Article Figures & Data
Figures
- FIGURE 1.
Expression of SS and sst1–5 mRNAs in different tissues of wild-type and sst2 knockout mice, as determined by RT-PCR. All mock-reverse-transcribed samples and all controls with no added template showed no PCR products. Marker lanes (M) contain 100-bp DNA ladder. H = hprt; Mw = molecular weight.
- FIGURE 2.
Uptake values of radioactivity after injection of [111In-DTPA-d-Phe1]octreotide (A) and [111In-DTPA]SS-14 (B), expressed as percentage injected dose per gram of tissue (% ID/gram) in pituitary gland, adrenals, pancreas, and thymus of wild-type mice (white bars) and sst2 knockout mice (black bars) (n = 4).
Tables
Specificity Primer Sequence (5′-3′) Expected size (bp) sst1 M1-F817 -gtgatgatggtggtgatggt- 259 M1-R1075 -tcagggcagtggcatagtag- sst2 M2-F694 -atcatcaaggtgaagtcctctg- 376 M2-R1069 -gggtctccgtggtctcatt- sst3 M3-F732 -ctcgtgtcagtgggtacagg- 297 M3-R1028 -cgacgtgatggtcttagcag- sst4 M4-F1317 -ctaggactggctccaaggac- 299 M4-R1615 -agaccgacacagagggaaac- sst5 M5-F722 -gctcagaacgcaaggtgact- 268 M5-R989 -gcatcctccacaccgtatc- Somatostatin MSS15F -gatgctgtcctgccgtct- 290 MSS304R -ccattgctgggttcgagt- hprt MHP513F -tgttggatacaggccagactt- 228 MHP740R -ggccacaggactagaacacc- Position vs. stopcodon.
Tissue sst mRNA sst1 sst2 sst3 sst4 sst5 SS mRNA wt ko wt ko wt ko wt ko wt ko wt ko Brain cortex + + + − + + + + + + + + Pituitary gland + + + − + + + + + + + + Adrenals + + + − + + + + + + + + Thymus − − + − − − + + − − + + Spleen + + − − − − + + − − − − Liver + + + − − − + + + + − − Kidneys + + − − − − + + − − − − Soft tissue + + + − − − + + − − + + Blood (PBMC) + + + − − − + + − − − − wt = wild-type mice; ko = sst2 knockout mice.
- TABLE 3
Tissue Distribution of [111ln-DTPA-d-Phe1]Octreotide in Wild-Type and sst2 Knockout Mice
Tissue Wild type sst2 knockout Without blockade With blockade Without blockade With blockade Pituitary gland 1.2 ± 0.2 0.25 ± 0.04* 0.033 ± 0.037† 0.19 ± 0.03 Adrenals 0.26 ± 0.03 0.12 ± 0.04* 0.045 ± 0.020† 0.11 ± 0.03‡ Thymus 0.30 ± 0.05 0.061 ± 0.020* 0.017 ± 0.003† 0.039 ± 0.010* Pancreas 0.18 ± 0.03 0.035 ± 0.008* 0.007 ± 0.002† 0.014 ± 0.005 Spleen 0.048 ± 0.008 0.074 ± 0.021 0.075 ± 0.006 0.072 ± 0.016 Liver 0.090 ± 0.007 0.19 ± 0.05‡ 0.11 ± 0.01 0.15 ± 0.03 Kidneys 1.4 ± 0.3 1.9 ± 0.4 2.4 ± 0.5 2.3 ± 1.1 Soft tissue 0.004 ± 0.001 0.010 ± 0.006 0.003 ± 0.000 0.009 ± 0.002 Blood 0.004 ± 0.001 0.10 ± 0.00 0.005 ± 0.001 0.011 ± 0.004‡ ↵* P < 0.01 for [111ln-DTPA-d-Phe1]octreotide vs. [111ln-DTPA-d-Phe1]octreotide with blockade.
↵† P < 0.01 for [111ln-DTPA-d-Phe1]octreotide wild type vs. [111ln-DTPA-d-Phe1]octreotide sst2 knockout.
↵‡ P < 0.05 for [111ln-DTPA-d-Phe1]octreotide vs. [111ln-DTPA-d-Phe1]octreotide with blockade.
Values are mean ± SD percentage injected dose per gram of tissue (n = 4 animals per group). Blockade means coinjection of 100 μg octreotide with [111ln-DTPA-d-Phe1]octreotide.
- TABLE 4
Binding Affinity Profiles of SS-28, SS-14, and [DTPA]SS-14 for Human sst1–5 Receptors
Compound Displacement of binding of [125I-LTT]SS-28 sst1 sst2 sst3 sst4 sst5 SS-28 2.5 ± 0.3 2.1 ± 0.3 2.5 ± 0.2 2.2 ± 0.3 2.1 ± 0.4 SS-14 2.1 ± 0.4 0.6 ± 0.1 3.9 ± 1.3 1.9 ± 0.6 11.0 ± 3.5 [DTPA]SS-14 35 ± 1.6 3.9 ± 0.8 7.5 ± 1.3 5.5 ± 1.1 16.0 ± 2.0 [DTPA]octreotide* >10,000 12 ± 2 376 ± 84 >1,000 299 ± 50 ↵* Data are from (20).
Values are mean ± SEM of 3 experiments and represent IC50 values (in nmol/L) of displacement of binding of [125I-Leu8,d-Trp22,Tyr25]SS-28 to cryostat sections of membrane pellets of cells stably expressing sst1 or sst5 (CHO-K1) and sst2, sst3, and sst4 (CCL39 cells), as described in detail previously (20).
Tissue Wild type sst2 knockout Without blockade With blockade Without blockade With blockade Pituitary gland 1.9 ± 0.1 0.24 ± 0.06* 0.26 ± 0.16† 0.43 ± 0.21 Adrenals 0.36 ± 0.03 0.16 ± 0.04* 0.088 ± 0.010† 0.63 ± 0.38* Thymus 0.20 ± 0.00 0.079 ± 0.006* 0.025 ± 0.005† 0.33 ± 0.19* Pancreas 1.2 ± 0.1 0.050 ± 0.008* 0.034 ± 0.011† 0.21 ± 0.15* Spleen 0.081 ± 0.014 0.12 ± 0.02 0.065 ± 0.005 0.32 ± 0.22* Liver 0.076 ± 0.009 0.14 ± 0.03 0.077 ± 0.020 0.44 ± 0.20* Kidneys 19.3 ± 4.8 18.6 ± 2.8 20.5 ± 3.2 22.6 ± 6.6 Soft tissue 0.006 ± 0.001 0.023 ± 0.004* 0.010 ± 0.004 0.085 ± 0.045* Blood 0.011 ± 0.001 0.036 ± 0.007* 0.005 ± 0.001 0.011 ± 0.002* ↵* P < 0.01 for [111ln-DTPA]SS-14 vs. [111ln-DTPA]SS-14 with blockade.
↵† P < 0.01 for [111ln-DTPA]SS-14 wild type vs. [111ln-DTPA]SS-14 sst2 knockout.
Values are mean ± SD percentage injected dose per gram of tissue (n = 4 animals per group). Blockade means coinjection of 100 μg SS-14 with [111ln-DTPA]SS-14.
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