Pharmacophore comparison and development of recently discovered long chain arylpiperazine and sulfonamide based 5-HT7 ligands

Andrea Rague, Kevin Tidgewell

Research output: Contribution to journalReview articlepeer-review

13 Scopus citations

Abstract

The serotonin system exerts its effects on the CNS and many peripheral systems. Of the 14 serotonin receptors, the 5-HT7 receptor is the most recently discovered. The 5-HT7 receptor has been shown to be involved in stress reduction, depression, and nociceptive control. Despite the 20 years since the discovery of 5-HT7R, there are still few truly selective ligands. Two of the common scaffolds for 5-HT7R ligands are long chain arylpiperazines (LCAPs) and sulfonamide containing compounds. This review focuses on recently developed (2014-2016) 5-HT7R ligands, their selectivity for the receptor, and suggests the possible new pharmacophore models for these ligands.

Original languageEnglish
Pages (from-to)552-560
Number of pages9
JournalMini-Reviews in Medicinal Chemistry
Volume18
Issue number7
DOIs
StatePublished - Apr 1 2018

Bibliographical note

Publisher Copyright:
© 2018 Bentham Science Publishers.

Funding

FundersFunder number
National Center for Complementary and Integrative HealthR15AT008060

    Keywords

    • 5-HT7
    • Arylpiperazine
    • CNS
    • Drug design
    • Pharmacophore
    • Serotonin

    ASJC Scopus subject areas

    • Molecular Medicine
    • Pharmacology
    • Drug Discovery
    • Cancer Research

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