Figure 1.
Structures of opioid antagonists nor-BNI, GNTI, JDTic and naltrexone.
Table 1.
Binding affinities of nor-BNI, GNTI and JDTic for 46 neurotransmitter receptors and transporters, determined by radioligand displacement.
Figure 2.
GNTI enhances maximal Ca2+ mobilization by noradrenaline at α1A-AR without affecting potency (A); maximal PI hydrolysis is not increased (B).
Some intermediate curves have been omitted for clarity. Error bars represent mean ± S.E.M. For raw data, see Datasets S1 and S2.
Figure 3.
GNTI is a weak antagonist of acetylcholine at M1-R (A); JDTic weakly inhibits the noradrenaline transporter (B).
Error bars represent mean ± S.E.M. For raw data, see Datasets S3 and S4.
Figure 4.
Antagonism of N/OFQ at NOP by JDTic (A) and SB-612,111 (B): inhibition of cAMP production.
Error bars represent mean ± S.E.M. For raw data, see Dataset S5.
Table 2.
Mean permeation rates and efflux ratios in Caco-2 cell monolayers.
Figure 5.
Structural similarities between GNTI and α1-AR ligands.