444902-32-3Relevant articles and documents
Synthesis and in-vivo evaluation of [11C]p-PVP-MEMA as a PET radioligand for imaging nicotinic receptors
Dolle, Frederic,Langle, Sandrine,Roger, Gaelle,Fulton, Roger R.,Lagnel-De Bruin, Beatrice,Henderson, David J.,Hinnen, Francoise,Paine, Taliesha,Coster, Mark J.,Valette, Heric,Bottlaender, Michel,Kassiou, Michael
, p. 438 - 445 (2008/12/20)
Within the class of (4-pyridinyl)vinylpyridines developed by Abbott laboratories as potent neuronal nicotinic acetylcholine receptor ligands, p-PVP-MEMA ({(R)-2-[6-chloro-5-((E)-2-pyridin-4-ylvinyl)pyridin-3-yloxy]-1- methylethyl}methylamine) is the lead compound of a novel series that do not display the traditional nicotinic-like pyrrole-ring but still possessing high subnanomolar affinity (Ki 0.077 nm?displacement of [ 3H](?)cytisine from whole rat brain synaptic membranes). In the present study, p-PVP-MEMA and its nor-derivative ({(R)-2-[6-chloro-5-((E)-2- pyridin-4-ylvinyl)pyridin-3-yloxy]-1-methylethyl}methylamine) as precursor for labelling with the short-lived positron-emitter carbon-11 (T1/2 20.4 min) were synthesized in 10 chemical steps from 2-hydroxy-5-nitropyridine and Boc-d-alanine. N-Alkylation of nor-p-PVP-MEMA with [11C]methyl iodide afforded [11C]p-PVP-MEMA (>98% radiochemically pure, specific activity of 86.4 GBq ?mol?1) in 2% (non-decay corrected and non-optimized) radiochemical yield, in 34 min (including HPLC purification and formulation). Preliminary positron emission tomography (PET) results obtained in a Papio hamadryas baboon showed that [11C]p-PVP-MEMA is not a suitable PET-radioligand. CSIRO 2008.
Fused heterocyclic succinimide compounds and analogs thereof, modulators of nuclear hormone receptor function
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, (2008/06/13)
Fused cyclic compounds, methods of using such compounds in the treatment of nuclear hormone receptor-associated conditions such as cancer and immune disorders, and pharmaceutical compositions containing such compounds.