Synthesis of [123I]iodine labelled imidazo[1,2-b] pyridazines as potential probes for the study of peripheral benzodiazepine receptors using SPECT
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| 024 | 7 | 0 | |a 10.1524/ract.92.4.305.35581 |2 doi |
| 035 | |a (NATIONALLICENCE)gruyter-10.1524/ract.92.4.305.35581 | ||
| 245 | 0 | 0 | |a Synthesis of [123I]iodine labelled imidazo[1,2-b] pyridazines as potential probes for the study of peripheral benzodiazepine receptors using SPECT |h [Elektronische Daten] |c [Andrew Katsifis, G. Barlin, F. Mattner, B. Dikic] |
| 520 | 3 | |a The pyridazines 3-acetamidomethyl-6-chloro-2-(4´-iodophenyl)imidazo[1,2-b]pyridazine 1 (IC50=1.6nM) and 3-benzamidomethyl-6-iodo-2-(4´-t-butylphenyl)imidazo[1,2-b] pyridazine 2 (IC50=4.2nM), are high affinity and selective ligands for the Peripheral Benzodiazepine Receptors (PBR) compared to the Central Benzodiazepine counterparts. The [123I]1 and [123I]2 labelled analogues of these compounds were subsequently synthesised for the potential study of the PBR in vivo using SPECT. Radioiodination of [123I]1 was achieved by iododestannylation of the corresponding tributyl tin precursor with Na[ 123I] in the presence of peracetic acid or chloramine-T and the product isolated by C-18 RP HPLC. Radioiodination of [123I]2 was achieved by copper assisted bromine [123I]iodine exchange of the corresponding bromo precursor in the presence of acetic acid and sodium bisulfate as reducing agent at 200°C. Purification of the crude products were achieved by semi-preparative C-18 RP HPLC to give the products in radiochemical yields >90%. The products were obtained in >97% chemical and radiochemical purity and with specific activities >180GBq/μmol. | |
| 540 | |a © 2004 Oldenbourg Wissenschaftsverlag GmbH | ||
| 690 | 7 | |a Laboratory techniques, experiments |2 nationallicence | |
| 690 | 7 | |a Analytical chemistry |2 nationallicence | |
| 690 | 7 | |a Inorganic chemistry |2 nationallicence | |
| 700 | 1 | |a Katsifis |D Andrew |4 aut | |
| 700 | 1 | |a Barlin |D G. |4 aut | |
| 700 | 1 | |a Mattner |D F. |4 aut | |
| 700 | 1 | |a Dikic |D B. |4 aut | |
| 773 | 0 | |t Radiochimica Acta/International journal for chemical aspects of nuclear science and technology |d Oldenbourg Wissenschaftsverlag GmbH |g 92/4-6/2004(2004-04-01), 305-309 |x 0033-8230 |q 92:4-6/2004<305 |1 2004 |2 92 |o ract | |
| 856 | 4 | 0 | |u https://doi.org/10.1524/ract.92.4.305.35581 |q text/html |z Onlinezugriff via DOI |
| 908 | |D 1 |a research article |2 jats | ||
| 950 | |B NATIONALLICENCE |P 856 |E 40 |u https://doi.org/10.1524/ract.92.4.305.35581 |q text/html |z Onlinezugriff via DOI | ||
| 950 | |B NATIONALLICENCE |P 700 |E 1- |a Katsifis |D Andrew |4 aut | ||
| 950 | |B NATIONALLICENCE |P 700 |E 1- |a Barlin |D G. |4 aut | ||
| 950 | |B NATIONALLICENCE |P 700 |E 1- |a Mattner |D F. |4 aut | ||
| 950 | |B NATIONALLICENCE |P 700 |E 1- |a Dikic |D B. |4 aut | ||
| 950 | |B NATIONALLICENCE |P 773 |E 0- |t Radiochimica Acta/International journal for chemical aspects of nuclear science and technology |d Oldenbourg Wissenschaftsverlag GmbH |g 92/4-6/2004(2004-04-01), 305-309 |x 0033-8230 |q 92:4-6/2004<305 |1 2004 |2 92 |o ract | ||
| 900 | 7 | |b CC0 |u http://creativecommons.org/publicdomain/zero/1.0 |2 nationallicence | |
| 898 | |a BK010053 |b XK010053 |c XK010000 | ||
| 949 | |B NATIONALLICENCE |F NATIONALLICENCE |b NL-gruyter | ||