Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C18H23FINO2 |
| Molecular Weight | 430.2861 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 4 / 4 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
[H][C@]12CC[C@]([H])([C@H]([C@H](C1)C3=CC=C(I)C=C3)C(=O)OC)N2CCC[18F]
InChI
InChIKey=HXWLAJVUJSVENX-LNYNZGDVSA-N
InChI=1S/C18H23FINO2/c1-23-18(22)17-15(12-3-5-13(20)6-4-12)11-14-7-8-16(17)21(14)10-2-9-19/h3-6,14-17H,2,7-11H2,1H3/t14-,15+,16+,17-/m0/s1/i19-1
| Molecular Formula | C18H23FINO2 |
| Molecular Weight | 430.2861 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 4 / 4 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
CNS Activity
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| Radiosynthesis of [18F] N-3-fluoropropyl-2-beta-carbomethoxy-3-beta-(4-iodophenyl) nortropane and the first human study with positron emission tomography. | 1996 Nov |
|
| [18F] beta-CIT-FP is superior to [11C] beta-CIT-FP for quantitation of the dopamine transporter. | 1997 Oct |
|
| Head-to-head comparison of (18) F-FP-CIT and (123) I-FP-CIT for dopamine transporter imaging in patients with Parkinson's disease: A preliminary study. | 2018 Jul |
| Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 11:34:57 GMT 2023
by
admin
on
Sat Dec 16 11:34:57 GMT 2023
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| Record UNII |
NT4P0L3OCX
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| Record Status |
Validated (UNII)
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| Record Version |
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FDA ORPHAN DRUG |
451114
Created by
admin on Sat Dec 16 11:34:57 GMT 2023 , Edited by admin on Sat Dec 16 11:34:57 GMT 2023
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| Code System | Code | Type | Description | ||
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NT4P0L3OCX
Created by
admin on Sat Dec 16 11:34:57 GMT 2023 , Edited by admin on Sat Dec 16 11:34:57 GMT 2023
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186381-69-1
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11626128
Created by
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ACTIVE MOIETY |
We therefore labelled beta-CIT-FP with fluorine-18 in a position that may avoid the formation of labelled lipophilic metabolites. The more long-lived radionuclide (18F) was used to allow for measurements over longer time. (N-fluoropropyl- 18F) beta-CIT-FP ((18F) beta-CIT-FP) was prepared by N-alkylation of nor-beta-CIT with (18F)fluoropropyl bromide. PET studies were performed in cynomolgus monkeys. (18F) beta-CIT-FP entered the brain rapidly. There was a high concentration of radioactivity in the striatum and much lower in the thalamus, neocortex, and cerebellum. The striatum-to-cerebellum ratio was about 5 at time of transient equilibrium, which occurred after 60 to 100 min. After pretreatment with GBR 12909, radioactivity in the striatum was markedly reduced, thus indicating specific (18F) beta-CIT-FP binding to the dopamine transporter. The fraction of unchanged (18F) beta-CIT-FP determined by HPLC was 10-15% after 140 min. No lipophilic labelled metabolites were detected. The absence of measurable lipophilic labelled metabolites and the occurrence of transient equilibrium within the time of the PET measurement indicate that (18F) beta-CIT-FP is superior to (11C) beta-CIT-FP as a PET radioligand for quantification of the dopamine transporter in the human brain.
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