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 efficient, the earlier decade of study has been impressive by way of either quantity produced and insights won. it's not often miraculous that 5-HT2c receptor study has grown so fruitful, on condition that it's a famous vital serotonin receptor subtype extensively expressed in the principal and the peripheral frightened method and is assumed to play an incredible position within the legislation of various behaviors. It has additional been proven through experimental and medical remark that it could characterize a potential healing objective for the advance of substances for quite a number valuable apprehensive approach issues. The time, for this reason, is greater than applicable to supply the 1st ever evaluation of the study of 5-HT2c receptors. a part of the preferred and demanding sequence, “The Receptors,” The 5-HT2c Receptor presents a radical replace of the practical prestige of the 5-HT2c receptor. It covers the molecular, mobile, anatomical, biochemical and behavioral facets of this receptor in order to spotlight its special regulatory homes and the rising useful value of constitutive job and RNA-editing in vivo. furthermore, the booklet investigates the receptors’ healing strength in more than a few diversified illnesses, taken care of separately in separate chapters, together with melancholy, drug abuse, schizophrenia, consuming problems, Parkinson’s disorder, Prader-Willi Syndrome, Alzheimer’s sickness and epilepsy. whereas no longer exhaustive, this article is an important device in realizing the prior and encouraging the way forward for interdisciplinary learn at the 5-HT2c receptor.
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Additional info for 5-HT2C Receptors in the Pathophysiology of CNS Disease
Scale bars: (a) 1 mm; (b) 20 mm In fact, the interaction of cholinergic and serotonergic systems has been extensively studied, especially those aspects relating to the modulation of central cholinergic function by serotonin and its possible cognitive implications (See the review in Cassel and Jeltsch (1995)). Regarding 5-HT2C receptors and cholinergic function, several microdialysis studies carried out in rat brain showed the effect of 1-(3-chlorophenyl)piperazine (mCPP) (an unselective 5-HT2C receptor agonist) on the release of acetylcholine in rat cortex (Zhelyazkova-Savova et al.
2006). 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.
Zhelyazkova-Savova M, Giovannini MG, Pepeu G (1997) Increase of cortical acetylcholine release after systemic administration of chlorophenylpiperazine in the rat: an in vivo microdialysis study. Neurosci Lett 236:151–154. Zhelyazkova-Savova M, Giovannini MG, Pepeu G (1999) Systemic chlorophenylpiperazine increases acetylcholine release from rat hippocampus-implication of 5-HT2C receptors. Pharmacol Res 40:165–170. 1 Introduction 5-HT2 receptors are major targets for a wide array of psychoactive drugs, ranging from nonclassical antipsychotic drugs, anxiolytics and antidepressants, which have a 5-HT2 antagonistic action, to hallucinogens, which are agonists of the 5-HT2 receptors.
5-HT2C Receptors in the Pathophysiology of CNS Disease by Jose M. Palacios, Angel Pazos, Daniel Hoyer (auth.), Giuseppe Di Giovanni, Ennio Esposito, Vincenzo Di Matteo (eds.)