Journal: Bioconjugate Chemistry

Article Title: Design, Synthesis, and Preliminary Evaluation of [ 68 Ga]Ga-NOTA-Insulin as a PET Probe in an Alzheimer’s Disease Mouse Model

doi: 10.1021/acs.bioconjchem.2c00126

Figure Lengend Snippet: Uptake (SUV) of [ 68 Ga]Ga-NOTA-insulin in the brain (A–D) and heart (E–H) of AD ( n = 6), AD (+S961) ( n = 5), normal ( n = 4) and normal (+S961) ( n = 3) mice at 5, 10, 15, and 20 min post intravenous (i.v.) administration. The uptake (SUV) data were extracted from microPET/CT images by drawing the region of interest (ROI) at different time points. * p value < 0.05 AD vs normal, # p value < 0.05 AD (+S961) vs normal (+S961), and § p value < 0.05 normal vs normal (+S961).

Article Snippet: In the case of the [ 68 Ga]Ga-NOTA-insulin group, the radiolabeled insulin was coinjected without or with 10 μg of the insulin receptor inhibitor, S961 acetate (MedChemExpress, Monmouth Junction, NJ) per animal.

Techniques:

Journal: Bioconjugate Chemistry

Article Title: Design, Synthesis, and Preliminary Evaluation of [ 68 Ga]Ga-NOTA-Insulin as a PET Probe in an Alzheimer’s Disease Mouse Model

doi: 10.1021/acs.bioconjchem.2c00126

Figure Lengend Snippet: Boxplots of uptake (SUV) and the biodistribution of [ 68 Ga]Ga-NOTA-insulin in different brain regions of AD ( n = 12), AD (+S961) ( n = 5), normal ( n = 13), and normal (+S961) ( n = 3) mice at 30 min post intravenous (i.v.) administration. The y-axis is presented on the log10 scale. Statistically significant differences indicated by symbols above (** = P < 0.01, * = P < 0.05).

Article Snippet: In the case of the [ 68 Ga]Ga-NOTA-insulin group, the radiolabeled insulin was coinjected without or with 10 μg of the insulin receptor inhibitor, S961 acetate (MedChemExpress, Monmouth Junction, NJ) per animal.

Techniques:

Journal: Bioconjugate Chemistry

Article Title: Design, Synthesis, and Preliminary Evaluation of [ 68 Ga]Ga-NOTA-Insulin as a PET Probe in an Alzheimer’s Disease Mouse Model

doi: 10.1021/acs.bioconjchem.2c00126

Figure Lengend Snippet: Boxplots of uptake (SUV) and biodistribution of [ 68 Ga]Ga-NOTA-insulin in AD ( n = 12), AD (+S961) ( n = 5), normal ( n = 13), and normal (+S961) ( n = 3) mice at 30 min post intravenous (i.v.) administration. The y -axis is presented on the log10 scale. Statistically significant differences indicated by symbols above (** = P < 0.01, * = P < 0.05).

Article Snippet: In the case of the [ 68 Ga]Ga-NOTA-insulin group, the radiolabeled insulin was coinjected without or with 10 μg of the insulin receptor inhibitor, S961 acetate (MedChemExpress, Monmouth Junction, NJ) per animal.

Techniques:

Journal: Bioconjugate Chemistry

Article Title: Design, Synthesis, and Preliminary Evaluation of [ 68 Ga]Ga-NOTA-Insulin as a PET Probe in an Alzheimer’s Disease Mouse Model

doi: 10.1021/acs.bioconjchem.2c00126

Figure Lengend Snippet: Boxplots of uptake (SUV) and biodistribution of [ 68 Ga]Ga-NOTA-insulin in the excretory organs of AD ( n = 12), AD (+S961) ( n = 5), normal ( n = 13), and normal (+S961) ( n = 3) mice at 30 min post intravenous (i.v.) administration. The y -axis is presented on the log10 scale. Statistically significant differences indicated by symbols above (* = P < 0.05).

Article Snippet: In the case of the [ 68 Ga]Ga-NOTA-insulin group, the radiolabeled insulin was coinjected without or with 10 μg of the insulin receptor inhibitor, S961 acetate (MedChemExpress, Monmouth Junction, NJ) per animal.

Techniques:

Journal: Bioconjugate Chemistry

Article Title: Design, Synthesis, and Preliminary Evaluation of [ 68 Ga]Ga-NOTA-Insulin as a PET Probe in an Alzheimer’s Disease Mouse Model

doi: 10.1021/acs.bioconjchem.2c00126

Figure Lengend Snippet: Representative microPET/CT images of [ 68 Ga]Ga-NOTA-insulin in (A) normal and AD mice and (B) normal (+S961) and AD (+S961) mice at different time points post intravenous (i.v.) administration.

Article Snippet: In the case of the [ 68 Ga]Ga-NOTA-insulin group, the radiolabeled insulin was coinjected without or with 10 μg of the insulin receptor inhibitor, S961 acetate (MedChemExpress, Monmouth Junction, NJ) per animal.

Techniques:

Journal: Bioconjugate Chemistry

Article Title: Design, Synthesis, and Preliminary Evaluation of [ 68 Ga]Ga-NOTA-Insulin as a PET Probe in an Alzheimer’s Disease Mouse Model

doi: 10.1021/acs.bioconjchem.2c00126

Figure Lengend Snippet: Uptake (SUV) of [ 68 Ga]Ga-NOTA-Insulin without and with the Insulin Receptor Inhibitor (S961) in the Brain of AD (APP/PS1) and Normal (B6SJL) Mice Post Intravenous Administration Measured via microPET/CT Image Analysis and Drawing the Region of Interest (ROI) on Whole Mice Brain and Whole Heart at Different Time Points

Article Snippet: In the case of the [ 68 Ga]Ga-NOTA-insulin group, the radiolabeled insulin was coinjected without or with 10 μg of the insulin receptor inhibitor, S961 acetate (MedChemExpress, Monmouth Junction, NJ) per animal.

Techniques:

Journal: Bioconjugate Chemistry

Article Title: Design, Synthesis, and Preliminary Evaluation of [ 68 Ga]Ga-NOTA-Insulin as a PET Probe in an Alzheimer’s Disease Mouse Model

doi: 10.1021/acs.bioconjchem.2c00126

Figure Lengend Snippet: Uptake (SUV) of [ 68 Ga]Ga-NOTA-Insulin without and with the Insulin Receptor Inhibitor (+S961) in the Heart of AD (APP/PS1) and Normal (B6SJL) Mice Post Intravenous Administration Measured via microPET/CT Image Analysis and Drawing the Region of Interest (ROI) on Whole Mice Brain and Whole Heart at Different Time Points

Article Snippet: In the case of the [ 68 Ga]Ga-NOTA-insulin group, the radiolabeled insulin was coinjected without or with 10 μg of the insulin receptor inhibitor, S961 acetate (MedChemExpress, Monmouth Junction, NJ) per animal.

Techniques:

Journal: Bioconjugate Chemistry

Article Title: Design, Synthesis, and Preliminary Evaluation of [ 68 Ga]Ga-NOTA-Insulin as a PET Probe in an Alzheimer’s Disease Mouse Model

doi: 10.1021/acs.bioconjchem.2c00126

Figure Lengend Snippet: Uptake (SUV) of [ 68 Ga]Ga-NOTA-Insulin without and with the Insulin Receptor Inhibitor (+S961) in Different Brain Regions of Normal (B6SJL) and AD (APP/PS1) Mouse Models at 30 min Post Intravenous Administration Measured via Organ/Tissue Harvesting

Article Snippet: In the case of the [ 68 Ga]Ga-NOTA-insulin group, the radiolabeled insulin was coinjected without or with 10 μg of the insulin receptor inhibitor, S961 acetate (MedChemExpress, Monmouth Junction, NJ) per animal.

Techniques:

Journal: Bioconjugate Chemistry

Article Title: Design, Synthesis, and Preliminary Evaluation of [ 68 Ga]Ga-NOTA-Insulin as a PET Probe in an Alzheimer’s Disease Mouse Model

doi: 10.1021/acs.bioconjchem.2c00126

Figure Lengend Snippet: Uptake (SUV) of [ 68 Ga]Ga-NOTA-Insulin without and with the Insulin Receptor Inhibitor (+S961) in Normal (B6SJL) and AD (APP/PS1) Mouse Models at 30 min Post Intravenous Administration Measured via Organ/Tissue Harvesting

Article Snippet: In the case of the [ 68 Ga]Ga-NOTA-insulin group, the radiolabeled insulin was coinjected without or with 10 μg of the insulin receptor inhibitor, S961 acetate (MedChemExpress, Monmouth Junction, NJ) per animal.

Techniques:

Journal: Neural Regeneration Research

Article Title: Hippocampal insulin resistance and the Sirtuin 1 signaling pathway in diabetes-induced cognitive dysfunction

doi: 10.4103/1673-5374.313051

Figure Lengend Snippet: Insulin receptor inhibitor S961 aggravates the impairment of cognitive function in diabetic model rats and inhibits insulin signaling and SIRT1 expression. (A) Schematic diagram of the experimental schedule. After 8 weeks of diabetes, diabetic rats were administered S961 or vehicle for 7 days, and rat behaviors were investigated by MWM ( n = 15 per group). (B–H) Behavioral data. (B) The learning curve. (C–E) The escape latency time on days 2 (C), 3 (D), and 4 (E). (F) The time spent in the target quadrant, (G) the number of times crossing the expected platform location, and (H) is the percentage of swimming distance in the target quadrant. (I–L) S961 decreased the expression of p-IR (optical density ratio to IR) (J), p-IRS-1 (optical density ratio to IRS-1) (K), and SIRT1 (optical density ratio to GAPDH) (L) in the hippocampus of diabetic model rats with cognitive decline ( n = 6 per group). Data are presented as the mean ± SEM. * P < 0.05, ** P < 0.01 (one-way analysis of variance). The experiments were repeated three times. DIA: Diabetic rats; GAPDH: glyceraldehyde-3-phosphate dehydrogenase; IR: insulin receptor; IRS-1: insulin receptor substrate-1; MWM: Morris water maze test; NS: non-streptozotocin rats; p-IR: phospho-insulin receptor; p-IRS-1: phospho-insulin receptor substrate-1; SIRT1: Sirtuin 1.

Article Snippet: S961 (1 μg/20 μL; MedChemExpress, Monmouth Junction, NJ, USA), an insulin receptor inhibitor, was administered to another 15 diabetic model rats once daily for 7 days, and the same number of diabetic model rats received intranasal saline (20 μL).

Techniques: Expressing