| Literature DB >> 16039851 |
Tom D Heightman1, Laramie M Gaster, Sarah L Pardoe, Jean-Pierre Pilleux, Michael S Hadley, Derek N Middlemiss, Gary W Price, Claire Roberts, Claire M Scott, Jeannette M Watson, Laurie J Gordon, Vicky A Holland, Jenifer Powles, Graham J Riley, Tania O Stean, Brenda K Trail, Neil Upton, Nigel E Austin, Andrew D Ayrton, Tanya Coleman, Leanne Cutler.
Abstract
The novel 8-piperazinyl-2,3-dihydropyrroloisoquinoline template was synthesized in nine steps. The template was N-substituted to give a series of compounds showing binding to human cloned 5-HT1A, 5-HT1B and 5-HT1D receptors with pKi's greater than 9 and selectivities up to 1000-fold against other serotonin, dopamine and adrenergic receptors. Several compounds were shown to possess weak partial agonist activity in cloned receptors, which translated to antagonism in in vitro studies.Entities:
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Year: 2005 PMID： 16039851 DOI： 10.1016/j.bmcl.2005.06.042
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823