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. Author manuscript; available in PMC: 2016 Oct 25.
Published in final edited form as: Annu Rev Pharmacol Toxicol. 2013;53:557–580. doi: 10.1146/annurev-pharmtox-010510-100456

Table 2.

Binding affinity assays and biological assays of β-methyl-2′,6′-dimethyltyrosine (trimethyltyrosine, TMT) analogs of Tyr-Tic

Compound Binding affinity assays Biological assays
vs[3H]pCl-DPDPE(δ) IC50 (nM) [3H]DAMGO(μ) IC50 (nM) MVD (δ) GPI (μ)
H-L-Tyr-L-Tic-OHa 190 ± 50 28,000 ± 2,900 – –
[2S,3S]TMT-L-Tic-OHb 120 ± 27 >80,000 ND ND
[2S,3R]TMT-L-Tic-OH 9.3 ± 0.53 35,000 ± 18,000 1 μM shifts DPDPE 547-fold 1 μM does not antagonize PL-017 30% at 30 μM
[2R,3S]TMT-L-Tic >10,000 >80,000 ND ND
[2R,3R]TMT-L-Tic >10,000 >80,000 ND ND
a

Data from Reference 43.

b

Data from Reference 45.

Abbreviations: DAMGO, [D-Ala2,N-MePhe4,Gly-ol]enkephalin; DPDPE, c[D-Pen2,D-Pen5]enkephalin; GPI, guinea pig ileum; MVD, mouse vas deferens; ND, not determined; TMT, β-methyl-2′,6′-dimethyltyrosine (trimethyltyrosine).