Animal studies of 99mTc–i-PIDP: A new bone imaging agent

Radiopharmaceuticals in China: current status and prospects

“…Besides the radiopharmaceuticals mentioned above, some radiotracers targeting other organs including 99m Tc-BPHA for renal function [86], 99m Tc-labeled fatty acid [87,88], 99m Tc-labeled RGD-BBN peptide [89], 99m Tc-labeled radiotracers for apoptosis imaging [90][91][92], 99m Tc-labeled zoledronic acid derivatives for bone imaging agents [93][94][95][96][97][98][99] have been reported. In the past two decades, 131 Iradiopharmaceuticals have also been investigated.…”

Synthesis, preclinical, and pharmacokinetic evaluation of a new zoledronate derivative as a promising antiosteoporotic candidate using radiolabeling technique

“…The R 2 side chain appears to play an important role in the interaction of DPs with a pharmacological target, since minor modifications to the structure or conformation of the R 2 side chain can dramatically affect antiresorptive potency . It is also worthy to note that optimization of imidazolyl ring or extension of the linker chain between the imidazolyl and geminal bisphosphonate group in the ZL brings significant influence on the biological properties of the bone resorption and the clearance from blood and soft tissues . Moreover, substituents at different positions in the imidazole ring of ZL may be another important factor for the biological properties of the compounds .…”

“…[9][10][11][12] It is also worthy to note that optimization of imidazolyl ring or extension of the linker chain between the imidazolyl and geminal bisphosphonate group in the ZL brings significant influence on the biological properties of the bone resorption and the clearance from blood and soft tissues. 13,14 Moreover, substituents at different positions in the imidazole ring of ZL may be another important factor for the biological properties of the compounds. 15 Based on the previous facts for the purpose of developing a new candidate with excellent biological properties, we continue to extend the number of the methylene chain between the methyl imidazolyl and geminal bisphosphonate group in the diphosphonate and add a substituents in the imidazole ring (see Figure 1).…”

Synthesis and pharmacological evaluation of 99mTc‐labeled imidazolyl‐containing diphosphonic acid as a novel bone imaging agent

“…In the last decade, a series of 99m Tc‐labeled DPs with different alkyl substituents at the 2‐position of the imidazole ring of ZL were prepared, and their in vivo biological properties were investigated systematically by our group for developing new potential bone imaging agents . Previous studies showed that optimization of the alkyl substituent in the imidazole ring and the carbon chain between the imidazolyl and geminal DP groups can bring significant influence on the biological properties of 99m Tc‐labeled complexes, including the bone uptake, blood, and soft‐tissue clearance . In a continuing effort to find better bone imaging agents, a novel 99m Tc‐labeled imidazolyl‐containing diphosphonic acid was designed and synthesized (see Figure ).…”