8-Piperazinyl-2,3-dihydropyrrolo[3,2-g]isoquinolines: potent, selective, orally bioavailable 5-HT1 receptor ligands.

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 oth...

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Bibliographic Details
Main Authors: Heightman, T, Gaster, L, Pardoe, S, Pilleux, J, Hadley, MS, Middlemiss, D, Price, G, Roberts, C, Scott, C, Watson, J, Gordon, L, Holland, V, Powles, J, Riley, G, Stean, T, Trail, B, Upton, N, Austin, N, Ayrton, A, Coleman, T, Cutler, L
Format: Journal article
Language:English
Published: 2005