TY - JOUR
T1 - Dynorphin(1-10)amide
T2 - A potent and selective analog of dynorphin(1-13)
AU - Woo, Sidney
AU - Garzon, Javier
AU - Sanchez-Blazquez, Pilar
AU - Tulunay, F. Cankat
AU - Chang, Jaw Kang
AU - Loh, Horace H.
PY - 1982
Y1 - 1982
N2 - Dynorphin(1-10)amide was more potent than Dynorphin(1-13) in inhibiting the twitch of the mouse vas deferens (IC50) of Dynorphin(1-10)amide = 0.3 nM and IC50 of Dynorphin (1-13) = 4.0 nM. Binding assaays indicated that two opioid peptides had similar profiles in that they enhanced dihydromorphine (DHM) binding in picomolar concentrations but displaced DHM binding in nanomolar concentrations (IC50 for Dynorphin(1-10)amide = 5 nM). In the mouse tail-flick assay, however, Dynorphin(1-10)-amide showed a more selective action on morphine-induced analgesia. Although Dynorphin(1-10)amide had no significant analgesic activity by itself, it differed from the (1-13) analog by neither potentiating nor antagonizing morphine in naive animals. In tolerant animals, on the other hand, 50 ug of this analog administered icv shifted the ED50 of morphine from 43.0(33.0-55.9) to 17.0 (12.4-23.3). Thus, Dynorphin(1-10)amide appears to be a more potent and selective analog of Dynorphin(1-13).
AB - Dynorphin(1-10)amide was more potent than Dynorphin(1-13) in inhibiting the twitch of the mouse vas deferens (IC50) of Dynorphin(1-10)amide = 0.3 nM and IC50 of Dynorphin (1-13) = 4.0 nM. Binding assaays indicated that two opioid peptides had similar profiles in that they enhanced dihydromorphine (DHM) binding in picomolar concentrations but displaced DHM binding in nanomolar concentrations (IC50 for Dynorphin(1-10)amide = 5 nM). In the mouse tail-flick assay, however, Dynorphin(1-10)-amide showed a more selective action on morphine-induced analgesia. Although Dynorphin(1-10)amide had no significant analgesic activity by itself, it differed from the (1-13) analog by neither potentiating nor antagonizing morphine in naive animals. In tolerant animals, on the other hand, 50 ug of this analog administered icv shifted the ED50 of morphine from 43.0(33.0-55.9) to 17.0 (12.4-23.3). Thus, Dynorphin(1-10)amide appears to be a more potent and selective analog of Dynorphin(1-13).
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U2 - 10.1016/0024-3205(82)90218-1
DO - 10.1016/0024-3205(82)90218-1
M3 - Article
C2 - 6130447
AN - SCOPUS:0020463686
SN - 0024-3205
VL - 31
SP - 1817
EP - 1820
JO - Life Sciences
JF - Life Sciences
IS - 16-17
ER -