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Related Concept Videos

Antipsychotic Drugs: Typical and Atypical Agents01:21

Antipsychotic Drugs: Typical and Atypical Agents

Antipsychotic drugs are classified into first-generation (typical) drugs including phenothiazines; and second-generation (atypical) drugs. Chlorpromazine hydrochloride (Thorazine), a phenothiazine derivative, broadly impacts the central, autonomic, and endocrine systems. This drug, along with typical agents like haloperidol (Haldol), primarily works by antagonizing D2 receptors, thus reducing dopaminergic neurotransmission. However, typical antipsychotics can cause side effects such as sedation...
Parkinson's Disease: Treatment01:24

Parkinson's Disease: Treatment

Neurodegenerative disorders, such as Parkinson's Disease (PD), involve the gradual and irreversible destruction of neurons in particular brain areas. These disorders exhibit standard features like proteinopathies, selective vulnerability of some neurons, and an interaction of intrinsic properties, genetics, and environmental influences in neural injury.
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Antidepressant Drugs: MAOIs and Other Agents01:23

Antidepressant Drugs: MAOIs and Other Agents

Atypical antidepressants, including bupropion (Wellbutrin), mirtazapine (Remeron), nefazodone (Serzone), trazodone (Desyrel), and vilazodone (Viibryd), offer unique mechanisms of action. Bupropion weakly inhibits dopamine and norepinephrine reuptake, aiding depression treatment and smoking cessation, with a low risk of sexual dysfunction. Mirtazapine enhances serotonin and norepinephrine neurotransmission, leading to sedation, increased appetite, and weight gain. As a result, it helps treat...
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Drugs Affecting Neurotransmitter Synthesis

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Adrenergic Agonists: Chemistry and Structure-Activity Relationship01:16

Adrenergic Agonists: Chemistry and Structure-Activity Relationship

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Chemotherapy-Induced Nausea and Vomiting: Dopamine Receptor Antagonists

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Related Experiment Video

Updated: Jun 9, 2026

Rating L-DOPA-Induced Dyskinesias in the Unilaterally 6-OHDA-Lesioned Rat Model of Parkinson's Disease
06:45

Rating L-DOPA-Induced Dyskinesias in the Unilaterally 6-OHDA-Lesioned Rat Model of Parkinson's Disease

Published on: October 4, 2021

6-Alkoxyisoindolin-1-one based dopamine D2 partial agonists as potential antipsychotics.

David A Favor1, James J Powers, Andrew D White

  • 1Pfizer Global Research and Development, Michigan Laboratories, 2800 Plymouth Road, Ann Arbor, MI 48105, United States. dafavor@gmail.com

Bioorganic & Medicinal Chemistry Letters
|August 31, 2010
PubMed
Summary

New antipsychotic drug candidates, 6-alkoxyisoindolin-1-ones, show promising pharmacological activity. These compounds exhibit dual D(2) and serotonin receptor modulation for potential use in treating psychosis.

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A Direct, Regioselective and Atom-Economical Synthesis of 3-Aroyl-N-hydroxy-5-nitroindoles by Cycloaddition of 4-Nitronitrosobenzene with Alkynones
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The 6-hydroxydopamine Rat Model of Parkinson's Disease
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The 6-hydroxydopamine Rat Model of Parkinson's Disease

Published on: October 27, 2021

Related Experiment Videos

Last Updated: Jun 9, 2026

Rating L-DOPA-Induced Dyskinesias in the Unilaterally 6-OHDA-Lesioned Rat Model of Parkinson's Disease
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Rating L-DOPA-Induced Dyskinesias in the Unilaterally 6-OHDA-Lesioned Rat Model of Parkinson's Disease

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A Direct, Regioselective and Atom-Economical Synthesis of 3-Aroyl-N-hydroxy-5-nitroindoles by Cycloaddition of 4-Nitronitrosobenzene with Alkynones
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The 6-hydroxydopamine Rat Model of Parkinson's Disease
08:10

The 6-hydroxydopamine Rat Model of Parkinson's Disease

Published on: October 27, 2021

Area of Science:

  • Medicinal Chemistry
  • Neuropharmacology
  • Drug Discovery

Background:

  • Schizophrenia and related psychoses represent significant unmet medical needs.
  • Current antipsychotic treatments often suffer from limited efficacy and burdensome side effects.
  • Novel therapeutic agents with improved pharmacological profiles are crucial for advancing psychiatric care.

Purpose of the Study:

  • To synthesize and characterize a novel series of 6-alkoxyisoindolin-1-one compounds.
  • To evaluate the in vitro and in vivo pharmacological properties of these compounds as potential antipsychotics.
  • To explore the structure-activity relationships within this chemical class.

Main Methods:

  • Chemical synthesis of 6-alkoxyisoindolin-1-one derivatives.
  • In vitro receptor binding and functional assays (D2, 5-HT1A, 5-HT2A).
  • In vivo behavioral models to assess antipsychotic-like activity and potency.

Main Results:

  • The synthesized compounds demonstrated a unique 'magic shotgun' pharmacological profile.
  • In vitro results showed D(2) partial agonism (30-55%), 5-HT(1A) partial agonism (60-90%), and 5-HT(2A) antagonism.
  • Selected compounds exhibited significant in vivo antipsychotic activity and potency in preclinical models.

Conclusions:

  • The 6-alkoxyisoindolin-1-one series represents a promising new class of potential antipsychotic agents.
  • The observed pharmacological profile suggests a favorable balance of efficacy and tolerability.
  • Further investigation is warranted to optimize these compounds for clinical development.