PMID: 11918968Mar 29, 2002Paper

Synthesis and evaluation of (S)-[18F]-fluoroethylcarazolol for in vivo beta-adrenoceptor imaging in the brain

Neurochemistry International
P DozePhilip H. Elsinga

Abstract

The beta-adrenergic receptor ligand (S)-4-(3-(2'-[18F]-fluoroethylamino)-2-hydroxypropoxy)-carbazol ((S)-[18F]-fluoroethylcarazolol) was prepared by reaction of [18F]-fluoroethylamine with the corresponding (S)-epoxide and was evaluated in rats by studying its pharmacokinetics and its binding profile both in vitro and in vivo. In vitro, (S)-fluoroethylcarazolol binds preferentially to beta-adrenoceptors (pK(i)=9.3 for beta(1) and 9.4 for beta(2)) and has less affinity to 5HT(1A) and 5HT(1D) receptors (pK(i)=6.7 and 5.2). In vivo, standard uptake values (SUVs) up to 0.63+/-0.07 in cortical regions were found after 60 min. Metabolites (90%) appeared within 10 min in plasma, whereas, in brain 70-75% parent compound was found after 60 min. Clearance from plasma occurred within 5 min. Cerebral uptake could be blocked by 'cold' fluoroethylcarazolol in every region, except medulla. Uptake was also blocked by propranolol and pindolol, but not by WAY 100635. ICI 89406 hardly lowered [18F] levels in brain. ICI 118551 reduced uptake of [18F] in cerebellum (mainly beta(2)) by 30%. Specific binding (tissue minus medulla values) in various brain regions corresponded with those observed for [18F]-fluorocarazolol (r(2)=0.95) and with in vitro ...Continue Reading

References

Jul 21, 1998·Journal of the American College of Cardiology·M SchäfersP G Camici

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Citations

Oct 27, 2007·Neurochemistry International·Aren van WaardePhilip H Elsinga
Jun 14, 2006·Pediatric Radiology·Rosemary Arthur
Sep 10, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Santosh Reddy AlluriKun-Eek Kil

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