phosphonic analogue
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Molecules ◽  
2021 ◽  
Vol 26 (8) ◽  
pp. 2357
Author(s):  
Alesya Ya. Maruk ◽  
Valery V. Ragulin ◽  
Iurii A. Mitrofanov ◽  
Galina S. Tsebrikova ◽  
Vitaly P. Solov’ev ◽  
...  

Two new aminodiphosphonic acids derived from salicylic acid and its phosphonic analogue were prepared through a simple and efficient synthesis. 2-[(2-Amino-2,2-diphosphono)ethyloxy]-benzoic acid 8 and 2-[(2-amino-2,2-diphosphono)ethyloxy]-5-ethyl-phenylphosphonic acid 9 were evaluated for their applicability as 68Ga binding bone-seeking agents. Protonation constants of 8 and 9 and stability constants of the Ga3+ complexes with 8 and 9 in water were determined. The stability constant of Ga3+ complex with fully phosphorylated acid 9 (logKGaL = 31.92 ± 0.32) significantly exceeds stability constant of Ga3+ complex with 8 (logKGaL = 26.63 ± 0.24). Ligands 8 and 9 are as effective for Ga3+ cation binding as ethylenediamine-N,N’-diacetic-N,N’-bis(methy1enephosphonic) acid and ethylenediamine-N,N,N’,N’-tetrakis(methylenephosphonic) acid, respectively. The labelling process and stability of [68Ga]Ga-8 and [68Ga]Ga-9 were studied. Both 8 and 9 readily form 68Ga-complexes stable to ten-fold dilution with saline. However, in fetal bovine serum, only [68Ga]Ga-9 was stable enough to be subject to biological evaluation. It was injected into rats with bone pathology and aseptic inflammation of soft tissues. For [68Ga]Ga-9 in animals with a bone pathology model in 60 and 120 min after injection, a slight accumulation in the pathology site, stable blood percentage level, and moderate accumulation in the liver were observed. For animals with an aseptic inflammation, the accumulation of [68Ga]Ga-9 in the pathology site was higher than that in animals with bone pathology. Moreover, the accumulation of [68Ga]Ga-9 in inflammation sites was more stable than that for [68Ga]Ga-citrate. The percentage of [68Ga]Ga-9 in the blood decreased from 3.1% ID/g (60 min) to 1.5% ID/g (120 min). Accumulation in the liver was comparable to that obtained for [68Ga]Ga-citrate.


ChemInform ◽  
2010 ◽  
Vol 23 (18) ◽  
pp. no-no
Author(s):  
A.-M. CHOLLET-GRAVEY ◽  
L. VO-QUANG ◽  
Y. VO-QUANG ◽  
F. LE GOFFIC

ChemInform ◽  
2010 ◽  
Vol 31 (12) ◽  
pp. no-no
Author(s):  
Alain Hercouet ◽  
Maurice Le Corre ◽  
Bertrand Carboni

ChemInform ◽  
2010 ◽  
Vol 31 (21) ◽  
pp. no-no
Author(s):  
Celine Duquenne ◽  
Sophie Goumain ◽  
Philippe Jubault ◽  
Christian Feasson ◽  
Jean-Charles Quirion
Keyword(s):  

2000 ◽  
Vol 2 (4) ◽  
pp. 453-455 ◽  
Author(s):  
Céline Duquenne ◽  
Sophie Goumain ◽  
Philippe Jubault ◽  
Christian Feasson ◽  
Jean-Charles Quirion
Keyword(s):  

2000 ◽  
Vol 41 (2) ◽  
pp. 197-199 ◽  
Author(s):  
Alain Hercouet ◽  
Maurice Le Corre ◽  
Bertrand Carboni

Amino Acids ◽  
1994 ◽  
Vol 7 (1) ◽  
pp. 97-103
Author(s):  
A. Iron ◽  
E. Neuzil ◽  
A. Cassaigne

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