| Stereochemistry | RACEMIC |
| Molecular Formula | C13H28N4O2 |
| Molecular Weight | 272.387 |
| Optical Activity | ( + / - ) |
| Defined Stereocenters | 2 / 2 |
| E/Z Centers | 2 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
C[C@@H](NCC(C)(C)CN[C@H](C)C(\C)=N\O)C(\C)=N\O
InChI
InChIKey=BPNZYADGDZPRTK-UDUYQYQQSA-N
InChI=1S/C13H28N4O2/c1-9(11(3)16-18)14-7-13(5,6)8-15-10(2)12(4)17-19/h9-10,14-15,18-19H,7-8H2,1-6H3/b16-11+,17-12+/t9-,10-/m1/s1
| Molecular Formula | C13H28N4O2 |
| Molecular Weight | 272.387 |
| Charge | 0 |
| Count |
MOL RATIO
1 MOL RATIO (average) |
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 2 / 2 |
| E/Z Centers | 2 |
| Optical Activity | UNSPECIFIED |
Technetium (99mTc) exametazime is a radiopharmaceutical agent, which is known as trade name Ceretec. The Ceretec kit is supplied as five packs of three vials for use in the preparation of a technetium Tc99m exametazime intravenous injection as a diagnostic radiopharmaceutical. When technetium Tc99m pertechnetate is added to exametazime in the presence of stannous reductant, a lipophilic technetium Tc99m complex is formed. This lipophilic complex is the active moiety. It converts at approximately 12%/hour to less lipophilic species. When the secondary complex is separated from the lipophilic species, it is unable to cross the blood-brain-barrier. The useful life of the reconstituted agent is limited to 30 minutes. This complex is used as an adjunct in the detection of altered regional cerebral perfusion in stroke. And in addition, is indicated for leukocyte labeled scintigraphy as an adjunct in the localization of intra-abdominal infection and inflammatory bowel disease. Also exist clinical trials, where this complex is used for diagnostic purposes in Crohn's Disease and in vascular prosthesis infection.
CNS Activity
Approval Year
PubMed
Patents
Sample Use Guides
The normal adult (70 kg) dose is 0.259-0.925 GBq (7-25 mCi) as Tc99m labeled leukocytes by intravenous injection. Optimal planar imaging is between 2-4 hours. Do not use methylene blue in the preparation of the Tc99m labeled leukocytes.
Cerebral Scintigraphy: The recommended dose range for i.v. administration, of reconstituted sodium pertechnetate Tc99m exametazime (with or without methylene blue) in the average adult (70 kg) is 370-740 MBq (10-20 mCi).
Dynamic imaging may be performed between 0 to 10 minutes following injection. Static imaging may be performed from 15 minutes up to 6 hours after injection.
Route of Administration:
Intravenous
Whole blood (480 mL) was obtained from each of 3 healthy donors and divided equally into eight 60-mL aliquots. Two aliquots from each of the 3 subjects were used as a control (i.e., leukocytes were not labeled with either nonstabilized or stabilized 99mTc-exametazime) in this study. The remaining 6 aliquots from each of the 3 subjects were divided equally into the following formulation groups: (a) leukocytes labeled with nonstabilized 99mTc-exametazime, (b) leukocytes labeled with stabilized 99mTc-exametazime containing 250 microg methylene blue, and (c) leukocytes labeled with stabilized 99mTc-exametazime containing 500 microg methylene blue. It was revealed that, the methylene blue/phosphate buffer stabilizer (250 or 500 microg methylene blue) did not affect the cell membrane integrity, chemotactic capacity, labeling efficiency, in vitro stability, or complete blood count of leukocytes labeled with stabilized 99mTc-exametazime.
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SALT/SOLVATE -> PARENT |
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