title: Selective agonists for serotonin 7 (5-HT7) receptor and their applications in preclinical models: an overview.
abstract: The serotonin 7 (5-HT7) receptor was the last serotonin receptor subtype to be discovered in 1993. This receptor system has been implicated in several central nervous system (CNS) functions, including circadian rhythm, rapid eye movement sleep, thermoregulation, nociception, memory and neuropsychiatric symptoms and pathologies, such as anxiety, depression and schizophrenia. In 1999, medicinal chemistry efforts led to the identification of SB-269970, which became the gold standard selective 5-HT7 receptor antagonist, and later of various selective agonists such as AS-19, LP-44, LP-12, LP-211 and E-55888. In this review, we summarize the preclinical pharmacological studies performed using these agonists, highlighting their strengths and weaknesses. The data indicate that 5-HT7 receptor agonists can have neuroprotective effects against N-methyl-d-aspartate-induced toxicity, modulate neuronal plasticity in rats, enhance morphine-induced antinociception and alleviate hyperalgesia consecutive to nerve lesion in neuropathic animals.
authors.forename: Pantaleo
authors.initials: P
authors.lastname: Di Pilato
authors.forename: Mauro
authors.initials: M
authors.lastname: Niso
authors.forename: Walter
authors.initials: W
authors.lastname: Adriani
authors.forename: Emilia
authors.initials: E
authors.lastname: Romano
authors.forename: Domenica
authors.initials: D
authors.lastname: Travaglini
authors.forename: Francesco
authors.initials: F
authors.lastname: Berardi
authors.forename: Nicola A
authors.initials: NA
authors.lastname: Colabufo
authors.forename: Roberto
authors.initials: R
authors.lastname: Perrone
authors.forename: Giovanni
authors.initials: G
authors.lastname: Laviola
authors.forename: Enza
authors.initials: E
authors.lastname: Lacivita
authors.forename: Marcello
authors.initials: M
authors.lastname: Leopoldo
mesh_terms: D000818:Animals; D001833:Body Temperature Regulation / Q000187:drug effects; D002940:Circadian Rhythm / Q000187:drug effects; D004353:Drug Evaluation, Preclinical; D006801:Humans; D007858:Learning / Q000187:drug effects; D009422:Nervous System Diseases / Q000188:drug therapy* / Q000517:prevention & control; D051381:Rats; D011985:Receptors, Serotonin / Q000378:metabolism*; D017366:Serotonin Receptor Agonists / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*
chemical_list: D011985:Receptors, Serotonin; D017366:Serotonin Receptor Agonists; C104425:serotonin 7 receptor