Pharmacokinetics of iodine-123-IMBA for melanoma imaging
<p>The development of an effective radiopharmaceutical with affinity for malignant melanoma has been a research goal for some time. The early detection of melanoma metastases would greatly improve the therapy outcome for this disease. This article describes the synthesis of radioiodinated IMBA...
Saved in:
| Main Authors: | , , , , |
|---|---|
| Format: | Article (Journal) |
| Language: | English |
| Published: |
January 1997
|
| In: |
Journal of nuclear medicine
Year: 1997, Volume: 38, Issue: 1, Pages: 127-133 |
| ISSN: | 2159-662X |
| Online Access: | Verlag, lizenzpflichtig, Volltext: https://jnm.snmjournals.org/content/38/1/127
|
| Author Notes: | Ciaran Nicholl, Ashour Mohammed, William E. Hull, Bernd Bubeck, Michael Eisenhut |
MARC
| LEADER | 00000caa a2200000 c 4500 | ||
|---|---|---|---|
| 001 | 1911212125 | ||
| 003 | DE-627 | ||
| 005 | 20250716214720.0 | ||
| 007 | cr uuu---uuuuu | ||
| 008 | 241209s1997 xx |||||o 00| ||eng c | ||
| 035 | |a (DE-627)1911212125 | ||
| 035 | |a (DE-599)KXP1911212125 | ||
| 035 | |a (OCoLC)1528014817 | ||
| 040 | |a DE-627 |b ger |c DE-627 |e rda | ||
| 041 | |a eng | ||
| 084 | |a 33 |2 sdnb | ||
| 100 | 1 | |a Nicholl, Ciaran |e VerfasserIn |0 (DE-588)1350414123 |0 (DE-627)1910922919 |4 aut | |
| 245 | 1 | 0 | |a Pharmacokinetics of iodine-123-IMBA for melanoma imaging |c Ciaran Nicholl, Ashour Mohammed, William E. Hull, Bernd Bubeck, Michael Eisenhut |
| 264 | 1 | |c January 1997 | |
| 300 | |a 7 | ||
| 336 | |a Text |b txt |2 rdacontent | ||
| 337 | |a Computermedien |b c |2 rdamedia | ||
| 338 | |a Online-Ressource |b cr |2 rdacarrier | ||
| 500 | |a Gesehen am 09.122024 | ||
| 520 | |a <p>The development of an effective radiopharmaceutical with affinity for malignant melanoma has been a research goal for some time. The early detection of melanoma metastases would greatly improve the therapy outcome for this disease. This article describes the synthesis of radioiodinated IMBA, N-(2-diethylaminoethyl)-3-[<sup>123</sup>I/<sup>131</sup>I]iodo- 4-methoxybenzamide 8, its organ distribution, its comparison with BZA and other benzamides, and demonstrates the scintigraphic efficacy of the title compound with three melanoma patients. <b>Methods:</b> The syntheses and radioiodination of eight benzamide derivatives are described. After intravenous injection into C57BI 6-mice subcutaneously transplanted with B16 melanoma, the organ distribution of the respective benzamides were investigated at 1 and 6 hr. n-octanol/phosphate buffer partition coefficients. The whole-body retention, erythrocyte and serum protein bound fractions of radioiodinated benzamides were measured. <b>Results:</b> While structural changes in the amide substituents of N-(2-dialkylaminoalkyl)- 4-iodobenzamides 2-7 resulted in no improvement in organ distribution compared with BZA, the 3-iodo-4-methoxyphenyl form of IMBA showed high melanoma uptake with significantly higher melanoma/nontarget tissue ratios. Compared with BZA the average ratio improved after 1 hr by a factor of eight and was still four times better after 6 hr. BZA and IMBA exhibit almost identical n-octanol/phosphate buffer partition coefficients, however, IMBA has a faster urinary excretion facilitated by a lower affinity to erythrocytes and serum proteins; this could explain the improved tissue partinioning observed. Scintigraphy of patients with melanoma metastases confirmed the promising characteristics derived from the animal studies <b>Conclusion:</b> Due to rapid background clearance and high melanoma affinity, IMBA showed high tumor contrast already at 4 hr after injection which makes it a promising new radiopharmaceutical for the scintigraphic detection of melanoma metastases.</p> | ||
| 700 | 1 | |a Mohammed, Ashour B. |d 1963- |e VerfasserIn |0 (DE-588)114226436X |0 (DE-627)1001437381 |0 (DE-576)174701128 |4 aut | |
| 700 | 1 | |a Hull, William Edmund |e VerfasserIn |0 (DE-588)1180547306 |0 (DE-627)1067775978 |0 (DE-576)520275551 |4 aut | |
| 700 | 1 | |a Bubeck, Bernd |d 1949- |e VerfasserIn |0 (DE-588)1067692207 |0 (DE-627)819091502 |0 (DE-576)426855493 |4 aut | |
| 700 | 1 | |a Eisenhut, Michael |e VerfasserIn |0 (DE-588)1113306122 |0 (DE-627)867174501 |0 (DE-576)160846080 |4 aut | |
| 773 | 0 | 8 | |i Enthalten in |t Journal of nuclear medicine |d New York, NY : Soc., 1964 |g 38(1997), 1, Seite 127-133 |h Online-Ressource |w (DE-627)325793603 |w (DE-600)2040222-3 |w (DE-576)09475277X |x 2159-662X |7 nnas |a Pharmacokinetics of iodine-123-IMBA for melanoma imaging |
| 773 | 1 | 8 | |g volume:38 |g year:1997 |g number:1 |g pages:127-133 |g extent:7 |a Pharmacokinetics of iodine-123-IMBA for melanoma imaging |
| 856 | 4 | 0 | |u https://jnm.snmjournals.org/content/38/1/127 |x Verlag |z lizenzpflichtig |3 Volltext |
| 951 | |a AR | ||
| 992 | |a 20241209 | ||
| 993 | |a Article | ||
| 994 | |a 1997 | ||
| 998 | |g 1113306122 |a Eisenhut, Michael |m 1113306122:Eisenhut, Michael |d 50000 |e 50000PE1113306122 |k 0/50000/ |p 5 |y j | ||
| 998 | |g 1067692207 |a Bubeck, Bernd |m 1067692207:Bubeck, Bernd |d 50000 |e 50000PB1067692207 |k 0/50000/ |p 4 | ||
| 999 | |a KXP-PPN1911212125 |e 4633364944 | ||
| BIB | |a Y | ||
| SER | |a journal | ||
| JSO | |a {"relHost":[{"physDesc":[{"extent":"Online-Ressource"}],"origin":[{"dateIssuedDisp":"1964-","publisher":"Soc.","dateIssuedKey":"1964","publisherPlace":"New York, NY"}],"id":{"eki":["325793603"],"zdb":["2040222-3"],"issn":["2159-662X","1535-5667"]},"name":{"displayForm":["Society of Nuclear Medicine"]},"pubHistory":["Nachgewiesen 5.1964 -"],"part":{"pages":"127-133","issue":"1","year":"1997","extent":"7","text":"38(1997), 1, Seite 127-133","volume":"38"},"titleAlt":[{"title":"JNM"}],"disp":"Pharmacokinetics of iodine-123-IMBA for melanoma imagingJournal of nuclear medicine","note":["Gesehen am 13.12.2021"],"type":{"bibl":"periodical","media":"Online-Ressource"},"corporate":[{"roleDisplay":"Herausgebendes Organ","display":"Society of Nuclear Medicine","role":"isb"}],"language":["eng"],"recId":"325793603","title":[{"title_sort":"Journal of nuclear medicine","subtitle":"JNM","title":"Journal of nuclear medicine"}]}],"physDesc":[{"extent":"7 S."}],"name":{"displayForm":["Ciaran Nicholl, Ashour Mohammed, William E. Hull, Bernd Bubeck, Michael Eisenhut"]},"id":{"eki":["1911212125"]},"origin":[{"dateIssuedDisp":"January 1997","dateIssuedKey":"1997"}],"recId":"1911212125","language":["eng"],"type":{"bibl":"article-journal","media":"Online-Ressource"},"note":["Gesehen am 09.122024"],"person":[{"family":"Nicholl","given":"Ciaran","display":"Nicholl, Ciaran","roleDisplay":"VerfasserIn","role":"aut"},{"family":"Mohammed","given":"Ashour B.","roleDisplay":"VerfasserIn","display":"Mohammed, Ashour B.","role":"aut"},{"roleDisplay":"VerfasserIn","display":"Hull, William Edmund","role":"aut","family":"Hull","given":"William Edmund"},{"role":"aut","display":"Bubeck, Bernd","roleDisplay":"VerfasserIn","given":"Bernd","family":"Bubeck"},{"display":"Eisenhut, Michael","roleDisplay":"VerfasserIn","role":"aut","family":"Eisenhut","given":"Michael"}],"title":[{"title":"Pharmacokinetics of iodine-123-IMBA for melanoma imaging","title_sort":"Pharmacokinetics of iodine-123-IMBA for melanoma imaging"}]} | ||
| SRT | |a NICHOLLCIAPHARMACOKI1997 | ||