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
COC(=O)[C@@H]1[C@H]2CC[C@@H](C[C@@H]1C3=CC=C(I)C=C3)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
T1/2
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
175.9 h |
167 MBq single, intravenous dose: 167 MBq route of administration: Intravenous experiment type: SINGLE co-administered: |
IOFLUPANE I-123 blood | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
Funbound
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
6.5% |
IOFLUPANE I-123 blood | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
PubMed
| Title | Date | PubMed |
|---|---|---|
| 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. | 2018-07 |
|
| [18F] beta-CIT-FP is superior to [11C] beta-CIT-FP for quantitation of the dopamine transporter. | 1997-10 |
|
| Radiosynthesis of [18F] N-3-fluoropropyl-2-beta-carbomethoxy-3-beta-(4-iodophenyl) nortropane and the first human study with positron emission tomography. | 1996-11 |
| Substance Class |
Chemical
Created
by
admin
on
Edited
Tue Apr 01 16:34:55 GMT 2025
by
admin
on
Tue Apr 01 16:34:55 GMT 2025
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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 Tue Apr 01 16:34:55 GMT 2025 , Edited by admin on Tue Apr 01 16:34:55 GMT 2025
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| Code System | Code | Type | Description | ||
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NT4P0L3OCX
Created by
admin on Tue Apr 01 16:34:55 GMT 2025 , Edited by admin on Tue Apr 01 16:34:55 GMT 2025
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186381-69-1
Created by
admin on Tue Apr 01 16:34:55 GMT 2025 , Edited by admin on Tue Apr 01 16:34:55 GMT 2025
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11626128
Created by
admin on Tue Apr 01 16:34:55 GMT 2025 , Edited by admin on Tue Apr 01 16:34:55 GMT 2025
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| Related Record | Type | Details | ||
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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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