Table 2 Functional activity of Dezocine at human κ-, rat μ, or rat δ-opioid receptors.

From: Pharmacological Characterization of Dezocine, a Potent Analgesic Acting as a κ Partial Agonist and μ Partial Agonist

Compounds

Agonist activity

Antagonist activity

MOR

KOR

DOR

MOR

KOR

DOR

EC50 (nM)

Emax (%)

EC50 (nM)

Emax (%)

EC50 (nM)

Emax (%)

Ke (nM)

Ke (nM)

Ke (nM)

DAMGO

16.1 ± 0.3

240.7 ± 33.8

c

c

c

c

c

c

c

U50,488 H

c

c

5.6 ± 1.2

198.9 ± 7.5

c

c

c

c

c

DPDPE

c

c

c

c

1.4 ± 0.2

231.3 ± 7.1

c

c

c

Dezocine

b

45.8 ± 1.1d

b

33.6 ± 2.4d

b

26.1 ± 1.0d

10.4 ± 4.9

324.1 ± 23.6

a

  1. Membranes were incubated with varying concentrations of ligands in the presence of 0.1 nM [35S]GTPγS. Data are expressed as the mean ± SEM for at least three independent experiments performed in triplicate.
  2. aNot tested because of low affinity at DOR. bLow stimulation at 10 μM. cNot applicable. dThe agonist efficacy at 10 μM.
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