PMID: 8104642Aug 1, 1993Paper

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

British Journal of Pharmacology
M P Law

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 ...Continue Reading

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Citations

May 5, 2007·European Journal of Nuclear Medicine and Molecular Imaging·Riikka LautamäkiFrank M Bengel
Oct 2, 2007·European Journal of Nuclear Medicine and Molecular Imaging·Marilyn P LawMichael Schäfers
Oct 9, 2004·Journal of Nuclear Cardiology : Official Publication of the American Society of Nuclear Cardiology·Frank M Bengel, Markus Schwaiger
May 17, 2000·Pharmaceutica acta Helvetiae·V W PikeP G Camici
May 9, 2000·Applied Radiation and Isotopes : Including Data, Instrumentation and Methods for Use in Agriculture, Industry and Medicine·T J VisserW Vaalburg
May 1, 1996·Journal of Nuclear Cardiology : Official Publication of the American Society of Nuclear Cardiology·G MünchM Schwaiger
Aug 26, 1999·Journal of Nuclear Cardiology : Official Publication of the American Society of Nuclear Cardiology·A J Fischman
Oct 1, 2003·Clinical Positron Imaging : Official Journal of the Institute for Clinical P.E.T·Philip H. ElsingaWillem Vaalburg
Sep 19, 2002·British Journal of Pharmacology·Jillian G BakerStephen J Hill
Apr 1, 1997·European Journal of Drug Metabolism and Pharmacokinetics·A StammatiG Brambilla
Mar 10, 2006·Current Cardiology Reports·Takahiro Higuchi, Markus Schwaiger
May 8, 2010·Nuclear Medicine and Biology·Marilyn P LawMichael Schäfers
Mar 28, 2007·Heart Failure Clinics·Takahiro Higuchi, Markus Schwaiger
Aug 4, 2010·Journal of Nuclear Medicine : Official Publication, Society of Nuclear Medicine·Marilyn P LawMichael Schäfers

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