The therapeutic potential of 5-HT1A receptors: a patent review

Abstract

Introduction: The 5-HT_1A receptors are implicated in mood disorders (anxiety, depression), in cognition, and in modulation of pain. Nearly 30 years of research in this field, there is still interest in developing new chemical entities capable of 5-HT_1A receptor activation or blockade.

Areas covered: This review article will highlight and review the research advances published in the patent literature between January 2007 and December 2011, giving emphasis to the medicinal chemist's standpoint. Literature search methodology included search in Scifinder and PubMed Databases and browsing clinicaltrials.gov website.

Expert opinion: Almost no new therapeutic applications have been proposed for molecules targeting the 5-HT_1A receptor, during the years covered by the present review. The discovery that stimulation of 5-HT_1A receptor can promote neurogenesis will likely renew the interest for selective 5-HT_1A receptor agonists as therapeutics to replace neural populations damaged by disease or injury.

Keywords::

• anxiety
• central nervous system
• depression
• G-protein-coupled receptors
• medicinal chemistry
• neurogenesis
• pain
• Parkinson's disease
• schizophrenia
• serotonin 5-HT1A receptor
• structure–activity relationships

Notes

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