Serotonin receptor modulators

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

Zhou F-M, Hablitz JJ (1999) Activation of serotonin receptors modulates synaptic transmission in rat cerebral cortex. J Neurophysiol 82 2989-99... 

A detailed review of oleamide, including a discussion of its possible modes of action such as serotonin receptor modulation and gap junction inhibition, is available (208). 

Table 21.11. Pharmacokinetics of the Dopamine and Norepinephrine Reuptake Inhibitors (DNRIs) and Serotonin Receptor Modulators (SRMs) ...

Raiiy, R. V Heffeman, M. Pharmaceutical compositions comprising an agent with serotonin receptor modulating activity for sleep disorders. PCX Int. Appl. WO 2006069030, 2006 Chem. Abstr. 2006, 145, 110313. 

Robichaud AJ, Largent BL (2000) Recent advances in selective serotonin receptor modulation. Aimu Rep Med Chem 35 11 (Chapter 2)... 

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. 

Over 95% of the body s serotonin (5-HT) is found in the gastrointestinal tract in enterochromaffin cells and neurons. There are 18 known serotonin receptor sub-types, of which 5-HT, 5-HT3, and 5-HT are located in the gut and modulate gut secretion, motility, and sensation (57). The 5-HT in the synaptic spaces stimulates these receptors until it is actively cleared by a 5-HT transporter protein located on the presynaptic neuronal endings. 

Several different types of serotonin receptor (for example, S-HTi / 5-HT2A/ 5-HT2C/ 5-HTib/id) have been associated with the motor side effects of the SSRIs which may arise should these drugs be administered in conjunction with a monoamine oxidase inhibitor. The 5-HT3 receptor is an example of a non-selective cation charmel receptor which is permeable to both sodium and potassium ions and, because both calcium and magnesium ions can modulate its activity, the 5-HT3 receptor resembles the glutamate-NMDA receptor. Antagonists of the 5-HT3 receptor, such as ondansetron, are effective antiemetics and are particularly useful when... 

Dulawa SC, Hen R, Scearce-Levie K, Geyer M (1997) Serotonin IB receptor modulation of startle reactivity, habituation, and prepulse inhibition in wildtype and serotonin IB knock-out mice. Neiuoreport 132 125-134... 

Serotonin (5-hydroxytryptamine [5-HT]) pathways play an important role in postprandial satiety. Treatments that increase intrasynaptic serotonin or directly activate serotonin receptors tend to reduce food consumption, whereas interventions that dampen serotonergic neurotransmission or block receptor activation reportedly increase food consumption and promote weight gain (Blundell, 1984 Teibowitz, 1986). Moreover, CNS serotonin pathways have been implicated in the modulation of mood, impulse regulation and be-... 

The anxiolytic activity of several compounds in some, but not all, animal models of anxiety in fact suggests that different receptor subtypes may modulate different types of anxiety as discussed below. It would not be surprising if the specific serotonin links to disorders of anxiety also differ among the various disorders of anxiety such as generalized anxiety versus obsessive-compulsive disorder versus panic disorder versus social phobia versus mixed anxiety depression. Such studies are in progress, and much further research is necessary to clarify the potential links between subtypes of anxiety and subtypes of serotonin receptors. 

The 5-HTja receptor was first described in 1981 and is perhaps the best characterized of the serotonin receptors. 5-HTja receptors have been implicated in the regulation of aggression, affect, anxiety, appetite, sexual behavior, and in the control of stress-related disorders [Dourish et al. 1987]. Also, these receptors play a major role in modulating serotonergic transmission. 

A very similar twofold mechanism modulates acetylcholine release in the human neocortex, with one exception the inhibitory presynaptic serotonin receptor is 5-HTif (Feuerstein and Seeger 1997). 

---