Skip to main content
. Author manuscript; available in PMC: 2019 Aug 13.
Published in final edited form as: J Med Chem. 2018 Aug 29;61(17):7525–7545. doi: 10.1021/acs.jmedchem.8b00673

Table 6.

Inhibition of Agonist-Stimulated [35S]GTPγS Binding in Cloned Human μ, δ, and κ Opioid Receptors, Importance of the Isopropyl and 7-Hydroxy-d-Tic Groups

graphic file with name nihms-1043744-t0021.jpg
compd Ke (nM)a
μ/κ δ/κ
μ, DAMGO δ, DPDPE κ, U69,593
34 >3000 >3000 113 ± 21 >27 >27
35 586 ± 130 >3000 5.58 ± 1.6 105 >538
36 >3000 >3000 387 ± 89 >8 >8
37 431 ± 110 >3000 20.5 ± 4.6 21 >146
38 153 ± 37 >3000 11.1 ± 2.9 14 >270
39 569 ± 110 >3000 17.2 ± 5.8 33 >174
a

Data are mean ± SEM of at least three independent experiments conducted in duplicate. None of the compounds had agonist activity at 10 μM.