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Chemical Compound Review:

FP-Cit methyl(1R,2S,3S)-8-(3- fluoropropyl)-3-(4...

Synonyms: beta-Cit-FP, AC1L3U61, (123I)FP-Cit, 155797-99-2, (O-Methyl-11C)beta-cit-FP

Okada, T. et al., Ishikawa, T. et al., Lundkvist, C. et al.

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Disease relevance of FP-Cit

We compared [123I] beta CIT-FP/SPECT and [18F]FDOPA/PET in the assessment of nigrostriatal dopaminergic function in Parkinson's disease (PD) and normal aging [1].

High impact information on FP-Cit

We generated cell lines stably expressing DA, 5-HT, and NE transporters, respectively, by the Chen-Okayama method, and then tested the abilities of (-)cocaine, beta-CIT, beta-CIT-FE, beta-CIT-FP, and clomipramine to inhibit the uptake of [3H]DA, 5-HT, and 2-NE [2].
Assessment of affinities of beta-CIT, beta-CIT-FE, and beta-CIT-FP for monoamine transporters permanently expressed in cell lines [2].
Beta-CIT and beta-CIT-FP were highly potent and selective dopamine uptake inhibitors, and therefore might be useful for imaging of DA transporter with single photon emission computed tomography (SPECT) or positron emission tomography (PET) [2].

Analytical, diagnostic and therapeutic context of FP-Cit

CONCLUSION: These results indicate that [123I] beta CIT-FP/SPECT can provide quantitative descriptors of presynaptic dopaminergic function comparable to those obtained with [18F]FDOPA/PET [1].
UPDRS motor ratings correlated with SOR values obtained by both imaging techniques (r = -0.69 and -0.60, p < 0.04 for [123I] beta CIT-FP and [18F]FDOPA, respectively) [1].
Positron emission tomography (PET) studies with [O-methyl-11C] beta-CIT-FP ([11C] beta-CIT-FP) has shown that equilibrium conditions were approached but, however, not reached at the end of measurement [3].
The fraction of unchanged [18F] beta-CIT-FP determined by HPLC was 10-15% after 140 min [3].

References

Comparative nigrostriatal dopaminergic imaging with iodine-123-beta CIT-FP/SPECT and fluorine-18-FDOPA/PET. Ishikawa, T., Dhawan, V., Kazumata, K., Chaly, T., Mandel, F., Neumeyer, J., Margouleff, C., Babchyck, B., Zanzi, I., Eidelberg, D. J. Nucl. Med. (1996) [Pubmed]
Assessment of affinities of beta-CIT, beta-CIT-FE, and beta-CIT-FP for monoamine transporters permanently expressed in cell lines. Okada, T., Fujita, M., Shimada, S., Sato, K., Schloss, P., Watanabe, Y., Itoh, Y., Tohyama, M., Nishimura, T. Nucl. Med. Biol. (1998) [Pubmed]
[18F] beta-CIT-FP is superior to [11C] beta-CIT-FP for quantitation of the dopamine transporter. Lundkvist, C., Halldin, C., Ginovart, N., Swahn, C.G., Farde, L. Nucl. Med. Biol. (1997) [Pubmed]

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