. Author manuscript; available in PMC: 2015 Sep 1.

Published in final edited form as: Bioorg Med Chem. 2014 Jul 29;22(17):4581–4586. doi: 10.1016/j.bmc.2014.07.033

Table 2.

GPI and MVD assay of ‘carba’-carfentanil and N-formylnormorphine

No.	Compound	GPI^a			MVD^a
No.	Compound	IC₅₀ [nM]	K_e^μ [nM]	K_e^κ [nM]	IC₅₀ [nM]
8a	c-carfentanil (cis)		4050 ± 1050	2980 ± 560	inactive
8b	c-carfentanil (trans)	116 ± 7 (IC₂₅)^b			3890 ± 350 (IC₃₅)^b
3	carfentanil^c	0.019 ± 0.002			17 ± 8
9	N-formylnormorphine		1240 ± 10	1890 ± 300	> 10,000
10	morphine	29.3 ± 2.2			155 ± 31

Mean of 3–4 determinations ± SEM.

Partial agonist.⁵

Data taken from ref.³².