Figure 1. Structure and pharmacologic profile of PG01037.
The chemical structure and summary of our current available information on the pharmacological properties of PG01037 is shown. Mean values for the affinity measurements (Ki values) are expressed as nM. Mean values ± S.E.M. are provided for the human D2 and D3 dopamine receptor with n ≥ 3. The remaining affinity values were obtained from Novascreen through the NIDA Contract N01-DA-8-8839. PG01037 was tested at a concentration of 10 μM in 61 binding assays. For the assays in which PG01037 inhibited binding >50%, mean Ki values were obtained (n=2).
Ki values for the binding to the low affinity state of human D2 and D3 dopamine receptors were obtained using competitive radioligand binding experiments with 125I-IABN as the radiotracer (Luedtke et al., 2000). Maximal intrinsic activity was achieved using the test ligand and the full D2-like dopamine receptor agonist quinpirole at concentrations approximately 10× the Ki values (PG01037, 1000 nM for D2 and 10 nM for D3; quinpirole, 1000 nM for D2 and 100 nM for D3). The percent maximum mitogenesis is based upon dose response curves (one concentration per decade) using a maximum of 10−5 M test drug performed by the Division of Treatment Research and Development (DTRD) of NIDA. The numerical values are the mean ± the S.E.M. and the number in the parentheses is the number of independent experiments (n).