Serotonin ! receptors

Serotonin antagonist Serotomnergic agents Serotomnergic neurons Serotonin receptors Seroxat Serpak process Serpasil Serpentine... 

Table 17. Serotonin and Serotonin Receptor Agonists and Antagonists...

Future Outlook for Antidepressants. Third-generation antidepressants are expected to combine superior efficacy and improved safety, but are unlikely to reduce the onset of therapeutic action in depressed patients (179). Many dmgs in clinical development as antidepressive agents focus on estabhshed properties such as inhibition of serotonin, dopamine, and/or noradrenaline reuptake, agonistic or antagonistic action at various serotonin receptor subtypes, presynaptic tt2-adrenoceptor antagonism, or specific monoamine—oxidase type A inhibition. Examples include buspirone (3) (only... 

The involvement of serotonin (5-hydroxytryptamine) in disease states has been recognized for several decades. Research on antagonists awaited the recent development of methodology involving serotonin receptors. A thiazolopyrimidone serves as the nucleus for a pair of serotonin antagonists. The key intermediate 118 is in fact simply the lactonized form of 2-hydroxyethyl acetoace-tate. Condensation of this P-keto ester can be visualized to involve initial attack on the reactive... 

Anxiolytics are drugs used for the treatment of anxiety disorders. Apart from benzodiazpines, a frequently used anxiolytic is the 5HT1A (serotonin) receptor agonist buspiron, which has no sedative, amnestic or muscle-relaxant side effects, but whose action takes about a week to develop. Furthermore, it is less efficaceous than the benzodiazepines. Buspiron s mechanism of action is not fully understood. 

Aghajanian GK, Haigler HJ Hallucinogenic indoleamines preferential action upon presynaptic serotonin receptors. Psychopharmacol Commun 1 619-629, 1975... 

Nichols DE Studies ofthe relationship between molecular structure and hallucinogenic activity. Pharmacol Biochem Behav 24 335-340, 1986 Nichols DE Hallucinogens. Pharmacol Ther 101 131-191, 2004 Peroutka SJ Serotonin receptors, in Psychopharmacology The Third Generation of Progress. Edited by Meltzer HY. New York, Raven, 1987, pp 303-311 Perry PJ, Wilding OC, Juhl RP Anticholinergic psychosis. Am J Hosp Pharm 35 725— 728, 1978... 

Uphouse, L (1997) Multiple serotonin receptors too many, not enough, or just the right number ... 

Deakin, JFW, Graeff, FG and Guimaraes, FS (1992) 5-HT receptor subtypes and the modulation of aversion. In Central Serotonin Receptors and Psychotropic Drugs (Eds Marsden, CA and Heal, DJ), Blackwell Scientific Publications, Oxford, pp. 147-174. 

IsmaielAM et al. (1997) 2-(l-Naphthyloxy)ethylamines with enhanced affinity for human 5-HTlD beta (h5-HTlB) serotonin receptors. J Med Chem 40(26) 4415-4419... 

In earlier proposals (Anderson et al. 1978), based on this stereoselectivity for the S enantiomer of MDMA, it was suggested that, rather than having a direct effect at serotonin receptors, perhaps MDMA was a neurotransmitterreleasing agent, acting in a fashion similar to amphetamine, for which the S enantiomer is also more active than the R enantiomer. A subsequent study... 

Glennon, R.A. Liebowitz, S.M. and Anderson, G.M. Serotonin receptor affinities of psychoactive phenalkylamine analogues. J Med Chem 23 294-299, 1980. 

Essman, E.J., and Valzelli, L. Regional brain serotonin receptor changes in differentially housed mice Effects of amphetamine. Pharmacol Res Commun 16 401-408, 1984. 

Although initial studies indicated that the various derivatives of 2,5-DMA exhibited low affinity for 5-HTi serotonin receptors (Shannon et al. 1984). it was unclear from these studies what the affinities of the drugs were for the respective subtypes of 5-HTjserotonin sites (i.e., 5-HTia, 5-HTjb, and 5-HTic receptors). In subsequent studies (Titeler et al. 1988), the affinities... 

TABLE 2. Two-site analysis of the interaction of tryptamine agonists and 2,5-DATA derivatives with 5-HT2 serotonin receptors... 

FIGURE 2. Competition curves of R(-)-DOI for [ HJketanserin binding to 5-HT2 serotonin receptors in rat frontal cortex membranes in the presence and absence of the guanine nucleotide analog Gpp(NH)p... 

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