Synthesis of 3-[[4-(4-[18F] fluorophenyl)piperazin-1-yl]methyl]-1H-pyrrolo[2,3-b]pyridine
3-[[4-(4-[18F]fluorophenyl)piperazin-1-yl]methyl] -1H-pyrrolo[2,3-b]pyridine, a candidate to image dopamine D4 receptors, was synthesised via electrophilic fluorination of a trimethylstannyl precursor with high specific radioactivity
3-[[4-(4-Chlorophenyl)piperazin-1-yl]-methyl]-1H-pyrrolo[2,3-b]pyridine: An antagonist with high affinity and selectivity for the human dopamine D4 receptor
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Kulagowski, Janusz J.,Broughton, Howard B.,Curtis, Neil R.,Mawer, Ian M.,Ridgill, Mark P.,Baker, Raymond,Emms, Frances,Freedman, Stephen B.,Marwood, Rosemarie,Patel, Shil,Patel, Smita,Ragan, C. Ian,Leeson, Paul D.
p. 1941 - 1942
(2007/10/03)
Pyrrolo-pyridine derivatives
A class of pyrrolo[2,3-b]pyridine derivatives, substituted at the 3-position by a substituted piperazinylmethyl moiety, are antagonists of dopamine receptor subtypes within the brain, having a selective affinity for the dopamine D 4 receptor subtype over other dopamine receptor subtypes, and are accordingly of benefit in the treatment and/or prevention of psychotic disorders such as schizophrenia while manifesting fewer side-effects than those associated with classical neuroleptic drugs.
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(2008/06/13)
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