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 previous decade of study has been striking when it comes to either volume produced and insights received. it really is hardly ever excellent that 5-HT2c receptor examine has grown so fruitful, provided that it's a sought after significant serotonin receptor subtype generally expressed in the important and the peripheral apprehensive procedure and is believed to play an immense position within the law of diverse behaviors. It has extra been proven via experimental and scientific remark that it may well signify a potential healing goal for the improvement of gear for quite a number significant fearful process problems. The time, for this reason, is greater than applicable to supply the 1st ever review of the learn of 5-HT2c receptors. a part of the preferred and critical sequence, “The Receptors,” The 5-HT2c Receptor offers a radical replace of the sensible prestige of the 5-HT2c receptor. It covers the molecular, mobile, anatomical, biochemical and behavioral facets of this receptor to be able to spotlight its precise regulatory houses and the rising useful importance of constitutive task and RNA-editing in vivo. furthermore, the ebook investigates the receptors’ healing power in more than a few diverse illnesses, taken care of separately in separate chapters, together with melancholy, drug abuse, schizophrenia, consuming issues, Parkinson’s disorder, Prader-Willi Syndrome, Alzheimer’s ailment and epilepsy. whereas now not exhaustive, this article is an important software in realizing the earlier and encouraging the way forward for interdisciplinary examine at the 5-HT2c receptor.
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Extra info for 5-HT2C Receptors in the Pathophysiology of CNS Disease
Neuroscience 21:97–122. Pompeiano M, Palacios JM, Mengod G (1994) Distribution of the serotonin 5-HT2 receptor family mRNAs: comparison between 5-HT2A and 5-HT2C receptors. Brain Res Mol Brain Res 23:163–178. Porras G, Di Matteo V, Fracasso C, et al (2002) 5-HT2A and 5-HT2C/2B receptor subtypes modulate dopamine release induced in vivo by amphetamine and morphine in both rat nucleus accumbens and striatum. Neuropsychopharmacology 26:311–324. Prichett DB, Bach AWJ, Wozny M, et al (1988) Structure and functional expression of cloned rat serotonin 5-HT2 receptor.
Additionally, the signal transduction characteristics of transfected receptors may be dependent on the identity of the host cell line. Clearly, all these aspects may have a profound impact on the observed functional selectivities over 5-HT2A and 5-HT2B receptors. Generally, functional data are based on measurements of a second messenger response, such as phosphoinositide hydrolysis or increase in intracellular calcium at 5-HT2C, 5-HT2A, and 5-HT2B receptors expressed in the same host cell line.
1). The different decoration of the scaffold led to different values in potency. In particular, a methoxy group on the phenyl ring was favored; substitution of the left hand side aromatic portion was well tolerated with respect to the potency and selectivity; the piperidine was the best basic moiety; hydrogenation of the lactamic double bond affected negatively both affinity and metabolic stability (Micheli et al. 2006). Conformational analysis of the template 34 (Fig. 3) showed a rather small dihedral angle between the lactam and the adjacent left hand side phenyl ring for the global minimum conformer.