Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C24H25FN2O5 |
| Molecular Weight | 439.4666 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
COC1=CC=C(OC2=C(C=CC=N2)N(CC3=CC(OC)=CC=C3OCC[18F])C(C)=O)C=C1
InChI
InChIKey=WDCDJYGFOQXTQD-FNNGWQQSSA-N
InChI=1S/C24H25FN2O5/c1-17(28)27(16-18-15-21(30-3)10-11-23(18)31-14-12-25)22-5-4-13-26-24(22)32-20-8-6-19(29-2)7-9-20/h4-11,13,15H,12,14,16H2,1-3H3/i25-1
| Molecular Formula | C24H25FN2O5 |
| Molecular Weight | 439.4666 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
Approval Year
| Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 11:45:48 GMT 2023
by
admin
on
Sat Dec 16 11:45:48 GMT 2023
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| Record UNII |
UA3W78XY6J
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| Record Status |
Validated (UNII)
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| Record Version |
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-
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44632752
Created by
admin on Sat Dec 16 11:45:48 GMT 2023 , Edited by admin on Sat Dec 16 11:45:48 GMT 2023
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1207345-42-3
Created by
admin on Sat Dec 16 11:45:48 GMT 2023 , Edited by admin on Sat Dec 16 11:45:48 GMT 2023
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UA3W78XY6J
Created by
admin on Sat Dec 16 11:45:48 GMT 2023 , Edited by admin on Sat Dec 16 11:45:48 GMT 2023
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PRIMARY |
| Related Record | Type | Details | ||
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TARGET->RADIOLIGAND |
Drugs: 18F FEMPA(Primary); Indications: Alzheimer's disease; Focus: Diagnostic use; Most Recent Event: 20 Nov 2014 New trial record
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NON-LABELED -> LABELED |
| Related Record | Type | Details | ||
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ACTIVE MOIETY |
Results: Five AD and 4 controls were high-affinity binders (HABs). Three AD and 3 controls were mixed-affinity binders. In the medial temporal cortex, a significant difference of VT (p=0.044) was found if the TSPO binding profile was entered as covariate. If only HABs were included, significant differences of VT (p<0.05, Figure) were found in the medial and lateral temporal cortex, caudate, putamen, thalamus, posterior cingulate, and cerebellum.
Conclusions: (18F)FEMPA seems to be a suitable radioligand to detect increased TSPO binding in AD if the binding status is taken into account.
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ACTIVE MOIETY |
The distribution kinetics of (18)F-FEMPA was evaluated by in vivo PET/CT imaging. (18)F-FEMPA uptake was compared in atherosclerotic (LDLR(-/-)ApoB(100/100), n = 10) and healthy mice (C57BL/6 N, n = 7) ex vivo at twenty minutes post-injection. Biodistribution was analyzed from harvested tissue samples, and aortas were sectioned for autoradiography. Aortas of LDLR(-/-)ApoB(100/100) mice showed large, macrophage-rich atherosclerotic plaques. In vivo, (18)F-FEMPA showed rapid blood clearance but no difference in aortic uptake between atherosclerotic and healthy mice. In the mice studied ex vivo at 20 minutes post-injection, quantification of radioactivity in the whole aorta showed 1.3-fold higher (18)F-FEMPA accumulation in atherosclerotic than healthy mice (P = .028). Autoradiography showed higher tracer uptake in plaque areas with high macrophage content as compared with areas of no macrophages (count densities 190 +/- 54 vs 40 +/- 13 PSL/mm(2), P < .001), but the uptake in the plaques was not higher than in the normal vessel wall (230 +/- 78 PSL/mm(2)).
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