Carbon-11 labelling of 8[[3-[4-(2-[(11)C]methoxyphenyl)piperazin-1-yl]-2-hydroxypropyl]oxy]thiochroman, a presynaptic 5-HT(1A) receptor agonist, and its in vivo evaluation in anaesthetised rat and in awake cat.
A new compound, 8[[3-[4-(2-[(11)C]methoxyphenyl)piperazin-1-yl]-2-hydroxypropyl]oxy]thiochroman was labeled via O-methylation with [(11)C]methyl iodide in good yield and specific activity. Original biological evaluations included (i) the study in anesthetized rat with a beta-sensitive intracerebral probe (beta-Microprobe), allowing to measure locally the kinetic of the new PET ligand, and (ii) a PET-scan on a conditioned cat maintained awake during the acquisition. In both in vivo techniques, the new ligand did not reveal any specific binding in hippocampus indicating that this radiotracer is not suitable for mapping 5HT(1A) receptors using positron emission tomography.
Zimmer
Luc
L
CERMEP, Biomedical Cyclotron, 59 Bd Pinel, 69003 Lyon, France.
Fournet
Guy
G
Benoît
Joseph
J
Guillaumet
Gérald
G
Le Bars
Didier
D
D000758:Anesthesia; D000818:Animals; D001921:Brain / Q000000981:diagnostic imaging* / Q000378:metabolism*; D002415:Cats; D007553:Isotope Labeling / Q000379:methods; D008297:Male; D008657:Metabolic Clearance Rate; D010879:Piperazines / Q000138:chemical synthesis / Q000493:pharmacokinetics*; D011877:Radionuclide Imaging; D019275:Radiopharmaceuticals / Q000138:chemical synthesis / Q000493:pharmacokinetics; D051381:Rats; D017207:Rats, Sprague-Dawley; D017661:Receptors, Presynaptic / Q000037:antagonists & inhibitors / Q000378:metabolism; D044263:Receptors, Serotonin, 5-HT1 / Q000378:metabolism*; D058829:Serotonin 5-HT1 Receptor Antagonists; D013876:Thiophenes / Q000138:chemical synthesis / Q000493:pharmacokinetics*; D014018:Tissue Distribution; D014474:Unconsciousness; D014851:Wakefulness / Q000502:physiology
C483766:8-((3-(4-(2-methoxyphenyl)piperazin-1-yl)-2-hydroxypropyl)oxy)thiochroman; D010879:Piperazines; D019275:Radiopharmaceuticals; D017661:Receptors, Presynaptic; D044263:Receptors, Serotonin, 5-HT1; D058829:Serotonin 5-HT1 Receptor Antagonists; D013876:Thiophenes