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: Pantaleo Di Pilato, Mauro Niso, Walter Adriani, Emilia Romano, Domenica Travaglini, Francesco Berardi, Nicola A Colabufo, Roberto Perrone, Giovanni Laviola, Enza Lacivita, Marcello Leopoldo
• Journal: Reviews in the neurosciences (Rev Neurosci) Vol. 25 Issue 3 Pg. 401-15 ( 2014) ISSN: 0334-1763 [Print] Germany
• PMID: 24622785 (Publication Type: Journal Article, Review)

Chemical References

• Receptors, Serotonin
• Serotonin Receptor Agonists
• serotonin 7 receptor

Topics

• Animals
• Body Temperature Regulation (drug effects)
• Circadian Rhythm (drug effects)
• Drug Evaluation, Preclinical
• Humans
• Learning (drug effects)
• Nervous System Diseases (drug therapy, prevention & control)
• Rats
• Receptors, Serotonin (metabolism)
• Serotonin Receptor Agonists (chemistry, pharmacology, therapeutic use)