TABLE 1

Structural substituents, physicochemical properties, DAT binding, and DA uptake inhibition data on BZT analogs and cocaine (Agoston et al., 1997)


Compound

R

Mol. Wt.

cLogPa

[3H]WINBindingb (KI)

Dopamine Uptakec (IC50)
nM
AHN 2-003 H 365.85 3.10 11 9.7
AHN 1-055 CH3 393.16 3.95 12 71
AHN 2-005 CH2CH=CH2 405.92 4.52 30 14
JHW 007 (CH2)3CH3 421.96 5.53 25 370
Cocaine

303.31
2.72
300-400
150-200
  • a Calculated log of the partition coefficient (cLogP).

  • b Affinity for the DAT by determination of the displacement of [3H]WIN 35,428, an analog of cocaine.

  • c Inhibition of [3H]DA uptake.