detail the structures, biosynthesis pathways, and functions of various TAAR agonists.
  • To consolidate current knowledge on TAARs, bridging their roles in neurological and olfactory processes.

Main Methods:

  • Literature review and synthesis of existing research on TAAR agonists.
  • Analysis of structural, biochemical, and functional data pertaining to TAARs and their ligands.
  • Compilation of information on the origins and biological relevance of TAAR-activating compounds.

Main Results:

  • TAARs represent a diverse class of receptors with significant roles in both central nervous system function and sensory perception.
  • Agonists for TAARs include endogenous amines, synthetic compounds, and environmental odorants.
  • The identified agonists exhibit varied structures and are synthesized through distinct biochemical pathways, highlighting the versatility of TAAR signaling.

Conclusions:

  • TAARs and their agonists are crucial mediators of physiological and behavioral processes.
  • Understanding TAAR agonist pharmacology is vital for potential therapeutic interventions targeting neurological and olfactory disorders.
  • This review underscores the broad significance of TAARs in vertebrate biology, from neurotransmission to chemosensation.