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The pumps allow the synaptosomes to concentrate serotonin by taking it up from the fluid in which the synaptosomes are suspended.

By radioactively tagging the serotonin, the rate of uptake can measure by adding tagged serotonin to the suspension for a specified period of time, then centrifuging and counting radioactivity in the synaptosomal pellet and expressing the result as the amount of radioactivity per milligram of protein.

The results from such a study are plotted in Figure 3.1 as a classic concentration-response curve in which the Y-axis is the response (ie, effect of the drug) and the X-axis is increasing concentration of the investigational drug (ie, the potential inhibitor).

In the case of the serotonin uptake pump, the effect is the degree of slowing or inhibition of the uptake of the radioactive serotonin into the synaptosomes.

Medications used in the treatment of insomnia include nonbenzodiazepine receptor agonists, benzodiazepine receptor agonists, the selective melatonin receptor agonist ramelteon, and sedating antidepressants.

The first step involves isolating these neural SOAs so that the effects of drugs on them can be studied in vitro.Sedative-hypnotics include nonbenzodiazepine receptor agonists (zaleplon, zolpidem, eszopiclone); short-acting benzodiazepine receptor agonists (triazolam); intermediate-acting benzodiazepine receptor agonists (estazolam, temazepam); and selective melatonin agonists (ramelteon).Both eszopiclone and sustained-release zolpidem are effective for both sleep-onset and sleep-maintenance insomnia, with a reduced abuse potential and long-term efficacy of up to 6 months as compared with nonselective benzodiazepine receptor agonists.Short-acting (eg, triazolam) and intermediate-acting (eg, estazolam, temazepam) benzodiazepine receptor agonists are useful for sleep-onset insomnia.These agents have been the hypnotics of choice for many years because of their relative safety compared with the barbiturates, as well as their low cost.It also shares some of the properties of selective serotonin reuptake inhibitor antidepressants ( fluoxetine , paroxetine , and sertraline ).