TABLE 2

Ki values (nanomolar) for SRI-31142 at different receptor targets as determined by the PDSP

Previously published data on the potency of the compound to inhibit DAT-mediated monoamine uptake and bind to DAT are also shown for comparison.

Receptor TargetKi Value
nM
DAT uptake inhibition (IC50)1.9a
Rat DAT (IC50)2340a
Mu opioid116b
Peripheral BZP491b
Histamine H2617b
Norepinephrine alpha 2B1177b
5-HT 5-HT71218b
Acetylcholine M41261b
Delta opioid1390b
DA D31528b
Acetylcholine M21612b
BZP site1633b
Kappa opioid2413b
Acetylcholine M12470b
Norepinephrine beta 32654b
Norepinephrine alpha 2A2737b
Human DAT3520b
Acetylcholine M55229b
Histamine H45535b
Histamine H15585b
Acetylcholine M35951b
Otherc>10,000b
  • BZP, benzodiazepine.

  • a From Rothman et al. (2015) using [3H]WIN354428 as the radioligand. The same radioligand is used for DAT in PDSP.

  • b From PDSP.

  • c Other sites with Ki values >10,000 nM were 5-HT1A/B/D/E, 5-HT2A/B/C, 5-HT3, 5-HT5a, 5-HT6, norepinephrine alpha 1A/1B/1D, norepinephrine alpha 2C, norepinephrine beta 1/2, DA D1/2/4/5, GABAA, H3, NET, SERT, and Sigma 1/2.