TABLE 2

Inhibition by various compounds of specific binding to the DAT, σ1, or σ2 receptors

Ki values are presented with 95% confidence limits in parentheses.

Compoundσ1Ki Valueσ2Ki Valueσ1/σ2DAT Ki Value
CM 3040.684 (0.552–0.847)388 (215–702)0.0026840 (5270–8880)
BD 1063a8.81 (7.15–10.9)626 (447–876)0.0148020 (7100–9060)
AZ 664.70 (4.06–5.45)1.35 (0.911–2.00)3.481950 (1740–2190)
SN 7978.6 (65.2–94.7)11.3 (7.91–16.3)6.961820 (1590–2070)
SN 167392 (317–485)16.1 (10.4–24.9)24.3949 (821–1100)
CM 3981490 (1200–1860)4.50 (2.78–7.27)33111,100 (9940–12,400)
CM 3531120 (905–1380)4.48 (2.66–7.55)250206 (184–229)
(±)-SM 212760 (1700–4470)263 (166–409)10.5293 (264–326)
  • Low-affinity site Ki values for compounds for which σ2 binding modeled better for two sites than one site are as follows: CM 304, 12,800 (87.7–1,860,000); (±)-SM 21, 30,800 (4730–200,000); SN 79, 9130 (2860–29,100); SN 167, 373,000 (89,500–1,560,000); and CM 398, 180,000 (2230–14,500,000).

  • a The values for these compounds are those reported in the literature by Garcés-Ramírez et al. (2011) using methods identical to those in our study.