Serotonin enhancement

Mechanism of Action A central nervous system (CNS) stimulant that inhibits re-uptake of serotonin (enhancing satiety) and norepinephrine (raises metabolic rate) centrally. Therapeutic Effect Induces and maintains weight loss. 

Fluoxetine is absorbed well from the GI tract, is bound to plasma proteins to the extent of 95%, is metabolized in the Uver to norfluoxetine, and is excreted in the urine. Tryptophan is used as an antidepressant. However, the combined use of tryptophan, which increases the level of serotonin, and fluoxetine, which inhibits the neuronal uptake of serotonin, enhances the side effects of fluoxetine such as GI disturbances, anxiety, and insomnia (see Figure 86). 

Paroxetine is a selective serotonin reuptake inhibitor that blocks reuptake of serotonin, enhancing serotonergic function. It is used to treat panic disorder or social anxiety disorder (except Pexeva), as defined in the DSM-IV major depressive disorder, as defined in DSM-111 (immediate release) orDSM-lV (controlled release). Immediate release only for obsessive-compulsive disorder (OCD) generalized anxiety disorder (GAD) (except Pexeva) posttraumatic stress disorder (PTSD), as defined in the DSM-IV (except Pexeva). 

KLOPPENBURG, P., FERNS, D MERCER, A. R., Serotonin Enhances Central Olfactory Neuron Responses to Female Sex Pheromone in the Male Sphinx Moth Manduca sexta, J. Neurosci., 1999, 19, 8172-8181. 

Serotonin syndrome occurs primarily in patients taking monoamine oxidase (MAO) inhibitors (see p 269) who also take serotonin-enhancing drugs, such as meperidine (Demerol ), fluoxetine (Prozac ), or other serotonin reuptake inhibitors (SSRIs see Antidepressants, p 88), and is characterized by irritability, rigidity, myoclonus, diaphoresis, autonomic instability, and hyperthermia. It may also occur in people taking an overdose of or combinations of SSRIs even without concurrent use of MAO inhibitors. 

St. John s Wort Hypericum perforatum 1 Mild Gl upset mild serotonin enhancer (seep 215)... 

Guo X, Ma Z, Kang L. Serotonin enhances sohtaiiness in phase transition of the migratory locust. Front Behav Neurosci 2013 7 129. 

Another theory for the action of stimulant diugs in ADHD involves effects on nonstiiatal monoamine systems. Frontal cortical dopamine, norepinephrine, and serotonin are clearly important in cognitive functioning and impulse control. These neurotransmitters directly modulate reward-related behaviors associated with the striatal dopamine system. Moreover, the amygdala may be pharmacologically influenced leading to enhanced... 

TK NKxr displays a broad distribution in both peripheral tissues and in the central nervous system (CNS). In both CNS and enteric neurons, NKxr stimulation increase their excitability, whereas in trigeminal ganglion neurons SP has no intrinsic electrophysio-logical effects but is capable to enhance the amplitude of the inward current induced by the stimulation of serotonin 5-HT3 recqrtors. This enhancement dqjends on the activation of PKC via the stimulation of NKX recqrtors. This is an interesting case of receptor cross talk. Other functions of NKxr have been also highlighted. 

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... 

Enhancing the positive effects of serotonin and norepinephrine in the afferent and efferent pathways of the micturition reflex... 

The second cell-specific regulatory element within the distal enhancer is named SER. Loss of this element, which is at the extreme distal edge of the enhancer, leads to a selective loss of DDC expression in the ventral lateral serotonin cells (Johnson et al., 1989 Lundell and Hirsh, 1992) (Fig. 6C). This element has been delimited to about 40 bp and shows unexpected complexity, consisting of two functionally redundant elements. These two subelements, SERl and SERr, are each sufficient to allow normal DDC expression in the ventral lateral serotonin neurons if the other is deleted. In spite of this functional similarity, no sequence similarity is apparent between the two regions. The region of conservation between D. melanogaster and D. virilis is limited to SERl. 

---