TABLE 1

Comparison of binding parameters for [3H][Dmt1]DALDA

Saturation binding was carried with [3H][Dmt1]DALDA using membranes prepared from CHO cells transfected with hMOR (CHO-K1/hMOR), SH-SY5Y cells, which natively expresses μ and δ receptors and brain and spinal cord tissues from rats (Sprague-Dawley) and mice (CD-1). Membranes were incubated with [3H][Dmt1]DALDA (0.010-2.000 nM) for 60 min at 25°C. Nonspecific binding was assessed by including 0.1 μM unlabeled [Dmt1]DALDA or 10 μM naloxone. Kd and Bmax were determined by fitting the data to a one-site binding model using nonlinear regression. Data are presented as mean ± S.E.M.; n = number of independent determinations.




Kd

Bmax

n
nM fmol / mg protein
CHO-K1/hMOR 0.199 ± 0.019 926 ± 55 6
SH-SY5Y cells 0.118 ± 0.014 77 ± 10 3
Mouse brain 0.123 ± 0.012 130 ± 9 5
Mouse spinal cord 0.126 ± 0.008 125 ± 5 4
Rat brain 0.104 ± 0.018 160 ± 8 5
Rat spinal cord
0.104 ± 0.014
145 ± 8
5