TABLE 2

Ability of hBRS-3-selective analogs [d-Tyr6, (R)-Apa11-4Cl, Phe13, Nle14]Bn(6-14) (peptide 7) and the nonselective ligand [d-Tyr6, β-Ala11, Phe13, Nle14]Bn(6-14) (peptide 1) to interact with various gastrointestinal hormone/neurotransmitter receptors

AR42J cells (1 × 106 cells/ml), dispersed rat acini (1 pancreas/10 ml), and CHO cells that were stably transfected with hVPAC1-R (0.2 × 106 cells/ml) or hVPAC2-R (3.0 × 106 cells/ml), were incubated with 50 pM of the indicated 125I-ligand or 0.6 nM of [N-methyl-3H]scopolamine methyl chloride for 60 min as specified under Materials and Methods. Results are the percentage of the total saturable binding with or without 1 μM peptide 1 or peptide 7 (Table 1). All results are the means ± S.E.M. from at least four experiments, and in each experiment each value was performed in duplicate.


Cells Used

Ligand Added

125I-Ligand Saturably Bound
1 μM Peptide 1
1 μM Peptide 7
% Control
AR42J 125I-PACAP-27 104 ± 2 101 ± 3
125I-BH-CCK-8 109 ± 7 94 ± 1
125I-Somatostatin-14 83 ± 5 98 ± 6
125I-BH-Substance P 100 ± 12 104 ± 7
125I-[Tyr4]Bn 0* 50 ± 3*
Stably transfected CHO cells
hVPAC1-R 125I-VIP 97 ± 2 96 ± 4
hVPAC2-R 125I-PACAP 109 ± 5 91 ± 5
Rat pancreatic acini 125I-BH-CCK-8 95 ± 6 102 ± 3

[3H]Methyl scopolamine
100 ± 7
113 ± 7
  • h, human; VPAC, vasoactive intestinal peptide/pituitary adenylate cyclase activating peptide receptor.

  • * P < 0.01 compared with no additions (i.e., control) (paired Student's t test).