By Jose M. Palacios, Angel Pazos, Daniel Hoyer (auth.), Giuseppe Di Giovanni, Ennio Esposito, Vincenzo Di Matteo (eds.)
Research of 5-HT2c receptors stretches again twenty-five years, and whereas a lot of it's been effective, the prior decade of analysis has been striking by way of either volume produced and insights won. it really is rarely impressive that 5-HT2c receptor study has grown so fruitful, provided that it's a fashionable valuable serotonin receptor subtype largely expressed in the valuable and the peripheral apprehensive method and is believed to play a huge function within the rules of various behaviors. It has extra been proven by means of experimental and scientific remark that it might probably symbolize a potential healing objective for the improvement of gear for a variety of primary fearful method issues. The time, accordingly, is greater than acceptable to supply the 1st ever assessment of the learn of 5-HT2c receptors. a part of the preferred and significant sequence, “The Receptors,” The 5-HT2c Receptor offers an intensive replace of the sensible prestige of the 5-HT2c receptor. It covers the molecular, mobile, anatomical, biochemical and behavioral elements of this receptor on the way to spotlight its particular regulatory houses and the rising practical importance of constitutive task and RNA-editing in vivo. moreover, the booklet investigates the receptors’ healing strength in more than a few diverse illnesses, handled separately in separate chapters, together with melancholy, drug abuse, schizophrenia, consuming issues, Parkinson’s sickness, Prader-Willi Syndrome, Alzheimer’s sickness and epilepsy. whereas now not exhaustive, this article is a crucial software in knowing the prior and encouraging the way forward for interdisciplinary examine at the 5-HT2c receptor.
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Extra resources for 5-HT2C Receptors in the Pathophysiology of CNS Disease
Neuropharmacology 38:1083–1152. Boothman L, Raley J, Denk F, Hirani E, Sharp T (2006) In vivo evidence that 5-HT(2C) receptors inhibit 5-HT neuronal activity via a GABAergic mechanism. Br J Pharmacol 149:861–869. Cassel JC, Jeltsch H (1995) Serotonergic modulation of cholinergic function in the central nervous system: cognitive implications. Neuroscience 69:1–41. Clemett DA, Punhani T, Duxon MS, Blackburn TP, Fone KCF (2000) Immunohistochemical localisation of the 5-HT2C receptor protein in the rat CNS.
1994; Di Giovanni et al. 1999; Di Matteo et al. 1998). The implication of 5-HT 2C receptors in the regulation of nigrostriatal dopaminergic function has been a subject of debate mainly due to controversial results obtained with different 5-HT2C receptor acting molecules (Di Matteo et al. 2001; Porras et al. 2002; De Deurwaerdère et al. 2004; Navailles et al. 2004). Very recently (Abdallah et al. 2009) by using the 5-HT2C receptor null mutant mice, previously generated by Tecott and collaborators (Tecott et al.
1 Indoline-Containing Structures The search for selective 5-HT2C receptor antagonists has been extensively pursued by researchers at GlaxoSmithKline. 1. Early studies were aimed to obtain 5-HT2C agents with selectivity over 5-HT2A receptors, because both 5-HT2 M. it G. Di Giovanni et al. 1007/978-1-60761-941-3_3, © Springer Science + Business Media, LLC 2011 29 30 M. Leopoldo et al. Fig. 1 The evolution of the first template of 5-HT2C receptor antagonists developed by GlaxoSmithKline 3 The Medicinal Chemistry of 5-HT2C Receptor Ligands 31 receptor subtypes are localized within the central nervous system, in contrast to the 5-HT2B subtype, which is localized peripherally.