Preliminary studies of 99mTc-memantine derivatives for NMDA receptor imaging

Zhou, Xingqin; Zhang, Jiankang; Yan, Chenglong; Cao, Gaoping; Zhang, Rongjun; Cai, Gangming; Jiang, Meng-Jun; Songpei, Wang

doi:10.1016/j.nucmedbio.2012.02.008

Cited by 6 publications

(3 citation statements)

References 32 publications

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“…The animals were weighed, anesthetized by chloroform, and scarified at the predesigned time intervals, and their body organs and fluids were separated and weighed, and their radioactivities were assayed using a NaI(Tl) γ‐ray scintillation counter. The radioactivity was expressed as a percentage of the injected dose per gram of organ (ID%/g) . Samples of fresh blood, bone, and muscle were collected in preweighed vials and counted.…”

Section: Methodsmentioning

confidence: 99%

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

Motaleb

Ibrahim

El-Tawoosy

et al. 2017

Labelled Comp Radiopharmac

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A novel zoledronic acid (ZL) derivative, 3-(2-ethyl-4-methyi-1H-imidazole-1-yl)-1-hydroxy-1-phosphonopropyl phosphonic acid (EMIHPBP), was synthesized, characterized, and successfully radiolabeled with Tc. The in vivo biodistribution of Tc-EMIHPBP was investigated and compared with the previously reported zoledronate derivatives aiming to formulate a novel zoledronate derivative with a high-potential uptake to bone as a promising antiosteoporotic candidate. To further evaluate the bone uptake efficiency, the pharmacokinetics of Tc-EMIHPBP was investigated and showed that maximum concentration in bone (C ) was 31.60 ± 0.15%ID/gram after 60 minutes (t ). Cumulative residence of Tc-EMIHPBP in the bone [AUC (%ID∙min/gram bone)] was 3685.23, mean residence time was 384.354 minutes, and the calculated bone bioavailability was 15.831%. Finally, the time needed for half of the Tc-EMIHPBP formulation to be eliminated from bone (t ) was 263.914 minutes. Excellent bone uptake can be obtained 1-hour postinjection with high bone/blood ratio of 23.76 detected with gamma counter. The biodistribution and kinetic studies could recommend EMIHPBP as a promising antiosteoporotic candidate with high selectivity to the skeletal system and rapid clearance from soft tissues.

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Section: Methodsmentioning

confidence: 99%

“…The radioactivity was expressed as a percentage of the injected dose per gram of organ (ID%/g). 22 Samples of fresh blood, bone, and muscle were collected in preweighed vials and counted. Blood, bone, and muscles were assumed to be 7%, 10%, and 40% of the total body weight, respectively.…”

Section: Biodistribution Assaymentioning

confidence: 99%

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

Motaleb

Ibrahim

El-Tawoosy

et al. 2017

Labelled Comp Radiopharmac

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“…89 The autoradiography studies showed specific binding in rat brain cryosections and blocking studies demonstrated an up to 32% reduction of tracer binding, which represents a promising radiotracer for imaging NR2B subunit ( Figure 3b , compound e). It is worthy of mention that other approaches, including NMDA SPECT agents, 90 radiolabeled drug candidate ASP0777 91 , a NR2A selective radioligand [ 18 F]FP-PEAQX 92 and an array of candidate compounds based on CNS 1261, 93 are also disclosed in the literature in the pursue of NMDA imaging ligand.…”

Section: N-methyl-d-aspartate Receptormentioning

confidence: 99%

Selected PET Radioligands for Ion Channel Linked Neuroreceptor Imaging: Focus on GABA, NMDA and nACh Receptors

Kassenbrock¹,

Vasdev²,

Liang

2016

CTMC

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Positron emission tomography (PET) neuroimaging of ion channel linked receptors is a developing area of preclinical and clinical research. The present review focuses on recent advances with radiochemistry, preclinical and clinical PET imaging studies of three receptors that are actively pursued in neuropsychiatric drug discovery: namely the γ-aminobutyric acid-benzodiazapine (GABA) receptor, nicotinic acetylcholine receptor (nAChR), and N-methyl-d-aspartate (NMDA) receptor. Recent efforts to develop new PET radioligands for these targets with improved brain uptake, selectivity, stability and pharmacokinetics are highlighted.

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