Serotonin receptor activity

Glennon, R.A. and Lucki, I. Behavioral models of serotonin receptor activation. In Sanders-Bush, E., ed. The Serotonin Receptors. Clifton, NJ The Humana Press, 1988. pp. 253-293. 

C. W., Crossan, P.J., Klump, K.L. (in press) Altered medial orbital frontal serotonin receptor activity after recovery from bulimia nervosa. Am Psychiatry. 

Lotto B, Upton L, Price DJ, Gaspar P. Serotonin receptor activation enhances neu-rite outgrowth of thalamic neurones in rodents. Neurosci Lett 1999 269 87-90. 

Penington NJ, Kelly JS. Serotonin receptor activation reduces calcium current in an acutely dissociated adult central neuron. Neuron 1990 4 751-758. 

Nichols CD et al (2002) Hallucinogens and Drosophila linking serotonin receptor activation to behavior. Neirroscience 115 979-984... 

There are numerous transmitter substances. They include the amino acids glutamate, GABA and glycine acetylcholine the monoamines dopamine, noradrenaline and serotonin the neuropeptides ATP and NO. Many neurones use not a single transmitter but two or even more, a phenomenon called cotransmission. Chemical synaptic transmission hence is diversified. The basic steps, however, are similar across all neurones, irrespective of their transmitter, with the exception of NO transmitter production and vesicular storage transmitter release postsynaptic receptor activation and transmitter inactivation. Figure 1 shows an overview. Nitrergic transmission, i.e. transmission by NO, differs from transmission by other transmitters and is not covered in this essay. 

Antipsychotics (conventional agents have nonspecific dopamine receptor antagonsim atypical agents also have serotonin antagonist activity), ecopipam, GBR-12909 and other partial dopamine agonists (may be functional antagonists)... 

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... 

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... 

Cusin, C., Serretti, A., Zanardi, R. etal. (2002). Influence of monoamine oxidase A and serotonin receptor 2A polymorphisms in SSRI antidepressant activity. Int.. Neuropsychopharmacol, 5, 27-35. 

Witz, P., Amlaiky, N., Plassat, J. L., Maroteaux, L., Borrelli, E., and Hen, R. (1990). Cloning and characterization of a Drosophila serotonin receptor that activates adenylate cyclase. Proc. Natl. Acad. Sci. USA 87 8940-8944. 

Liu, R., Jolas, T. Aghajanian, G. (2000). Serotonin 5-HT(2) receptors activate local GABA inhibitory inputs to serotonergic neurons of the dorsal raphe nucleus. Brain Res. 873, 34-45. 

The pyrazino[ 1,2-3111,2 bcnzothiazinc 336 exhibits serotonin receptor modulator activity <2005USP2005/080074>. 

In connection with a study of potential serotonin receptor antagonists, some decahydrocyclazin-6-ones and -6-ols have been synthesized from acyclic precursors <1992SC3115> (Scheme 115), but those esters derived from the latter (both epimers) which have been tested to date as potential 5-HT3 receptor antagonists have shown little biological activity <1993EJM869>. 

Three families of serotonin receptor, the 5-HT family, the 5-HT2 family and the family that includes the 5-HT4, 5-ht6 and 5-HT7 receptors represent the three major classes of 5-HT receptor that are G-protein-coupled receptors (Ch. 19). The 5-HT3 receptor is a ligand-gated ion channel and is a separate family. Although each serotonin receptor can be potently activated by 5-HT, differences insignal transduction mechanisms,neuroanatomical distribution and affinities for synthetic chemicals create opportunities for drug discovery and make each 5-HT receptor subtype a potential therapeutic target. 

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