5-HT1A receptor ligands and their therapeutic applications: review of new patents

ABSTRACT

Introduction: 5-HT_1AR was one of the first discovered serotonin receptors and is one of the most thoroughly studied. Dysfunctions associated with 5-HT_1AR neurotransmission are linked to several psychiatric disorders, including anxiety, depression, and movement disorders.

Areas covered: The current review covers patent literature published between January 2012 and May 2018. Queries were performed on Espacenet, SciFinder, clinicaltrials.gov, pharmacodia.com, and the websites of pharmaceutical companies.

Expert opinion: Several novel therapeutic applications have been proposed for 5-HT_1AR ligands, i.e. prostate cancer treatment, gastrointestinal and cardiopulmonary disorders, facilitation of urination and defecation, and L-DOPA-induced dyskinesia. Interestingly, no patent application has been filed by big pharma companies, while numerous researches are being conducted in smaller companies and academia.

KEYWORDS:

• 5-HT_1A
• agonist
• antagonist
• serotonin receptor
• serotonin modulator
• therapeutic patent

Article highlights

• 5-HT_1AR remains as a promising target for anxiolytic drugs.

• Novel therapeutic applications were proposed for the 5-HT_1AR ligands, although most clinical trials are still directed at depression or anxiety.

• Emergence of a biased 5-HT_1AR agonist opened a new perspective in the pharmacotherapy with 5-HT_1AR ligands.

• The research on 5-HT_1AR switched to smaller pharmaceutical companies and academia.

Acknowledgment

The authors would like to make a special acknowledgment to Stanisław Jastrzębski from the Faculty of Mathematics and Computer Science of Jagiellonian University, Kraków, Poland, for preparing the comparison of structures covered by patents with ligands from the ChEMBL database (Figure 5).

Declaration of interest

The authors have no relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript. This includes employment, consultancies, honoraria, stock ownership or options, expert testimony, grants or patents received or pending, or royalties.

Reviewer disclosures

Peer reviewers on this manuscript have no relevant financial or other relationships to disclose.

Supplementary material

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Additional information

Funding

This article was not funded.