Table 3. Functional activities of Dmt-l(or d)Tic analogues.

	[35S]GTP-γ-S binding						MVD(δ)		GPI(μ)
	hDORa			rMORa			agonist	antagonist	agonist	antagonist
no.	log EC50b	EC50 (nM)c	Emax (%)d	log EC50b	EC50 (nM)c	Emax (%)d	IC50 (nM)e	Ke (nM)f	IC50 (nM)e	Ke (nM)f
3		nr			nr		20%	5.0 ± 3	740 ± 220
4		nr			nr		1.6%	0.79 ± 0.6	350 ± 90
5g		0.48	18		6.2	16	74 ± 14		0%	nr
6	–8.09 ± 0.07	8.1	128	–9.04 ± 0.28	0.90	40	42+6		82 ± 9
7		nr			nr		14%	150 ± 20	27%	nr
8	–7.84 ± 0.14	15	47	–8.35 ± 0.17	4.5	82	86 ± 29		720 ± 210
9		nr			nr		0%	nr	4%	nr
10		nr			nr		810 ± 140	nr	6%	nr
Dmt-Tic-NH2h								42	>10 μM
Dmt-Tic-Phe-Phe-NH2i								0.21 ± 0.04	18 ± 2

^aExpressed in CHO cells.

^bLogarithmic values determined from the nonlinear regression analysis of data collected from at least three independent experiments.

^cAntilogarithmic value of the respective EC₅₀ values.

^dNet total bound/basal binding ×100 ± SEM.

^eConcentration at 50% inhibition of muscle contraction at electrically stimulated isolated tissues or % inhibition of contraction height at 1 μM.

^fAntagonist.

^gSee ref (7).

^hSee ref (1).

ⁱSee refs (9) and (10). nr: no response.