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Source. Reprinted from Potter WZ, Manji HK, Rudorfer MV: "Tricyclics and Tetracyclics," in The American Psychiatric Press Textbook of Psychopharmacology, Second Edition. Edited by Schatzberg AF, Nemeroff CB. Washington, DC, American Psychiatric Press, 1998, p. 200. Copyright 1998, American Psychiatric Press, Inc. Used with permission.

Although the tricyclics are named for their central three-ring structure, the nature of the side chain appears more important for their function. The tertiary tricyclics—amitriptyline, imipramine, and clomipramine—are more potent in blocking the serotonin transporter. The secondary tricyclics are much more potent in blocking the norepinephrine transporter (Table 12-1) (Bolden-Watson and Richelson 1993; Tatsumi et al. 1997).

TABLE 12-1. Affinity of tricyclics and tetracyclics for the neurotransmitter transporters and specific receptors (expressed as equilibrium dissociation constants)

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