[(18)F]Fluspidine demonstrated favourable target affinity and specificity as well as metabolic stability both in vitro and in animal experiments. The in vivo properties of [(18)F]fluspidine offer a high potential of this radiotracer for neuroimaging and quantitation of σ(1) receptors in vivo.
A series of various N-substituted 3-(3-fluoropropyl)-3H-spiro[[2]benzofuran-1,4'-piperidines] (7) has been synthesized. In receptor binding studies, the N-benzyl derivative 7a (WMS-1813) revealed extraordinarily high sigma(1) receptor affinity (K(i) = 1.4 nM) and excellent sigma(1)/sigma(2) selectivity (>600 fold). In vitro biotransformation of 7a with rat liver microsomes led to three main metabolites. N-Debenzylation was inhibited by introduction of an N-phenylethyl residue (7 g). The PET tracer [(18)F]7a was synthesized by nucleophilic substitution of the tosylate 13 with K[(18)F]F-K222-carbonate complex. The decay corrected radiochemical yield of [(18)F]7a was 35-48% with a radiochemical purity of >99.5% and a specific activity of 150-238 GBq/micromol. The radiotracer properties were evaluated in female CD-1 mice by organ distribution and ex vivo brain autoradiography. The radiotracer uptake in the brain was fast and sufficient, with values of approximately 4% injected dose per gram. Target specificity of [(18)F]7a was validated in blocking studies by preapplication of haloperidol, and significant reduction in the uptake of radioactivity was observed in the brain and peripheral organs expressing sigma(1) receptors.
Solidified stomach oil deposits in snow petrel colonies in the Antarctic proved to be suitable for 14C dating and provide important palaeobiogeographical and palaeoenvironmental information. Following earlier studies in the Untersee oasis (Central Dronning Maud Land) we present here 14C measurements on comparable deposits from the Bunger Hills (66°10′S, 101°E). The conventional 14C age of the basal layer reflects the occupation age of any particular nesting site and therefore a minimum age for the time when this area became ice-free. According to the 14C results the occupation of the southern part of the Bunger Hills by petrels started about 10000yr ago. The breeding colonies expanded continuously following local ice retreat. The most intensive phases of colonization seem to have been from 8–6 kyr BP and during the past 2 kyr.
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