IMPORTANCE OF THE FIELD: The 5-HT(7) receptors are discretely localized within the CNS (thalamus, hypothalamus, limbic and cortical regions). The 5-HT(7) 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-HT(7) 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-HT(7) 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-HT(7) receptor modulators reported in the patent literature in the past 6 years. Furthermore, the readers will learn which structure type can interact with 5-HT(7) receptor and also the different companies that are the main players in the field. TAKE HOME MESSAGE: Although no 5-HT(7) modulator has entered clinical trials, the development and future use of different agonists and antagonists suitable for use in vivo seem very promising
5-HT7 receptor modulators: a medicinal chemistry survey of recent patent literature (2004 - 2009)
LEOPOLDO, Marcello;LACIVITA, ENZA;BERARDI, Francesco;PERRONE, Roberto
2010-01-01
Abstract
IMPORTANCE OF THE FIELD: The 5-HT(7) receptors are discretely localized within the CNS (thalamus, hypothalamus, limbic and cortical regions). The 5-HT(7) 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-HT(7) 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-HT(7) 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-HT(7) receptor modulators reported in the patent literature in the past 6 years. Furthermore, the readers will learn which structure type can interact with 5-HT(7) receptor and also the different companies that are the main players in the field. TAKE HOME MESSAGE: Although no 5-HT(7) modulator has entered clinical trials, the development and future use of different agonists and antagonists suitable for use in vivo seem very promisingI documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
