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.