Development of a 99Tcm-labelled radiopharmaceutical for cerebral blood flow imaging

Nowotnik, David P.; Canning, Lewis R.; CUMMING, S. A.; Harrison, Roger; Higley, Brian; NECHVATAL, G.; Pickett, R. D.; Piper, I; BAYNE, V. J.; Förster, A.; WEISNER, P. S.; Neirinckx, R.D.; Volkert, Wynn A.; Troutner, D.E.; Holmes, Richard A.

doi:10.1097/00006231-198509000-00002

Cited by 120 publications

(29 citation statements)

References 0 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…and [99mTc]hexamethylpropyleneamine oxime (HM-PAO) (Ell et al, 1985a;Nowotnik et al, 1985). The e2 3 I] and [20ITl] labels each suffer from disad vantages.…”

mentioning

confidence: 99%

The Retention Mechanism of Technetium-99m-HM-PAO: Intracellular Reaction with Glutathione

Neirinckx

Burke

Harrison

et al. 1988

J Cereb Blood Flow Metab

135

View full text Add to dashboard Cite

Summary: Preparations of d,/-and meso-hexamethyl propyleneamine oxime (HM-PAO) labeled with techne tium-99m were added to rat brain homogenates diluted with phosphate buffer (l: 10). The conversion of d, / HM-PAO to hydrophilic forms took place with an initial rate constant of 0.12 min -1. Incubation of the brain ho mogenate with 2% diethyl maleate for 5 h decreased the homogenate's measured glutathione (GSH) concentration from 160 to 16 f.LM and decreased the conversion rate to 0.012 min -]. Buffered aqueous solutions of glutathione rapidly converted the HM-PAO tracers to hydrophilic forms having the same chromatographic characteristics as found in the brain homogenates. The rate constant for the conversion reaction of d,l-HM-PAO in GSH aqueous solution was 208 and 317 LlmoIlmin in two different assay systems and for meso-HM-PAO the values were 14.7 and 23.2 LlmoIlmin, respectively. Rat brain has a GSH con centration of about 2.3 mM and the conversion of the d,l-HM-PAO due to GSH alone should proceed with a Over the last decade, several brain imaging ra diopharmaceuticals with sufficiently long brain res idence times to permit routine imaging by single photon emission computed tomography (SPECT) have been developed. These have included e2 3 I]_ labeled p-iodo-N -isopropylamphetamine (IMP) (Winchell et aI., 1980) and N ,N-dimethyl-N'(2-hydroxy-5-iodo-3-methylbenzyl)-1 ,3-propanediamine (HIPDM) (Tramposch et aI., 1983), eOITl] diethyldithiocarbamate (DDC) (Wyth et aI., 1983)

show abstract

“…and [99mTc]hexamethylpropyleneamine oxime (HM-PAO) (Ell et al, 1985a;Nowotnik et al, 1985). The e2 3 I] and [20ITl] labels each suffer from disad vantages.…”

mentioning

confidence: 99%

The Retention Mechanism of Technetium-99m-HM-PAO: Intracellular Reaction with Glutathione

Neirinckx

Burke

Harrison

et al. 1988

J Cereb Blood Flow Metab

135

View full text Add to dashboard Cite

show abstract

“…1 H NMR spectra were recorded using a Bruker 500 MHz spectrometer. CH 3 OD was used as solvent, and chemical shifts (d) were reported in ppm relative to TMS as an internal standard.…”

Section: Chemicals and Analytical Methodsmentioning

confidence: 99%

“…Technetium-99m exametazime ( 99m Tc-HMPAO) has been introduced as a tracer for brain imaging studies in humans as early as 1985 [1,2] and its diagnostic utility has been very well documented [3,4]. Currently, it is recommended by the European Association of Nuclear Medicine (EANM) for brain perfusion studies using Single Photon Emission Computed Tomography (SPECT) [5].…”

Section: Introductionmentioning

confidence: 99%

“…The synthesis of the active substance, ligand HMPAO (hexamethylpropylene amineoxime) has been first described by Novotnik www.nmr.viamedica.pl Justyna Pijarowska-Kruszyna et al, New synthesis route of active substance d,l-HMPAO for preparation Technetium Tc99m Exametazime Original et al [1,7]. As elucidated by Neirinckx et al [3], HMPAO has two chiral centers producing the meso-(R,S), d-(R,R) and l-(S,S) diastereomers (Fig.…”

Section: Introductionmentioning

confidence: 99%

See 1 more Smart Citation

New synthesis route of active substance d,l-HMPAO for preparation Technetium Tc99m Exametazime

et al. 2017

View full text Add to dashboard Cite

“…The majority of SPECT imaging of the brain uses 99m Tc labelled HMPAO [34] or ECD [35] (sometimes still 123 I-IMP [36] -especially in Japan) to trace the regional cerebral blood flow (rCBF). Mostly, decreases of rCBF are looked for, as they occur in a variety of brain disorders.…”

Section: Neurological Spectmentioning

confidence: 99%

In vivo functional imaging with SPECT and PET

Herzog

2001

Radiochimica Acta

View full text Add to dashboard Cite

Single photon emission computed tomography / Positron emission tomography / Functional imaging / Radiopharmaceuticals / Gamma cameraSummary. Nuclear medicine methods permit the visualisation of a variety of metabolic and physiological processes all over the body. Although planar scintigraphy has been found useful for many questions, detailed spatial information about the diseased organ can only be obtained with tomographic methods. Dependent on the radionuclide involved, two different tomographic procedures are available: single photon emission computed tomography (SPECT) and positron emission tomography (PET). The first part of this paper describes shortly the historical development of these methods as well as their technical and methodological basics. To elucidate the large variety of possible applications, an overview of SPECT and PET procedures utilised in research as well as in clinical practice are presented. Furthermore, both methods are compared and their individual advantages are pointed out.

show abstract

Development of a 99Tcm-labelled radiopharmaceutical for cerebral blood flow imaging

Cited by 120 publications

References 0 publications

The Retention Mechanism of Technetium-99m-HM-PAO: Intracellular Reaction with Glutathione

The Retention Mechanism of Technetium-99m-HM-PAO: Intracellular Reaction with Glutathione

New synthesis route of active substance d,l-HMPAO for preparation Technetium Tc99m Exametazime

In vivo functional imaging with SPECT and PET

Contact Info

Product

Resources

About