Evaluation of radioiodinated ethopabate as a potential tumor targeting agent
Overexpression of folate synthesis and folate receptor in a wide variety of tumors was reported. As a result, folate derivatives have emerged as a potential candidate for tumor imaging and therapy. Ethopabate is a structural analogue of para-aminobenzoic acid (PABA), a precursor of folic acid. Ethop...
Ausführliche Beschreibung
Gespeichert in:
| Autor*in: |
Aboumanei, Mohamed H. [verfasserIn] |
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| Format: |
E-Artikel |
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| Sprache: |
Englisch |
| Erschienen: |
2022transfer abstract |
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| Schlagwörter: |
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| Übergeordnetes Werk: |
Enthalten in: Time-dependent shape factors for fractured reservoir simulation: Effect of stress sensitivity in matrix system - Wang, Lu ELSEVIER, 2018, a journal of nuclear and radiation techniques and their applications in the physical, chemical, biological, medical, earth, planetary, environmental and engineering science, Amsterdam [u.a.] |
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| Übergeordnetes Werk: |
volume:180 ; year:2022 ; pages:0 |
| Links: |
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| DOI / URN: |
10.1016/j.apradiso.2021.110063 |
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ELV056326580 |
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| 245 | 1 | 0 | |a Evaluation of radioiodinated ethopabate as a potential tumor targeting agent |
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| 520 | |a Overexpression of folate synthesis and folate receptor in a wide variety of tumors was reported. As a result, folate derivatives have emerged as a potential candidate for tumor imaging and therapy. Ethopabate is a structural analogue of para-aminobenzoic acid (PABA), a precursor of folic acid. Ethopabate was radiolabeled with radioiodine-131 (131I) via direct electrophilic substitution reaction. Several factors that might affect the radiolabeling yield were studied. Paper chromatography was utilized for testing and evaluation of [131I]iodoethopabate, and HPLC was used as a co-chromatographic tool to confirm the radiochemical yield. The biodistribution of [131I]iodoethopabate in normal and tumor-bearing mice was investigated. The radioiodination of ethopabate resulted in a radiochemical yield of 93.70 ± 0.19%. The biodistribution data revealed that [131I]iodoethopabate was taken up by tumors with promising target/non-target (T/NT) ratios. Where, the tumor to-blood ratios were 3.30 ± 0.40 and 4.06 ± 0.10 at 1 and 4 h post injection, respectively. As a result of these findings, [131I]iodoethopabate appears to have excellent tumor uptake and adequate stability to be used for diagnostic purpose in the future. | ||
| 520 | |a Overexpression of folate synthesis and folate receptor in a wide variety of tumors was reported. As a result, folate derivatives have emerged as a potential candidate for tumor imaging and therapy. Ethopabate is a structural analogue of para-aminobenzoic acid (PABA), a precursor of folic acid. Ethopabate was radiolabeled with radioiodine-131 (131I) via direct electrophilic substitution reaction. Several factors that might affect the radiolabeling yield were studied. Paper chromatography was utilized for testing and evaluation of [131I]iodoethopabate, and HPLC was used as a co-chromatographic tool to confirm the radiochemical yield. The biodistribution of [131I]iodoethopabate in normal and tumor-bearing mice was investigated. The radioiodination of ethopabate resulted in a radiochemical yield of 93.70 ± 0.19%. The biodistribution data revealed that [131I]iodoethopabate was taken up by tumors with promising target/non-target (T/NT) ratios. Where, the tumor to-blood ratios were 3.30 ± 0.40 and 4.06 ± 0.10 at 1 and 4 h post injection, respectively. As a result of these findings, [131I]iodoethopabate appears to have excellent tumor uptake and adequate stability to be used for diagnostic purpose in the future. | ||
| 650 | 7 | |a Radioiodine-131 |2 Elsevier | |
| 650 | 7 | |a Solid tumor |2 Elsevier | |
| 650 | 7 | |a Ethopabate |2 Elsevier | |
| 650 | 7 | |a Radioiodination |2 Elsevier | |
| 650 | 7 | |a Biodistribution |2 Elsevier | |
| 700 | 1 | |a Mahmoud, Ashgan F. |4 oth | |
| 700 | 1 | |a Motaleb, Mohamed A. |4 oth | |
| 773 | 0 | 8 | |i Enthalten in |n Elsevier Science |a Wang, Lu ELSEVIER |t Time-dependent shape factors for fractured reservoir simulation: Effect of stress sensitivity in matrix system |d 2018 |d a journal of nuclear and radiation techniques and their applications in the physical, chemical, biological, medical, earth, planetary, environmental and engineering science |g Amsterdam [u.a.] |w (DE-627)ELV001919369 |
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10.1016/j.apradiso.2021.110063 doi /cbs_pica/cbs_olc/import_discovery/elsevier/einzuspielen/GBV00000000001646.pica (DE-627)ELV056326580 (ELSEVIER)S0969-8043(21)00454-1 DE-627 ger DE-627 rakwb eng 660 VZ 38.51 bkl 57.36 bkl Aboumanei, Mohamed H. verfasserin aut Evaluation of radioiodinated ethopabate as a potential tumor targeting agent 2022transfer abstract nicht spezifiziert zzz rdacontent nicht spezifiziert z rdamedia nicht spezifiziert zu rdacarrier Overexpression of folate synthesis and folate receptor in a wide variety of tumors was reported. As a result, folate derivatives have emerged as a potential candidate for tumor imaging and therapy. Ethopabate is a structural analogue of para-aminobenzoic acid (PABA), a precursor of folic acid. Ethopabate was radiolabeled with radioiodine-131 (131I) via direct electrophilic substitution reaction. Several factors that might affect the radiolabeling yield were studied. Paper chromatography was utilized for testing and evaluation of [131I]iodoethopabate, and HPLC was used as a co-chromatographic tool to confirm the radiochemical yield. The biodistribution of [131I]iodoethopabate in normal and tumor-bearing mice was investigated. The radioiodination of ethopabate resulted in a radiochemical yield of 93.70 ± 0.19%. The biodistribution data revealed that [131I]iodoethopabate was taken up by tumors with promising target/non-target (T/NT) ratios. Where, the tumor to-blood ratios were 3.30 ± 0.40 and 4.06 ± 0.10 at 1 and 4 h post injection, respectively. As a result of these findings, [131I]iodoethopabate appears to have excellent tumor uptake and adequate stability to be used for diagnostic purpose in the future. Overexpression of folate synthesis and folate receptor in a wide variety of tumors was reported. As a result, folate derivatives have emerged as a potential candidate for tumor imaging and therapy. Ethopabate is a structural analogue of para-aminobenzoic acid (PABA), a precursor of folic acid. Ethopabate was radiolabeled with radioiodine-131 (131I) via direct electrophilic substitution reaction. Several factors that might affect the radiolabeling yield were studied. Paper chromatography was utilized for testing and evaluation of [131I]iodoethopabate, and HPLC was used as a co-chromatographic tool to confirm the radiochemical yield. The biodistribution of [131I]iodoethopabate in normal and tumor-bearing mice was investigated. The radioiodination of ethopabate resulted in a radiochemical yield of 93.70 ± 0.19%. The biodistribution data revealed that [131I]iodoethopabate was taken up by tumors with promising target/non-target (T/NT) ratios. Where, the tumor to-blood ratios were 3.30 ± 0.40 and 4.06 ± 0.10 at 1 and 4 h post injection, respectively. As a result of these findings, [131I]iodoethopabate appears to have excellent tumor uptake and adequate stability to be used for diagnostic purpose in the future. Radioiodine-131 Elsevier Solid tumor Elsevier Ethopabate Elsevier Radioiodination Elsevier Biodistribution Elsevier Mahmoud, Ashgan F. oth Motaleb, Mohamed A. oth Enthalten in Elsevier Science Wang, Lu ELSEVIER Time-dependent shape factors for fractured reservoir simulation: Effect of stress sensitivity in matrix system 2018 a journal of nuclear and radiation techniques and their applications in the physical, chemical, biological, medical, earth, planetary, environmental and engineering science Amsterdam [u.a.] (DE-627)ELV001919369 volume:180 year:2022 pages:0 https://doi.org/10.1016/j.apradiso.2021.110063 Volltext GBV_USEFLAG_U GBV_ELV SYSFLAG_U SSG-OLC-PHA SSG-OPC-GGO 38.51 Geologie fossiler Brennstoffe VZ 57.36 Erdölgewinnung Erdgasgewinnung VZ AR 180 2022 0 |
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10.1016/j.apradiso.2021.110063 doi /cbs_pica/cbs_olc/import_discovery/elsevier/einzuspielen/GBV00000000001646.pica (DE-627)ELV056326580 (ELSEVIER)S0969-8043(21)00454-1 DE-627 ger DE-627 rakwb eng 660 VZ 38.51 bkl 57.36 bkl Aboumanei, Mohamed H. verfasserin aut Evaluation of radioiodinated ethopabate as a potential tumor targeting agent 2022transfer abstract nicht spezifiziert zzz rdacontent nicht spezifiziert z rdamedia nicht spezifiziert zu rdacarrier Overexpression of folate synthesis and folate receptor in a wide variety of tumors was reported. As a result, folate derivatives have emerged as a potential candidate for tumor imaging and therapy. Ethopabate is a structural analogue of para-aminobenzoic acid (PABA), a precursor of folic acid. Ethopabate was radiolabeled with radioiodine-131 (131I) via direct electrophilic substitution reaction. Several factors that might affect the radiolabeling yield were studied. Paper chromatography was utilized for testing and evaluation of [131I]iodoethopabate, and HPLC was used as a co-chromatographic tool to confirm the radiochemical yield. The biodistribution of [131I]iodoethopabate in normal and tumor-bearing mice was investigated. The radioiodination of ethopabate resulted in a radiochemical yield of 93.70 ± 0.19%. The biodistribution data revealed that [131I]iodoethopabate was taken up by tumors with promising target/non-target (T/NT) ratios. Where, the tumor to-blood ratios were 3.30 ± 0.40 and 4.06 ± 0.10 at 1 and 4 h post injection, respectively. As a result of these findings, [131I]iodoethopabate appears to have excellent tumor uptake and adequate stability to be used for diagnostic purpose in the future. Overexpression of folate synthesis and folate receptor in a wide variety of tumors was reported. As a result, folate derivatives have emerged as a potential candidate for tumor imaging and therapy. Ethopabate is a structural analogue of para-aminobenzoic acid (PABA), a precursor of folic acid. Ethopabate was radiolabeled with radioiodine-131 (131I) via direct electrophilic substitution reaction. Several factors that might affect the radiolabeling yield were studied. Paper chromatography was utilized for testing and evaluation of [131I]iodoethopabate, and HPLC was used as a co-chromatographic tool to confirm the radiochemical yield. The biodistribution of [131I]iodoethopabate in normal and tumor-bearing mice was investigated. The radioiodination of ethopabate resulted in a radiochemical yield of 93.70 ± 0.19%. The biodistribution data revealed that [131I]iodoethopabate was taken up by tumors with promising target/non-target (T/NT) ratios. Where, the tumor to-blood ratios were 3.30 ± 0.40 and 4.06 ± 0.10 at 1 and 4 h post injection, respectively. As a result of these findings, [131I]iodoethopabate appears to have excellent tumor uptake and adequate stability to be used for diagnostic purpose in the future. Radioiodine-131 Elsevier Solid tumor Elsevier Ethopabate Elsevier Radioiodination Elsevier Biodistribution Elsevier Mahmoud, Ashgan F. oth Motaleb, Mohamed A. oth Enthalten in Elsevier Science Wang, Lu ELSEVIER Time-dependent shape factors for fractured reservoir simulation: Effect of stress sensitivity in matrix system 2018 a journal of nuclear and radiation techniques and their applications in the physical, chemical, biological, medical, earth, planetary, environmental and engineering science Amsterdam [u.a.] (DE-627)ELV001919369 volume:180 year:2022 pages:0 https://doi.org/10.1016/j.apradiso.2021.110063 Volltext GBV_USEFLAG_U GBV_ELV SYSFLAG_U SSG-OLC-PHA SSG-OPC-GGO 38.51 Geologie fossiler Brennstoffe VZ 57.36 Erdölgewinnung Erdgasgewinnung VZ AR 180 2022 0 |
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10.1016/j.apradiso.2021.110063 doi /cbs_pica/cbs_olc/import_discovery/elsevier/einzuspielen/GBV00000000001646.pica (DE-627)ELV056326580 (ELSEVIER)S0969-8043(21)00454-1 DE-627 ger DE-627 rakwb eng 660 VZ 38.51 bkl 57.36 bkl Aboumanei, Mohamed H. verfasserin aut Evaluation of radioiodinated ethopabate as a potential tumor targeting agent 2022transfer abstract nicht spezifiziert zzz rdacontent nicht spezifiziert z rdamedia nicht spezifiziert zu rdacarrier Overexpression of folate synthesis and folate receptor in a wide variety of tumors was reported. As a result, folate derivatives have emerged as a potential candidate for tumor imaging and therapy. Ethopabate is a structural analogue of para-aminobenzoic acid (PABA), a precursor of folic acid. Ethopabate was radiolabeled with radioiodine-131 (131I) via direct electrophilic substitution reaction. Several factors that might affect the radiolabeling yield were studied. Paper chromatography was utilized for testing and evaluation of [131I]iodoethopabate, and HPLC was used as a co-chromatographic tool to confirm the radiochemical yield. The biodistribution of [131I]iodoethopabate in normal and tumor-bearing mice was investigated. The radioiodination of ethopabate resulted in a radiochemical yield of 93.70 ± 0.19%. The biodistribution data revealed that [131I]iodoethopabate was taken up by tumors with promising target/non-target (T/NT) ratios. Where, the tumor to-blood ratios were 3.30 ± 0.40 and 4.06 ± 0.10 at 1 and 4 h post injection, respectively. As a result of these findings, [131I]iodoethopabate appears to have excellent tumor uptake and adequate stability to be used for diagnostic purpose in the future. Overexpression of folate synthesis and folate receptor in a wide variety of tumors was reported. As a result, folate derivatives have emerged as a potential candidate for tumor imaging and therapy. Ethopabate is a structural analogue of para-aminobenzoic acid (PABA), a precursor of folic acid. Ethopabate was radiolabeled with radioiodine-131 (131I) via direct electrophilic substitution reaction. Several factors that might affect the radiolabeling yield were studied. Paper chromatography was utilized for testing and evaluation of [131I]iodoethopabate, and HPLC was used as a co-chromatographic tool to confirm the radiochemical yield. The biodistribution of [131I]iodoethopabate in normal and tumor-bearing mice was investigated. The radioiodination of ethopabate resulted in a radiochemical yield of 93.70 ± 0.19%. The biodistribution data revealed that [131I]iodoethopabate was taken up by tumors with promising target/non-target (T/NT) ratios. Where, the tumor to-blood ratios were 3.30 ± 0.40 and 4.06 ± 0.10 at 1 and 4 h post injection, respectively. As a result of these findings, [131I]iodoethopabate appears to have excellent tumor uptake and adequate stability to be used for diagnostic purpose in the future. Radioiodine-131 Elsevier Solid tumor Elsevier Ethopabate Elsevier Radioiodination Elsevier Biodistribution Elsevier Mahmoud, Ashgan F. oth Motaleb, Mohamed A. oth Enthalten in Elsevier Science Wang, Lu ELSEVIER Time-dependent shape factors for fractured reservoir simulation: Effect of stress sensitivity in matrix system 2018 a journal of nuclear and radiation techniques and their applications in the physical, chemical, biological, medical, earth, planetary, environmental and engineering science Amsterdam [u.a.] (DE-627)ELV001919369 volume:180 year:2022 pages:0 https://doi.org/10.1016/j.apradiso.2021.110063 Volltext GBV_USEFLAG_U GBV_ELV SYSFLAG_U SSG-OLC-PHA SSG-OPC-GGO 38.51 Geologie fossiler Brennstoffe VZ 57.36 Erdölgewinnung Erdgasgewinnung VZ AR 180 2022 0 |
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10.1016/j.apradiso.2021.110063 doi /cbs_pica/cbs_olc/import_discovery/elsevier/einzuspielen/GBV00000000001646.pica (DE-627)ELV056326580 (ELSEVIER)S0969-8043(21)00454-1 DE-627 ger DE-627 rakwb eng 660 VZ 38.51 bkl 57.36 bkl Aboumanei, Mohamed H. verfasserin aut Evaluation of radioiodinated ethopabate as a potential tumor targeting agent 2022transfer abstract nicht spezifiziert zzz rdacontent nicht spezifiziert z rdamedia nicht spezifiziert zu rdacarrier Overexpression of folate synthesis and folate receptor in a wide variety of tumors was reported. As a result, folate derivatives have emerged as a potential candidate for tumor imaging and therapy. Ethopabate is a structural analogue of para-aminobenzoic acid (PABA), a precursor of folic acid. Ethopabate was radiolabeled with radioiodine-131 (131I) via direct electrophilic substitution reaction. Several factors that might affect the radiolabeling yield were studied. Paper chromatography was utilized for testing and evaluation of [131I]iodoethopabate, and HPLC was used as a co-chromatographic tool to confirm the radiochemical yield. The biodistribution of [131I]iodoethopabate in normal and tumor-bearing mice was investigated. The radioiodination of ethopabate resulted in a radiochemical yield of 93.70 ± 0.19%. The biodistribution data revealed that [131I]iodoethopabate was taken up by tumors with promising target/non-target (T/NT) ratios. Where, the tumor to-blood ratios were 3.30 ± 0.40 and 4.06 ± 0.10 at 1 and 4 h post injection, respectively. As a result of these findings, [131I]iodoethopabate appears to have excellent tumor uptake and adequate stability to be used for diagnostic purpose in the future. Overexpression of folate synthesis and folate receptor in a wide variety of tumors was reported. As a result, folate derivatives have emerged as a potential candidate for tumor imaging and therapy. Ethopabate is a structural analogue of para-aminobenzoic acid (PABA), a precursor of folic acid. Ethopabate was radiolabeled with radioiodine-131 (131I) via direct electrophilic substitution reaction. Several factors that might affect the radiolabeling yield were studied. Paper chromatography was utilized for testing and evaluation of [131I]iodoethopabate, and HPLC was used as a co-chromatographic tool to confirm the radiochemical yield. The biodistribution of [131I]iodoethopabate in normal and tumor-bearing mice was investigated. The radioiodination of ethopabate resulted in a radiochemical yield of 93.70 ± 0.19%. The biodistribution data revealed that [131I]iodoethopabate was taken up by tumors with promising target/non-target (T/NT) ratios. Where, the tumor to-blood ratios were 3.30 ± 0.40 and 4.06 ± 0.10 at 1 and 4 h post injection, respectively. As a result of these findings, [131I]iodoethopabate appears to have excellent tumor uptake and adequate stability to be used for diagnostic purpose in the future. Radioiodine-131 Elsevier Solid tumor Elsevier Ethopabate Elsevier Radioiodination Elsevier Biodistribution Elsevier Mahmoud, Ashgan F. oth Motaleb, Mohamed A. oth Enthalten in Elsevier Science Wang, Lu ELSEVIER Time-dependent shape factors for fractured reservoir simulation: Effect of stress sensitivity in matrix system 2018 a journal of nuclear and radiation techniques and their applications in the physical, chemical, biological, medical, earth, planetary, environmental and engineering science Amsterdam [u.a.] (DE-627)ELV001919369 volume:180 year:2022 pages:0 https://doi.org/10.1016/j.apradiso.2021.110063 Volltext GBV_USEFLAG_U GBV_ELV SYSFLAG_U SSG-OLC-PHA SSG-OPC-GGO 38.51 Geologie fossiler Brennstoffe VZ 57.36 Erdölgewinnung Erdgasgewinnung VZ AR 180 2022 0 |
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10.1016/j.apradiso.2021.110063 doi /cbs_pica/cbs_olc/import_discovery/elsevier/einzuspielen/GBV00000000001646.pica (DE-627)ELV056326580 (ELSEVIER)S0969-8043(21)00454-1 DE-627 ger DE-627 rakwb eng 660 VZ 38.51 bkl 57.36 bkl Aboumanei, Mohamed H. verfasserin aut Evaluation of radioiodinated ethopabate as a potential tumor targeting agent 2022transfer abstract nicht spezifiziert zzz rdacontent nicht spezifiziert z rdamedia nicht spezifiziert zu rdacarrier Overexpression of folate synthesis and folate receptor in a wide variety of tumors was reported. As a result, folate derivatives have emerged as a potential candidate for tumor imaging and therapy. Ethopabate is a structural analogue of para-aminobenzoic acid (PABA), a precursor of folic acid. Ethopabate was radiolabeled with radioiodine-131 (131I) via direct electrophilic substitution reaction. Several factors that might affect the radiolabeling yield were studied. Paper chromatography was utilized for testing and evaluation of [131I]iodoethopabate, and HPLC was used as a co-chromatographic tool to confirm the radiochemical yield. The biodistribution of [131I]iodoethopabate in normal and tumor-bearing mice was investigated. The radioiodination of ethopabate resulted in a radiochemical yield of 93.70 ± 0.19%. The biodistribution data revealed that [131I]iodoethopabate was taken up by tumors with promising target/non-target (T/NT) ratios. Where, the tumor to-blood ratios were 3.30 ± 0.40 and 4.06 ± 0.10 at 1 and 4 h post injection, respectively. As a result of these findings, [131I]iodoethopabate appears to have excellent tumor uptake and adequate stability to be used for diagnostic purpose in the future. Overexpression of folate synthesis and folate receptor in a wide variety of tumors was reported. As a result, folate derivatives have emerged as a potential candidate for tumor imaging and therapy. Ethopabate is a structural analogue of para-aminobenzoic acid (PABA), a precursor of folic acid. Ethopabate was radiolabeled with radioiodine-131 (131I) via direct electrophilic substitution reaction. Several factors that might affect the radiolabeling yield were studied. Paper chromatography was utilized for testing and evaluation of [131I]iodoethopabate, and HPLC was used as a co-chromatographic tool to confirm the radiochemical yield. The biodistribution of [131I]iodoethopabate in normal and tumor-bearing mice was investigated. The radioiodination of ethopabate resulted in a radiochemical yield of 93.70 ± 0.19%. The biodistribution data revealed that [131I]iodoethopabate was taken up by tumors with promising target/non-target (T/NT) ratios. Where, the tumor to-blood ratios were 3.30 ± 0.40 and 4.06 ± 0.10 at 1 and 4 h post injection, respectively. As a result of these findings, [131I]iodoethopabate appears to have excellent tumor uptake and adequate stability to be used for diagnostic purpose in the future. Radioiodine-131 Elsevier Solid tumor Elsevier Ethopabate Elsevier Radioiodination Elsevier Biodistribution Elsevier Mahmoud, Ashgan F. oth Motaleb, Mohamed A. oth Enthalten in Elsevier Science Wang, Lu ELSEVIER Time-dependent shape factors for fractured reservoir simulation: Effect of stress sensitivity in matrix system 2018 a journal of nuclear and radiation techniques and their applications in the physical, chemical, biological, medical, earth, planetary, environmental and engineering science Amsterdam [u.a.] (DE-627)ELV001919369 volume:180 year:2022 pages:0 https://doi.org/10.1016/j.apradiso.2021.110063 Volltext GBV_USEFLAG_U GBV_ELV SYSFLAG_U SSG-OLC-PHA SSG-OPC-GGO 38.51 Geologie fossiler Brennstoffe VZ 57.36 Erdölgewinnung Erdgasgewinnung VZ AR 180 2022 0 |
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Evaluation of radioiodinated ethopabate as a potential tumor targeting agent |
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Overexpression of folate synthesis and folate receptor in a wide variety of tumors was reported. As a result, folate derivatives have emerged as a potential candidate for tumor imaging and therapy. Ethopabate is a structural analogue of para-aminobenzoic acid (PABA), a precursor of folic acid. Ethopabate was radiolabeled with radioiodine-131 (131I) via direct electrophilic substitution reaction. Several factors that might affect the radiolabeling yield were studied. Paper chromatography was utilized for testing and evaluation of [131I]iodoethopabate, and HPLC was used as a co-chromatographic tool to confirm the radiochemical yield. The biodistribution of [131I]iodoethopabate in normal and tumor-bearing mice was investigated. The radioiodination of ethopabate resulted in a radiochemical yield of 93.70 ± 0.19%. The biodistribution data revealed that [131I]iodoethopabate was taken up by tumors with promising target/non-target (T/NT) ratios. Where, the tumor to-blood ratios were 3.30 ± 0.40 and 4.06 ± 0.10 at 1 and 4 h post injection, respectively. As a result of these findings, [131I]iodoethopabate appears to have excellent tumor uptake and adequate stability to be used for diagnostic purpose in the future. |
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Overexpression of folate synthesis and folate receptor in a wide variety of tumors was reported. As a result, folate derivatives have emerged as a potential candidate for tumor imaging and therapy. Ethopabate is a structural analogue of para-aminobenzoic acid (PABA), a precursor of folic acid. Ethopabate was radiolabeled with radioiodine-131 (131I) via direct electrophilic substitution reaction. Several factors that might affect the radiolabeling yield were studied. Paper chromatography was utilized for testing and evaluation of [131I]iodoethopabate, and HPLC was used as a co-chromatographic tool to confirm the radiochemical yield. The biodistribution of [131I]iodoethopabate in normal and tumor-bearing mice was investigated. The radioiodination of ethopabate resulted in a radiochemical yield of 93.70 ± 0.19%. The biodistribution data revealed that [131I]iodoethopabate was taken up by tumors with promising target/non-target (T/NT) ratios. Where, the tumor to-blood ratios were 3.30 ± 0.40 and 4.06 ± 0.10 at 1 and 4 h post injection, respectively. As a result of these findings, [131I]iodoethopabate appears to have excellent tumor uptake and adequate stability to be used for diagnostic purpose in the future. |
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Overexpression of folate synthesis and folate receptor in a wide variety of tumors was reported. As a result, folate derivatives have emerged as a potential candidate for tumor imaging and therapy. Ethopabate is a structural analogue of para-aminobenzoic acid (PABA), a precursor of folic acid. Ethopabate was radiolabeled with radioiodine-131 (131I) via direct electrophilic substitution reaction. Several factors that might affect the radiolabeling yield were studied. Paper chromatography was utilized for testing and evaluation of [131I]iodoethopabate, and HPLC was used as a co-chromatographic tool to confirm the radiochemical yield. The biodistribution of [131I]iodoethopabate in normal and tumor-bearing mice was investigated. The radioiodination of ethopabate resulted in a radiochemical yield of 93.70 ± 0.19%. The biodistribution data revealed that [131I]iodoethopabate was taken up by tumors with promising target/non-target (T/NT) ratios. Where, the tumor to-blood ratios were 3.30 ± 0.40 and 4.06 ± 0.10 at 1 and 4 h post injection, respectively. As a result of these findings, [131I]iodoethopabate appears to have excellent tumor uptake and adequate stability to be used for diagnostic purpose in the future. |
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