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Chemical Name:3-[[4-(4-Chlorophenyl)-4-hydroxypiperidin-l-yl]methyl-1
H-indole
Biological Activity:
A
potent D2 dopamine receptor selective antagonist, with affinities of
2.4, 100 and 220 nM for D2, D3 and D4
receptors respectively. Centrally active following systemic administration in
vivo.
Kulagowskiet 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 dopamine D4
receptor.J.Med.Chem. 39 1941.
Boweryet al (1996) Antagonism of the effects of (+)-PD 128907 on
midbrain dopamine neurones in rat brain slices by a selective D2
receptor antagonist L-741,626. Br.J.Pharmacol. 119 1491. 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. Millanet al (2000) S33084, a novel, potent, selective, and competitive antagonist
at dopamine D3-receptors: II. Functional and behavioral profile compared with
GR218,231 and L741,626. J.Pharmacol.Exp.Ther. 293 1063.
