TY - JOUR
T1 - Synthesis of radioiodinated naltrindole analogues
T2 - Ligands for studies of delta opioid receptors
AU - Kinter, Chris M.
AU - Lever, John R.
N1 - Funding Information:
Acknowledgements-This research was supported by USPHS grants NIDA DA 08816 and NIDA DA 08870, and by a postdoctoral fellowship (CMK) through NC1 CA 09199. The NMR facility was established by USPHS Grants GM 27512 and lSlO-RR06262.
PY - 1995/7
Y1 - 1995/7
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).
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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 - International journal of radiation applications and instrumentation. Part B, Nuclear medicine and biology
JF - International journal of radiation applications and instrumentation. Part B, Nuclear medicine and biology
SN - 0969-8051
IS - 5
ER -