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. Author manuscript; available in PMC: 2009 Jan 13.
Published in final edited form as: J Med Chem. 2007 Apr 10;50(9):2078–2088. doi: 10.1021/jm061398y

Table 1.

graphic file with name nihms-62260-f0012.jpg Neuronal Uptake and Clearance Rates of [11C]Phenethylguanidines in Isolated Rat Hearta

compd R1 R2 R3 R4 name acronym Kup (ml/min/g) major clearance T1/2 (hr)
[11C]1a H H H H [11C]phenethylguanidine (PG) PG 1.56 3.3
[11C]1b OH H H H [11C]meta-hydroxy-PG MHPG 1.96 ± 0.13 >102
[11C]1c H OH H H [11C]para-hydroxy-PG PHPG 1.64 ± 0.15 >45
[11C]1d H H H (-)-OH [11C](-)-β-hydroxy-PG BHPG 0.42 22
[11C]1e OH H H (-)-OH N-[11C]guanyl-meta-octopamine GMO 0.30 ± 0.02 >152
[11C]1f H MeO H H [11C]para-methoxy-PG PMPG 0.73 2.3
[11C]1g F H H H [11C]meta-fluoro-PG MFPG 0.24 1.9
[11C]1h H F H H [11C]para-fluoro-PG PFPG 0.63 4.4
[11C]1i H H F H [11C]ortho-fluoro-PG OFPG 1.76 2.3
[11C]1j OH F H H [11C]para-fluoro-meta-hydroxy-PG 4F-MHPG 0.72 ± 0.05 >73
[11C]1k OH H F H [11C]ortho-fluoro-meta-hydoxy-PG 6F-MHPG 0.49 ± 0.07 >20
[11C]1l I H H H [11C]meta-iodo-PG MIPG 1.10 2.4
[11C]1m H I H H [11C]para-iodo-PG PIPG 0.56 1.9
a

For compounds with multiple determinations, Kup data are mean ± standard deviation (SD) and T1/2 is the fastest measured clearance rate for n = 5 independent determinations. Coefficients of variation (SD/mean) for these ranged from 7-14%. Single determination values can be expected to be within this range. Extraneuronal uptake (uptake-2) was inhibited in all studies by adding 54 μM corticosterone to the perfusate.