Section Review Central &amp; Peripheral Nervous Systems: New antidepressant agents: Recent pharmacological developments leading to improved efficacy

A series of triazolopyridine derivatives (compounds 2a-l) were synthesized in order to explore the effect of modifications of the alkylpiperazine moiety of trazodone (fragment A) on binding affinity for 5HT2A and alpha1 receptors. All of the synthesized compounds show a decrease of affinity for both 5HT2A and alpha1 receptors, as compared to trazodone, with the exception of compounds 2b,c which bear a methyl group in an alpha position to the aliphatic nitrogen atom N1. These compounds showed a decrease of affinity only for the alpha1 receptor. The stereochemical influence of the piperazine moiety of compound 2c was also evaluated. Enantiomer (S)-2c showed the most significant differences between 5HT2A and alpha1 receptor affinity (IC50 values) and among the corresponding functional properties (pA2 values). Since (S)-2c cannot generate the metabolite 4-(3-chlorophenyl)piperazine this product was selected for further pharmacological studies.

show abstract

Effect of Modifications of the Alkylpiperazine Moiety of Trazodone on 5HT_2Aand α₁Receptor Binding Affinity

Giannangeli

Cazzolla

Luparini

et al. 1999

J. Med. Chem.

View full text Add to dashboard Cite

show abstract

Untitled

Goodnick¹,

Jiménez²,

Kumar³

1997

Annals of Clinical Psychiatry

View full text Add to dashboard Cite

show abstract

Selective Serotonin Reuptake Inhibitors: Implications for Advanced Nursing Practice

Britton

1999

Journal of the American Academy of Nurse Practitioners

View full text Add to dashboard Cite

The efficacy of SSRIs in treating depression as compared to other classes of antidepressants is well documented. There is a growing body of knowledge documenting differences and similarities among these drugs, including half-life elimination, side effects, drug interactions, dosing and cost. These data must be reviewed before prescribing. Providers must take caution when giving SSRIs to patients who have been on other antipsychotics, especially MAO inhibitors, elderly patients, patients who are pregnant, and patients on type 1C antiarrhythmia agents.

show abstract

scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.

Contact Info

customersupport@researchsolutions.com

10624 S. Eastern Ave., Ste. A-614

Henderson, NV 89052, USA

This site is protected by reCAPTCHA and the Google Privacy Policy and Terms of Service apply.

Blog Terms and Conditions API Terms Privacy Policy Contact Cookie Preferences Do Not Sell or Share My Personal Information

Made with 💙 for researchers

Part of the Research Solutions Family.

Section Review Central & Peripheral Nervous Systems: New antidepressant agents: Recent pharmacological developments leading to improved efficacy

Cited by 5 publications

References 16 publications

Effect of Modifications of the Alkylpiperazine Moiety of Trazodone on 5HT_2Aand α₁Receptor Binding Affinity

Effect of Modifications of the Alkylpiperazine Moiety of Trazodone on 5HT_2Aand α₁Receptor Binding Affinity

Untitled

Selective Serotonin Reuptake Inhibitors: Implications for Advanced Nursing Practice

Contact Info

Product

Resources

About

Section Review Central & Peripheral Nervous Systems: New antidepressant agents: Recent pharmacological developments leading to improved efficacy

Cited by 5 publications

References 16 publications

Effect of Modifications of the Alkylpiperazine Moiety of Trazodone on 5HT2Aand α1Receptor Binding Affinity

Effect of Modifications of the Alkylpiperazine Moiety of Trazodone on 5HT2Aand α1Receptor Binding Affinity

Untitled

Selective Serotonin Reuptake Inhibitors: Implications for Advanced Nursing Practice

Contact Info

Product

Resources

About

Effect of Modifications of the Alkylpiperazine Moiety of Trazodone on 5HT_2Aand α₁Receptor Binding Affinity

Effect of Modifications of the Alkylpiperazine Moiety of Trazodone on 5HT_2Aand α₁Receptor Binding Affinity