Development of Radiolabeled Probes Directed against Sigma-1 Receptors

Comparison of Radioiodine- or Radiobromine-Labeled RGD Peptides between Direct and Indirect Labeling Methods

“…(13), which was synthesized using a method described previously, 24) was dissolved in 100 µL of DMF. Boc-NH-EG 2 -COOH (14) For deprotection of functional groups, compound 15 was treated with a mixture of 95% TFA, 2.5% water, and 2.5% triisopropylsilane for 2 h at room temperature.…”

“…7) A number of radiolabeled RGD peptide derivatives for use in positron emission tomography (PET) imaging, single-photon emission computed tomography (SPECT) imaging, and targeted radionuclide therapy have been reported. [8][9][10][11][12][13] Among the halogens, many useful radioisotopes for nuclear medicine and life sciences exist, such as 18 F (for PET), 76 Br (for PET), 77 Br (for basic research or Auger therapy), At (for α therapy). 14) A labeling method for proteins that uses radioiodine and an oxidation agent, such as chloramine-T, has been used classically.…”

Development of tumor-targeting aza-vesamicol derivatives with high affinity for sigma receptors for cancer theranostics

“…27,28 We synthesized and evaluated radiohalogen-labeled vesamicol analogs as probes targeting the sigma-1 receptor. [29][30][31] Our investigations of the probe-receptor interactions demonstrated that a compound with an iodine atom in the para position of the phenyl group in the vesamicol structure, 2-(4-(4-iodophenyl)piperidine)cyclohexanol (pIV, Fig. 1b), has over 10-fold higher affinity for the sigma-1 receptor than the lead compound, unmodified vesamicol.…”

Development of Diagnostic and Therapeutic Probes with Controlled Pharmacokinetics for Use in Radiotheranostics

“…This receptor is mainly located on the endoplasmic reticulum membrane in the cell and works to maintain cellular homeostasis as a molecular chaperone. 42,43) Since the sigma-1 receptor is related to functions of the central nervous system, such as signal transduction, memory, recognition, and emotion, determining the expression level of the sigma-1 receptor should be useful for diagnosis of neurodegenerative diseases, such as Alzhei mer's, Parkinson's diseases, and amyotrophic lateral sclerosis. [44][45][46] The sigma-1 receptor is also highly expressed in various cancer cells.…”