5-HT₇ receptor modulators: a medicinal chemistry survey of recent patent literature (2004 – 2009)

Abstract

Importance of the field: The 5-HT₇ receptors are discretely localized within the CNS (thalamus, hypothalamus, limbic and cortical regions). The 5-HT₇ receptors are also present in smooth muscle cells from blood vessels and have been reported in gastrointestinal tract as well as in rat lumbar dorsal root and sympathetic ganglia. The 5-HT₇ receptors have been implicated in depression, disorders related to circadian rhythms, pain and migraine. Thus, there is a great interest in developing potent and selective 5-HT₇ receptor modulators.

Areas covered in this review: This review article highlights the research advances published in the patent literature between January 2004 and December 2009, giving emphasis to the medicinal chemist's standpoint.

What the reader will gain: Readers will rapidly gain an overview of the various 5-HT₇ receptor modulators reported in the patent literature in the past 6 years. Furthermore, the readers will learn which structure type can interact with 5-HT₇ receptor and also the different companies that are the main players in the field.

Take home message: Although no 5-HT₇ modulator has entered clinical trials, the development and future use of different agonists and antagonists suitable for use in vivo seem very promising.

Keywords::

• AS-19
• circadian rhythm
• CNS
• depression
• GPCRs
• medicinal chemistry
• pain
• SB-269970
• serotonin 5-HT₇ receptor
• structure–activity relationships

Notes

This box summarizes key points contained in the article.