Preparation and evaluation of a new 99mTc labeled bombesin derivative for tumor imaging
A variety of human tumors like prostate and breast cancer express bombesin receptors. Due to this a new bombesin analogue was labeled with 99m Tc via HYNIC and tricine as a coligand and investigated further. Peptide was synthesized on a solid phase using Fmoc strategy. Labeling with 99m Tc was perfo...
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| Veröffentlicht in: | Journal of radioanalytical and nuclear chemistry 2010, Vol.283 (1), p.181-187 |
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| container_title | Journal of radioanalytical and nuclear chemistry |
| container_volume | 283 |
| creator | Sadeghzadeh, N. Gandomkar, M. Najafi, R. Shafiei, M. Sadat Ebrahimi, S. E. Shafiee, A. Larijani, B. |
| description | A variety of human tumors like prostate and breast cancer express bombesin receptors. Due to this a new bombesin analogue was labeled with
99m
Tc via HYNIC and tricine as a coligand and investigated further. Peptide was synthesized on a solid phase using Fmoc strategy. Labeling with
99m
Tc was performed at 100 °C for 10 min and radiochemical analysis involved ITLC and HPLC methods. The stability of radiopeptide was checked in the presence of human serum at 37 °C up to 24 h. Internalization was studied with the human GRP receptor cell line PC-3. The biodistribution was studied in mice. Labeling yield of >98% was obtained corresponding to a specific activity of ~80.9 GBq/μmol. Radiopeptide internalization into PC-3 cells was moderate and specific (10.7 ± 1.2% at 4 h). A high and specific GRP receptor expressing mouse tumor and pancreas uptake (1.12 ± 0.08 and 1.04 ± 0.11% ID/g after 1 h respectively) was also determined. |
| doi_str_mv | 10.1007/s10967-009-0138-z |
| format | Article |
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99m
Tc via HYNIC and tricine as a coligand and investigated further. Peptide was synthesized on a solid phase using Fmoc strategy. Labeling with
99m
Tc was performed at 100 °C for 10 min and radiochemical analysis involved ITLC and HPLC methods. The stability of radiopeptide was checked in the presence of human serum at 37 °C up to 24 h. Internalization was studied with the human GRP receptor cell line PC-3. The biodistribution was studied in mice. Labeling yield of >98% was obtained corresponding to a specific activity of ~80.9 GBq/μmol. Radiopeptide internalization into PC-3 cells was moderate and specific (10.7 ± 1.2% at 4 h). A high and specific GRP receptor expressing mouse tumor and pancreas uptake (1.12 ± 0.08 and 1.04 ± 0.11% ID/g after 1 h respectively) was also determined.</description><identifier>ISSN: 0236-5731</identifier><identifier>EISSN: 1588-2780</identifier><identifier>DOI: 10.1007/s10967-009-0138-z</identifier><language>eng</language><publisher>Dordrecht: Springer Netherlands</publisher><subject>Chemistry ; Chemistry and Materials Science ; Diagnostic Radiology ; Glass fiber reinforced plastics ; Hadrons ; Heavy Ions ; Inorganic Chemistry ; Nuclear Chemistry ; Nuclear Physics ; Physical Chemistry</subject><ispartof>Journal of radioanalytical and nuclear chemistry, 2010, Vol.283 (1), p.181-187</ispartof><rights>Akadémiai Kiadó, Budapest, Hungary 2009</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c165z-5a7a938f887131ddc7efe01f9e2cc1d018101013898dad1c85395012e50f643</citedby><cites>FETCH-LOGICAL-c165z-5a7a938f887131ddc7efe01f9e2cc1d018101013898dad1c85395012e50f643</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://link.springer.com/content/pdf/10.1007/s10967-009-0138-z$$EPDF$$P50$$Gspringer$$H</linktopdf><linktohtml>$$Uhttps://link.springer.com/10.1007/s10967-009-0138-z$$EHTML$$P50$$Gspringer$$H</linktohtml><link.rule.ids>314,780,784,27923,27924,41487,42556,51318</link.rule.ids></links><search><creatorcontrib>Sadeghzadeh, N.</creatorcontrib><creatorcontrib>Gandomkar, M.</creatorcontrib><creatorcontrib>Najafi, R.</creatorcontrib><creatorcontrib>Shafiei, M.</creatorcontrib><creatorcontrib>Sadat Ebrahimi, S. E.</creatorcontrib><creatorcontrib>Shafiee, A.</creatorcontrib><creatorcontrib>Larijani, B.</creatorcontrib><title>Preparation and evaluation of a new 99mTc labeled bombesin derivative for tumor imaging</title><title>Journal of radioanalytical and nuclear chemistry</title><addtitle>J Radioanal Nucl Chem</addtitle><description>A variety of human tumors like prostate and breast cancer express bombesin receptors. Due to this a new bombesin analogue was labeled with
99m
Tc via HYNIC and tricine as a coligand and investigated further. Peptide was synthesized on a solid phase using Fmoc strategy. Labeling with
99m
Tc was performed at 100 °C for 10 min and radiochemical analysis involved ITLC and HPLC methods. The stability of radiopeptide was checked in the presence of human serum at 37 °C up to 24 h. Internalization was studied with the human GRP receptor cell line PC-3. The biodistribution was studied in mice. Labeling yield of >98% was obtained corresponding to a specific activity of ~80.9 GBq/μmol. Radiopeptide internalization into PC-3 cells was moderate and specific (10.7 ± 1.2% at 4 h). A high and specific GRP receptor expressing mouse tumor and pancreas uptake (1.12 ± 0.08 and 1.04 ± 0.11% ID/g after 1 h respectively) was also determined.</description><subject>Chemistry</subject><subject>Chemistry and Materials Science</subject><subject>Diagnostic Radiology</subject><subject>Glass fiber reinforced plastics</subject><subject>Hadrons</subject><subject>Heavy Ions</subject><subject>Inorganic Chemistry</subject><subject>Nuclear Chemistry</subject><subject>Nuclear Physics</subject><subject>Physical Chemistry</subject><issn>0236-5731</issn><issn>1588-2780</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2010</creationdate><recordtype>article</recordtype><recordid>eNp9kE9LAzEQxYMoWKsfwFtunlZnNt0mOUrxHwgKFjyGNDtbtuwmNelW7Kc3ZT17mWHg92bmPcauEW4RQN4lBD2XBYAuAIUqDidsgpVSRSkVnLIJlGJeVFLgObtIaQMZVEpM2Od7pK2NdtcGz62vOe1tN4xjaLjlnr651v3S8c6uqKOar0K_otR6XlNs9xndE29C5Luhz7Xt7br160t21tgu0dVfn7KPx4fl4rl4fXt6Wdy_Fg7n1aGorLRaqEYpiQLr2klqCLDRVDqHNaBCwKMhrWpbo1OV0BVgSRU085mYsptx6zaGr4HSzvRtctR11lMYktEgtZgphZnEkXQxpBSpMduYX40_BsEcEzRjgiYHY44HzSFrylGTMuvXFM0mDNFnO_-IfgGRMnQs</recordid><startdate>2010</startdate><enddate>2010</enddate><creator>Sadeghzadeh, N.</creator><creator>Gandomkar, M.</creator><creator>Najafi, R.</creator><creator>Shafiei, M.</creator><creator>Sadat Ebrahimi, S. E.</creator><creator>Shafiee, A.</creator><creator>Larijani, B.</creator><general>Springer Netherlands</general><scope>AAYXX</scope><scope>CITATION</scope><scope>7SR</scope><scope>7U5</scope><scope>8BQ</scope><scope>8FD</scope><scope>H8D</scope><scope>JG9</scope><scope>L7M</scope></search><sort><creationdate>2010</creationdate><title>Preparation and evaluation of a new 99mTc labeled bombesin derivative for tumor imaging</title><author>Sadeghzadeh, N. ; Gandomkar, M. ; Najafi, R. ; Shafiei, M. ; Sadat Ebrahimi, S. E. ; Shafiee, A. ; Larijani, B.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c165z-5a7a938f887131ddc7efe01f9e2cc1d018101013898dad1c85395012e50f643</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2010</creationdate><topic>Chemistry</topic><topic>Chemistry and Materials Science</topic><topic>Diagnostic Radiology</topic><topic>Glass fiber reinforced plastics</topic><topic>Hadrons</topic><topic>Heavy Ions</topic><topic>Inorganic Chemistry</topic><topic>Nuclear Chemistry</topic><topic>Nuclear Physics</topic><topic>Physical Chemistry</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Sadeghzadeh, N.</creatorcontrib><creatorcontrib>Gandomkar, M.</creatorcontrib><creatorcontrib>Najafi, R.</creatorcontrib><creatorcontrib>Shafiei, M.</creatorcontrib><creatorcontrib>Sadat Ebrahimi, S. E.</creatorcontrib><creatorcontrib>Shafiee, A.</creatorcontrib><creatorcontrib>Larijani, B.</creatorcontrib><collection>CrossRef</collection><collection>Engineered Materials Abstracts</collection><collection>Solid State and Superconductivity Abstracts</collection><collection>METADEX</collection><collection>Technology Research Database</collection><collection>Aerospace Database</collection><collection>Materials Research Database</collection><collection>Advanced Technologies Database with Aerospace</collection><jtitle>Journal of radioanalytical and nuclear chemistry</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Sadeghzadeh, N.</au><au>Gandomkar, M.</au><au>Najafi, R.</au><au>Shafiei, M.</au><au>Sadat Ebrahimi, S. E.</au><au>Shafiee, A.</au><au>Larijani, B.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Preparation and evaluation of a new 99mTc labeled bombesin derivative for tumor imaging</atitle><jtitle>Journal of radioanalytical and nuclear chemistry</jtitle><stitle>J Radioanal Nucl Chem</stitle><date>2010</date><risdate>2010</risdate><volume>283</volume><issue>1</issue><spage>181</spage><epage>187</epage><pages>181-187</pages><issn>0236-5731</issn><eissn>1588-2780</eissn><abstract>A variety of human tumors like prostate and breast cancer express bombesin receptors. Due to this a new bombesin analogue was labeled with
99m
Tc via HYNIC and tricine as a coligand and investigated further. Peptide was synthesized on a solid phase using Fmoc strategy. Labeling with
99m
Tc was performed at 100 °C for 10 min and radiochemical analysis involved ITLC and HPLC methods. The stability of radiopeptide was checked in the presence of human serum at 37 °C up to 24 h. Internalization was studied with the human GRP receptor cell line PC-3. The biodistribution was studied in mice. Labeling yield of >98% was obtained corresponding to a specific activity of ~80.9 GBq/μmol. Radiopeptide internalization into PC-3 cells was moderate and specific (10.7 ± 1.2% at 4 h). A high and specific GRP receptor expressing mouse tumor and pancreas uptake (1.12 ± 0.08 and 1.04 ± 0.11% ID/g after 1 h respectively) was also determined.</abstract><cop>Dordrecht</cop><pub>Springer Netherlands</pub><doi>10.1007/s10967-009-0138-z</doi><tpages>7</tpages></addata></record> |
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| subjects | Chemistry Chemistry and Materials Science Diagnostic Radiology Glass fiber reinforced plastics Hadrons Heavy Ions Inorganic Chemistry Nuclear Chemistry Nuclear Physics Physical Chemistry |
| title | Preparation and evaluation of a new 99mTc labeled bombesin derivative for tumor imaging |
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