Neuropathic Pain: The Paradox of Dynorphin

TABLE 1.

Ki Values for Dynorphin Variants with Respect to Human Opioid Receptors

Variant hKORa Ki (nM) hDOR hMOR
a KOR, kappa opioid receptor; DOR delta opioid receptor; MOR, mu opioid receptor.
b Values represent the mean from two independent experiments. The values regarding the KOR were determined with 1.8 nM [3H]U69,593 (Kd=1.4 nM); those regarding the DOR were determined with 1.5 nM [3H]pCl-DPDPE (Kd=1.3 nM); and those regarding the MOR were determined with 0.45 nM [3H]DAMGO (Kd=0.37 nM).
Dynorphin A 5.3b 182 6.9
Y-G-G-F-L-R-R-I-R-P-K-L-K-W-D-N-Q
Dynorphin A (1-13) 6.4 141 16.4
Y-G-G-F-L-R-R-I-R-P-K-L-K
Dynorphin A (2-17) >10,000 >10,000 >10,000
G-G-F-L-R-R-I-R-P-K-L-K-W-D-N-Q
Dynorphin A (2-13) >10,000 >10,000 >10,000
G-G-F-L-R-R-I-R-P-K-L-K

This Article

  1. MI August 2001 vol. 1 no. 3 160-167