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The first data to consider in determining the biochemical profile of reuptake inhibitors are their affinity values for membranal carriers. These values can be calculated by determining the concentration of a medication necessary to displace 50% of the specific binding of a standard ligand for a given transporter subtype in a lyzed cell preparation (Ki). This technique generally provides rough estimates of the potential for drugs to inhibit reuptake. A somewhat more indicative approach consists of determining the concentrations of drugs necessary to inhibit the uptake of transmitters in intact cells from either animal brains or human cell lines. These physiological results are more reliable than mere binding data because of the integrity of the tissue. Indeed, recent data indicate that the binding of some norepinephrine reuptake blockers varies markedly when they are tested in membrane preparations versus intact cells, whereas with other agents, such as the tricyclic antidepressants (TCAs), it does not (Mason et al. 2007). As can be seen in Table 23–1, not only do the absolute potencies vary between the two preparations, their ratios vary as well.

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Table Reference Number
TABLE 23–1. In vitro affinity and inhibition values for milnacipran and duloxetine for human reuptake transporters

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