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Uptake and retention kinetics of para-fluorine-18-fluorobenzylguanidine in isolated rat heart.

Publication ,  Journal Article
Berry, CR; Garg, PK; Zalutsky, MR; Coleman, RE; DeGrado, TR
Published in: J Nucl Med
December 1996

UNLABELLED: Para-[18F]fluorobenzylguanidine ([18F]PFBG) is a newly developed tracer for imaging myocardial sympathetic neuronal innervation. This study investigated the uptake and retention mechanisms of [18F]PFBG in perfused, isolated rat heart. METHODS: Fluorine-18-PFBG was administered to working rat hearts within the perfusion medium at a constant activity concentration (1.5-2 MBq/liter) for 8 min, followed by a washout period (50 min). External scintillation probes with coincidence detection circuitry were used to measure myocardial radioactivity. Six groups of hearts (n = 6, except in Group 6) were studied: (Group 1) control; (Group 2) 100 nM desipramine (DMI); (Group 3) 0.8 microM SKF550; (Group 4) DMI + SKF550; (Group 5) SKF550 + 1.0 microM Ro 4-1284; and (Group 6) SKF550 with DMI chase at 30 min (n = 4). RESULTS: Groups 2, 3 and 4 showed a mean reduction of 19% (uptake-1 blockade), 58% (uptake-2 blockade) and 95% (uptake-1 and uptake-2 blockade) in uptake rates, respectively, compared with control (p < 0.01). A further 33% reduction in the uptake rate was noted with vesicular transport inhibition (Group 5 compared with 3, p = 0.054). Biphasic clearance consisting of rapid (T1/2 = 5.32 +/- 1.1 min) and slow (T1/2 = 35.2 +/- 9.6 min) components were noted in control hearts. The rapid (T1/2 = 1.6 +/- 0.3 min) and slow (T1/2 = 10.9 +/- 1.4 min) clearance rates were accelerated (p < 0.0001) in Group 5 compared to control. DMI chase conditions (Group 6) caused an inhibition of [18F]PFBG washout (p = 0.004) suggesting a role for reverse transport through the uptake-1 carrier. CONCLUSION: Fluorine-18-PFBG is specifically accumulated by sympathetic nerve terminals. However, further work is recommended in humans to evaluate the potential implications of specific extraneuronal uptake of [18F]PFBG through the uptake-2 mechanism.

Duke Scholars

Published In

J Nucl Med

ISSN

0161-5505

Publication Date

December 1996

Volume

37

Issue

12

Start / End Page

2011 / 2016

Location

United States

Related Subject Headings

  • Sympathetic Nervous System
  • Rats, Sprague-Dawley
  • Rats
  • Radionuclide Imaging
  • Nuclear Medicine & Medical Imaging
  • In Vitro Techniques
  • Hemodynamics
  • Heart
  • Guanidines
  • Fluorobenzenes
 

Citation

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Berry, C. R., Garg, P. K., Zalutsky, M. R., Coleman, R. E., & DeGrado, T. R. (1996). Uptake and retention kinetics of para-fluorine-18-fluorobenzylguanidine in isolated rat heart. J Nucl Med, 37(12), 2011–2016.
Berry, C. R., P. K. Garg, M. R. Zalutsky, R. E. Coleman, and T. R. DeGrado. “Uptake and retention kinetics of para-fluorine-18-fluorobenzylguanidine in isolated rat heart.J Nucl Med 37, no. 12 (December 1996): 2011–16.
Berry CR, Garg PK, Zalutsky MR, Coleman RE, DeGrado TR. Uptake and retention kinetics of para-fluorine-18-fluorobenzylguanidine in isolated rat heart. J Nucl Med. 1996 Dec;37(12):2011–6.
Berry, C. R., et al. “Uptake and retention kinetics of para-fluorine-18-fluorobenzylguanidine in isolated rat heart.J Nucl Med, vol. 37, no. 12, Dec. 1996, pp. 2011–16.
Berry CR, Garg PK, Zalutsky MR, Coleman RE, DeGrado TR. Uptake and retention kinetics of para-fluorine-18-fluorobenzylguanidine in isolated rat heart. J Nucl Med. 1996 Dec;37(12):2011–2016.

Published In

J Nucl Med

ISSN

0161-5505

Publication Date

December 1996

Volume

37

Issue

12

Start / End Page

2011 / 2016

Location

United States

Related Subject Headings

  • Sympathetic Nervous System
  • Rats, Sprague-Dawley
  • Rats
  • Radionuclide Imaging
  • Nuclear Medicine & Medical Imaging
  • In Vitro Techniques
  • Hemodynamics
  • Heart
  • Guanidines
  • Fluorobenzenes