Table 3 In vitro functional activities of corydine (1) and corydaline (2) to the MOR.

From: Identification and characterization of plant-derived alkaloids, corydine and corydaline, as novel mu opioid receptor agonists

Compound

G protein activationa

β-arrestin2 recruitmentb

EC50 (µM)

%stim

EC50 (µM)

%stim

Corydine (1)

0.51 ± 0.11*

102 ± 6

–c

–c

Corydaline (2)

1.50 ± 0.44

104 ± 6

–c

–c

DAMGO

0.015 ± 0.002

100

0.34 ± 0.02

100

  1. aDetermined in the [35S]GTPγS binding assay using CHO-hMOR cell membranes.
  2. bDetermined in the PathHunter β‐arrestin2 recruitment assay with U2OS cells co‐expressing the hMOR and the enzyme acceptor tagged β‐arrestin2 fusion protein. Efficacies are expressed as percentage stimulation (% stim.) relative to DAMGO (reference MOR agonist).
  3. c–denotes no measurable activity. Values are means ± SEM (n = 3–4 independent experiments performed in duplicate). *P < 0.05 for corydine (1) vs. corydaline (2) (unpaired t-test).
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