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Chemical Compound Review:

AC1NSMEG 2-(3,4-dimethoxyphenyl)-5-[2- (3,4...

Synonyms: CHEMBL483787, [11C]Verapamil, [11C]VER, [11C]-Verapamil

Hendrikse, N.H. et al., Bart, J. et al., Hendrikse, N.H. et al., Hendrikse, N.H. et al., Hendrikse, N.H. et al.

Hendrikse, de Vries, Franssen, Vaalburg, van der Graaf,

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High impact information on [11C]Verapamil

Biodistribution studies showed 159% and 185% higher levels of [11C]daunorubicin and [11C]verapamil, respectively, in GLC4 than in GLC4/P-gp tumors [1].
PET measurements demonstrated a lower [11C]verapamil content in GLC4/P-gp tumors compared with GLC4 tumors [1].
We measured the kinetics of the P-gp substrate [11C]verapamil (0.1 mg/kg) in rat brains using positron emission tomography (PET) and arterial blood sampling [2].
Quantitative assessment of P-glycoprotein function in the rat blood-brain barrier by distribution volume of [11C]verapamil measured with PET [2].
This indicates complete inhibition of P-gp mediated [11C]verapamil efflux [3].

Biological context of [11C]Verapamil

The [11C]verapamil kinetics were very well described by DV, computed by noncompartmental Logan analysis [2].

Anatomical context of [11C]Verapamil

3. Biodistribution studies revealed 9.5-fold (P < 0.001) and 3.4-fold (P < 0.001) higher [11C]verapamil in the brain and testes of mdr1a(-/-) mice than in mdr1a(+/+) mice [3].

Associations of [11C]Verapamil with other chemical compounds

Pretreatment with cyclosporin A increased [11C]verapamil levels in GLC4/P-gp tumors (184%) and in brains (1280%) [1].

Gene context of [11C]Verapamil

Several agents, including [11C]colchicine, [11C]verapamil and [11C]daunorubicin, have been evaluated for the quantification of Pgp-mediated transport with PET in vivo [4].

Analytical, diagnostic and therapeutic context of [11C]Verapamil

Therefore, P-gp function was measured in vivo with positron emission tomography (PET) and [11C]verapamil as radiolabeled P-gp substrate [1].
METHODS: After intravenous injection of [11C]verapamil (370 MBq, specific activity >1,600 GBq/mmol), kinetics were evaluated in five cancer patients using positron emission tomography (PET) [5].

References

A new in vivo method to study P-glycoprotein transport in tumors and the blood-brain barrier. Hendrikse, N.H., de Vries, E.G., Eriks-Fluks, L., van der Graaf, W.T., Hospers, G.A., Willemsen, A.T., Vaalburg, W., Franssen, E.J. Cancer Res. (1999) [Pubmed]
Quantitative assessment of P-glycoprotein function in the rat blood-brain barrier by distribution volume of [11C]verapamil measured with PET. Bart, J., Willemsen, A.T., Groen, H.J., van der Graaf, W.T., Wegman, T.D., Vaalburg, W., de Vries, E.G., Hendrikse, N.H. Neuroimage (2003) [Pubmed]
Complete in vivo reversal of P-glycoprotein pump function in the blood-brain barrier visualized with positron emission tomography. Hendrikse, N.H., Schinkel, A.H., de Vries, E.G., Fluks, E., Van der Graaf, W.T., Willemsen, A.T., Vaalburg, W., Franssen, E.J. Br. J. Pharmacol. (1998) [Pubmed]
Visualization of multidrug resistance in vivo. Hendrikse, N.H., Franssen, E.J., van der Graaf, W.T., Vaalburg, W., de Vries, E.G. European journal of nuclear medicine. (1999) [Pubmed]
In vivo measurement of [11C]verapamil kinetics in human tissues. Hendrikse, N.H., de Vries, E.G., Franssen, E.J., Vaalburg, W., van der Graaf, W.T. Eur. J. Clin. Pharmacol. (2001) [Pubmed]

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