TY - JOUR
T1 - Topographical requirements for delta opioid ligands
T2 - The synthesis and biological properties of a cyclic analogue of deltorphin I
AU - Misicka, Aleksandra
AU - Nikiforovich, Gregory
AU - Lipkowski, Andrzej W.
AU - Horvath, Robert
AU - Davis, Peg
AU - Kramer, Thomas H.
AU - Yamamura, Henry I.
AU - Hruby, Victor J.
PY - 1992/6
Y1 - 1992/6
N2 - A cyclic constrained analogue of deltorphin, {A figure is presented} has been proposed on the basis of an energetically favored model of a delta-selective conformation for deltorphin. The biological properties of this synthetic analogue demonstrate that incorporation of a disulfide bridge into Deltorphin I does not affect its high affinity for delta opioid receptors. The analogue shows low receptor selectivity as a result of a large increase in its affinity for mu receptors when compared to the parent deltorphin.
AB - A cyclic constrained analogue of deltorphin, {A figure is presented} has been proposed on the basis of an energetically favored model of a delta-selective conformation for deltorphin. The biological properties of this synthetic analogue demonstrate that incorporation of a disulfide bridge into Deltorphin I does not affect its high affinity for delta opioid receptors. The analogue shows low receptor selectivity as a result of a large increase in its affinity for mu receptors when compared to the parent deltorphin.
UR - http://www.scopus.com/inward/record.url?scp=0026707633&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=0026707633&partnerID=8YFLogxK
U2 - 10.1016/S0960-894X(01)81195-1
DO - 10.1016/S0960-894X(01)81195-1
M3 - Article
AN - SCOPUS:0026707633
SN - 0960-894X
VL - 2
SP - 547
EP - 552
JO - Bioorganic and Medicinal Chemistry Letters
JF - Bioorganic and Medicinal Chemistry Letters
IS - 6
ER -