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Chemical Name:3-(4-[4-Chlorophenyl]piperazin-1-yl)-methyl-1H-pyrrolo[
2,3-b]pyridine trihydrochloride
Biological Activity:
A highly potent and selective D4 dopamine receptor
antagonist; L-745,870 has Ki values of 0.51, 2300 and 960 nM for D4,
D3 and D2 subtypes respectively and > 1000-fold
selectivity over 5-HT2 , D1 and D5 receptors.
Kulagowski et al (1996)
3-[[4-(4-Chlorophenyl)piperazin-1-yl]methyl-1H-pyrrolo[2,3-b]pyridine: an
antagonist with high affinity and selectivity for the human D4
receptor. J. Med. Chem. 39 1941. Bristowetal (1997)
Schizophrenia and L-745, 870 a novel dopamine D4 receptor
antagonist. TiPS 18 186. Patelet al (1997)
Biological profile of L-745,870, a selective antagonist with high affinity for
the dopamine D4 receptor. J.Pharmacol.Exp.Ther. 283
636. Pillaiet al (1998) Human D2 and D4 dopamine
receptors couple through bg G-protein subunits to inwardly rectifying K+
channels (GIRK1) in a Xenopus oocyte expression system: selective
antagonism by L-741,626 and L-745,870 respectively. Neuropharmacology 37
983.
