The method to synthesize a high affinity muscarinic receptor antagonist (R,S)I-QNB[(R)-(-)-1-azabicyclo [2,2,2]oct-3-yl-(S)-(+)-α-hydroxy-α-(4-[127I]iodophenyl)-α-phenyl acetate] from 4-nitrobenzophenone with impro...The method to synthesize a high affinity muscarinic receptor antagonist (R,S)I-QNB[(R)-(-)-1-azabicyclo [2,2,2]oct-3-yl-(S)-(+)-α-hydroxy-α-(4-[127I]iodophenyl)-α-phenyl acetate] from 4-nitrobenzophenone with improvement compared to literatures was reported in this article. IR, MS and 1HNMR characterized the final product. (R,S)131I-QNB was prepared using Cu(I) assisted iodine exchange labeling, and showed by TLC that the radiolabeling yield(RLY) was over 80%, and radiochemical purity(RCP) was over 95%. Stability of the labeled compound was also determined. It was found that (R,S)131I-QNB dried by nitrogen blowing can stay at 4-10℃ for a week without change of RCP.展开更多
The pharmacokinetics local model was used to evaluate renal function. Some typical kinds of renal function cases, normal or disorder, were selected to be imaged with SPECT and those data measured were treated by the p...The pharmacokinetics local model was used to evaluate renal function. Some typical kinds of renal function cases, normal or disorder, were selected to be imaged with SPECT and those data measured were treated by the pharmacokinetics local model computer program (PLM). The results indicated that parameters, including peak value, peak time, inflexion time, half-excretion time, and kinetic equation played and important role in judging renal function. The fact confirms that local model is very useful in evaluating renal function.展开更多
The ligand of N-(3-fluoropropyl)-2β-carbomethoxy-3β-(4’-iodophenyl) nortropane (FP-β-CIT) and mesylate precursor were synthesized by hydrolysis of cocaine, followed by dehydration, esterification, Grignard reactio...The ligand of N-(3-fluoropropyl)-2β-carbomethoxy-3β-(4’-iodophenyl) nortropane (FP-β-CIT) and mesylate precursor were synthesized by hydrolysis of cocaine, followed by dehydration, esterification, Grignard reaction, N-demethylation, iodination, N-alkylation with 3-bromopropanol and methylsulfonylation. Finally, 18F-FP-β-CIT was prepared by nucleophilic fluorination of the mesylate with K18F/K2.2.2 (Kryptofix). The labeling yield of 18F-FP-β-CIT is 25%~30%. The total radiochemical yield of this compound, calculated from the end of bombardment (EOB) with decay correction, is 10%~12% with a synthesis time of 100~110.min. The radiochemical purity of 18F-FP-β-CIT is greater than 90%, and this compound in aqueous solution is also stable for more than 4 hours at room temperature. It is stable enough for clinical study.展开更多
基金Foundation for Outstanding Young Members of Health Ministry in China(9925)
文摘The method to synthesize a high affinity muscarinic receptor antagonist (R,S)I-QNB[(R)-(-)-1-azabicyclo [2,2,2]oct-3-yl-(S)-(+)-α-hydroxy-α-(4-[127I]iodophenyl)-α-phenyl acetate] from 4-nitrobenzophenone with improvement compared to literatures was reported in this article. IR, MS and 1HNMR characterized the final product. (R,S)131I-QNB was prepared using Cu(I) assisted iodine exchange labeling, and showed by TLC that the radiolabeling yield(RLY) was over 80%, and radiochemical purity(RCP) was over 95%. Stability of the labeled compound was also determined. It was found that (R,S)131I-QNB dried by nitrogen blowing can stay at 4-10℃ for a week without change of RCP.
文摘The pharmacokinetics local model was used to evaluate renal function. Some typical kinds of renal function cases, normal or disorder, were selected to be imaged with SPECT and those data measured were treated by the pharmacokinetics local model computer program (PLM). The results indicated that parameters, including peak value, peak time, inflexion time, half-excretion time, and kinetic equation played and important role in judging renal function. The fact confirms that local model is very useful in evaluating renal function.
基金the National Natural Science Foundation (39770230) Natural Science Foundation ofJiangsu Province (BK99163) and Department of
文摘The ligand of N-(3-fluoropropyl)-2β-carbomethoxy-3β-(4’-iodophenyl) nortropane (FP-β-CIT) and mesylate precursor were synthesized by hydrolysis of cocaine, followed by dehydration, esterification, Grignard reaction, N-demethylation, iodination, N-alkylation with 3-bromopropanol and methylsulfonylation. Finally, 18F-FP-β-CIT was prepared by nucleophilic fluorination of the mesylate with K18F/K2.2.2 (Kryptofix). The labeling yield of 18F-FP-β-CIT is 25%~30%. The total radiochemical yield of this compound, calculated from the end of bombardment (EOB) with decay correction, is 10%~12% with a synthesis time of 100~110.min. The radiochemical purity of 18F-FP-β-CIT is greater than 90%, and this compound in aqueous solution is also stable for more than 4 hours at room temperature. It is stable enough for clinical study.
