. Author manuscript; available in PMC: 2010 Jul 15.

Published in final edited form as: Bioorg Med Chem. 2009 Jun 2;17(14):5044–5053. doi: 10.1016/j.bmc.2009.05.065

Table 2.

Results in the MVD and GPI/LMMP

Assays	MVD	GPI/LMMP	DPDPE Antagonism at 1 µM in the MVD	PL-017 Antagonism at 1 µM in the GPI/LMMP
Compounds	Agonist activity (% inhibition of contraction at 1 µM) or IC₅₀ (nM) ± S.E.M.		DPDPE Antagonism at 1 µM in the MVD	PL-017 Antagonism at 1 µM in the GPI/LMMP
9a	17.9 % at 1 µM	0.7 % at 1 µM	none at 1 µM	none at 1 µM
9b	1266 +/− 355	5164 +/− 2043	--	--
9c	19.5 % at 1 µM	3.1 % at 1 µM	none at 1 µM	none at 1 µM
9d	2.8 % at 1 µM	0 % at 1 µM	none at 1 µM	none at 1 µM
9e	8.3 % at 1 µM	3 % at 1 µM	none at 1 µM	none at 1 µM
9f	0 % at 1 µM	6 % at 1 µM	none at 1 µM	none at 1 µM

Footnotes: DPDPE ([D-Pen², D-Pen ⁵]enkephalin) was used to inhibit MVD contraction by selective activation of the delta opioid receptors in this tissue. Compounds 9a–f (at 1 µM) did not reverse the effect of DPDPE. PL-017 was used to inhibit GPI contraction by selective activation of the μ opioid receptors in this tissue. Compounds 9a–f (at 1 µM) did not reverse the effect of PL-017.