Abstract
Analogues of naltrindole and N1′-methylnaltrindole having radioiodine in the 7′-position of the indole ring have been prepared for evaluation as delta opioid receptor ligands. The no-carrier-added radiosyntheses were conducted by Cu(I) assisted nucleophilic exchange of radioiodide for bromide under reducing conditions at 190 °C. A combination of HPLC and solid-phase extraction gave the 125I- or 123I-labeled products in satisfactory yields (47%) with high radiochemical purities (>98%) and high specific activities (125I: 43-68 GBq/μmol, 1155-1833 mCi/μmol; 123I: >92GBq/μmol, 2500mCi/μmol).
| Original language | English (US) |
|---|---|
| Pages (from-to) | 599-606 |
| Number of pages | 8 |
| Journal | Nuclear Medicine and Biology |
| Volume | 22 |
| Issue number | 5 |
| DOIs | |
| State | Published - 1995 |
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ASJC Scopus subject areas
- Cancer Research
- Molecular Medicine
- Radiology Nuclear Medicine and imaging
Cite this
Synthesis of radioiodinated naltrindole analogues : Ligands for studies of delta opioid receptors. / Kinter, Chris M.; Lever, John R.
In: Nuclear Medicine and Biology, Vol. 22, No. 5, 1995, p. 599-606.Research output: Contribution to journal › Article
}
TY - JOUR
T1 - Synthesis of radioiodinated naltrindole analogues
T2 - Ligands for studies of delta opioid receptors
AU - Kinter, Chris M.
AU - Lever, John R.
PY - 1995
Y1 - 1995
N2 - Analogues of naltrindole and N1′-methylnaltrindole having radioiodine in the 7′-position of the indole ring have been prepared for evaluation as delta opioid receptor ligands. The no-carrier-added radiosyntheses were conducted by Cu(I) assisted nucleophilic exchange of radioiodide for bromide under reducing conditions at 190 °C. A combination of HPLC and solid-phase extraction gave the 125I- or 123I-labeled products in satisfactory yields (47%) with high radiochemical purities (>98%) and high specific activities (125I: 43-68 GBq/μmol, 1155-1833 mCi/μmol; 123I: >92GBq/μmol, 2500mCi/μmol).
AB - Analogues of naltrindole and N1′-methylnaltrindole having radioiodine in the 7′-position of the indole ring have been prepared for evaluation as delta opioid receptor ligands. The no-carrier-added radiosyntheses were conducted by Cu(I) assisted nucleophilic exchange of radioiodide for bromide under reducing conditions at 190 °C. A combination of HPLC and solid-phase extraction gave the 125I- or 123I-labeled products in satisfactory yields (47%) with high radiochemical purities (>98%) and high specific activities (125I: 43-68 GBq/μmol, 1155-1833 mCi/μmol; 123I: >92GBq/μmol, 2500mCi/μmol).
UR - http://www.scopus.com/inward/record.url?scp=0029094002&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=0029094002&partnerID=8YFLogxK
U2 - 10.1016/0969-8051(94)00149-E
DO - 10.1016/0969-8051(94)00149-E
M3 - Article
C2 - 7581169
AN - SCOPUS:0029094002
VL - 22
SP - 599
EP - 606
JO - Nuclear Medicine and Biology
JF - Nuclear Medicine and Biology
SN - 0969-8051
IS - 5
ER -