5-HT(7) receptor modulators: a medicinal chemistry survey of recent patent literature (2004 - 2009).
BACKGROUND
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.


METHODS
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.


RESULTS
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.


CONCLUSIONS
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.
Leopoldo
Marcello
M
Dipartimento Farmaco-Chimico, Università degli Studi di Bari A. Moro, via Orabona 4, Bari 70125, Italy. leopoldo@farmchim.uniba.it
Lacivita
Enza
E
Berardi
Francesco
F
Perrone
Roberto
R
D000818:Animals; D016503:Drug Delivery Systems; D015195:Drug Design; D006801:Humans; D010330:Patents as Topic; D051381:Rats; D011985:Receptors, Serotonin / Q000187:drug effects* / Q000378:metabolism; D012702:Serotonin Antagonists / Q000494:pharmacology*; D017366:Serotonin Receptor Agonists / Q000494:pharmacology*
D011985:Receptors, Serotonin; D012702:Serotonin Antagonists; D017366:Serotonin Receptor Agonists; C104425:serotonin 7 receptor