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. 1993 Aug;109(4):1101–1109. doi: 10.1111/j.1476-5381.1993.tb13736.x

Demonstration of the suitability of CGP 12177 for in vivo studies of beta-adrenoceptors.

M P Law 1
PMCID: PMC2175765  PMID: 8104642

Abstract

1. Positron emission tomography (PET) with appropriate radioligands offers the possibility of studying receptors non-invasively in man. The suitability of CGP 12177, a hydrophilic non-selective beta-adrenoceptor antagonist which can be labelled with the positron emitter 11C, as a ligand for in vivo studies of beta-adrenoceptors was assessed in rats. 2. [3H]-CGP 12177 was injected into the tail veins of restrained conscious rats. Serial blood samples were taken from tail arteries to determine clearance from plasma. Rats were killed and tissues removed to determine tissue uptake. Radioactivity was assessed by liquid scintillation counting. 3. The uptake of (-)-[3H]-CGP 12177 in various tissues was compared to that of (+/-)-[3H]-CGP 12177. Maximum tissue:plasma ratios obtained for the (-)-enantiomer in lung, heart and liver were 170, 42 and 13 compared with 60, 15 and 12 for the racemate. Prior injection of excess unlabelled (+/-)-CGP 12177 blocked the uptake of both (-)- and (+/-)-[3H]-CGP 12177 in lung and heart but not liver, tissue:plasma ratios for both tracers being reduced to 7, 3 and 7 respectively. 4. Clearance of (-)-[3H]-CGP 12177 from plasma was rapid during the first 5 min but showed only small changes during 5 to 90 min. Uptake in lung and heart reached a maximum at 1 to 5 min and showed a slow decrease during 5-90 min. Prior injection of unlabelled (+/-)-CGP 12177 reduced uptake in lung and heart to 10% and 20% respectively.(ABSTRACT TRUNCATED AT 250 WORDS)

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Selected References

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