-transparent.png){kind=logo}
AR-M100613 ([I]-Dmt-c[-D-Orn-2-Nal-D-Pro-D-Ala-]) is the iodinated analog of a cyclic casomorphin previously shown to be a potent antagonist at the delta opioid receptor. Specific [125I]AR-M100613 binding to rat whole brain membranes was saturable, reversible, and best fit to a one-site model (Kd = 0.080 +/- 0.008 nM, Bmax = 45.2 +/- 4.4 fmol/mg protein). [125I]AR-M100613 binding was displaced with high affinity by the delta opioid receptor ligands SNC-80, Deltorphin II and DPDPE but not the mu or kappa-selective receptor ligands DAMGO and U69593. Residual non-selective binding of [125I]AR-M 100613 to mu opioid receptors is blocked by the addition of CTOP to the assay buffer. [35S]GTPgammaS binding assays indicate that AR-M100613 is a potent, selective, and reversible antagonist for delta opioid receptors in rat brain membranes. The high-affinity, high specific activity, low nonspecific binding and antagonist profile of [125I]AR-M100613 favor its use as a radiochemical probe for delta opioid receptors.
G L Fraser, and
M Labarre, and
C Godbout, and
J Butterworth, and
P B Clarke, and
K Payza, and
R Schmidt
September 1991,
The Journal of pharmacology and experimental therapeutics,
G L Fraser, and
M Labarre, and
C Godbout, and
J Butterworth, and
P B Clarke, and
K Payza, and
R Schmidt
January 1993,
Life sciences,
G L Fraser, and
M Labarre, and
C Godbout, and
J Butterworth, and
P B Clarke, and
K Payza, and
R Schmidt
January 1999,
The Journal of pharmacology and experimental therapeutics,
G L Fraser, and
M Labarre, and
C Godbout, and
J Butterworth, and
P B Clarke, and
K Payza, and
R Schmidt
October 1993,
Neurochemistry international,
G L Fraser, and
M Labarre, and
C Godbout, and
J Butterworth, and
P B Clarke, and
K Payza, and
R Schmidt
May 1988,
European journal of pharmacology,
G L Fraser, and
M Labarre, and
C Godbout, and
J Butterworth, and
P B Clarke, and
K Payza, and
R Schmidt
August 2003,
Life sciences,
G L Fraser, and
M Labarre, and
C Godbout, and
J Butterworth, and
P B Clarke, and
K Payza, and
R Schmidt
January 2001,
Neuropharmacology,
G L Fraser, and
M Labarre, and
C Godbout, and
J Butterworth, and
P B Clarke, and
K Payza, and
R Schmidt
January 1991,
Peptides,
G L Fraser, and
M Labarre, and
C Godbout, and
J Butterworth, and
P B Clarke, and
K Payza, and
R Schmidt
July 1981,
European journal of pharmacology,
G L Fraser, and
M Labarre, and
C Godbout, and
J Butterworth, and
P B Clarke, and
K Payza, and
R Schmidt
June 1984,
Life sciences,
