TY - JOUR
T1 - A new approach to enhance bioavailability of biologically active peptides
T2 - conjugation of a δ opioid agonist to β-cyclodextrin
AU - Hristova-Kazmierski, Maria K.
AU - Horan, P.
AU - Davis, P.
AU - Yamamura, H. I.
AU - Kramer, T.
AU - Horvath, R.
AU - Kazmierski, W. M.
AU - Porreca, F.
AU - Hruby, Victor J.
PY - 1993/5
Y1 - 1993/5
N2 - The cyclic δ opioid against [p-I-Phe4]DPDPE, 1, was conjugated to mono-6-amino-permethyl-β-cyclodextrin at the C-terminus to improve the bioavailability of 1. In the rat brain building assay, the conjugate 8 showed an IC50 = 134 nM vs. a δ ligand and IC50 > 10 μM at the μ receptor, making it less potent and selective than 1. However, 8 shows antinociceptive properties (i.v.) in the mouse tail flick test and prolonged activity.
AB - The cyclic δ opioid against [p-I-Phe4]DPDPE, 1, was conjugated to mono-6-amino-permethyl-β-cyclodextrin at the C-terminus to improve the bioavailability of 1. In the rat brain building assay, the conjugate 8 showed an IC50 = 134 nM vs. a δ ligand and IC50 > 10 μM at the μ receptor, making it less potent and selective than 1. However, 8 shows antinociceptive properties (i.v.) in the mouse tail flick test and prolonged activity.
UR - https://www.scopus.com/pages/publications/0027191259
UR - https://www.scopus.com/pages/publications/0027191259#tab=citedBy
U2 - 10.1016/S0960-894X(00)80675-7
DO - 10.1016/S0960-894X(00)80675-7
M3 - Article
AN - SCOPUS:0027191259
SN - 0960-894X
VL - 3
SP - 831
EP - 834
JO - Bioorganic and Medicinal Chemistry Letters
JF - Bioorganic and Medicinal Chemistry Letters
IS - 5
ER -