- PHENYLSULFONAMIDE-PHENYLETHYLAMINES USEFUL AS DOPAMINE RECEPTORS
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Compounds of Formula I and their pharmaceutically acceptable salts having selective dopamine D3 receptor activity suitable for treating central nervous system disorders. Formula I: R1 is independently H or a C1-C8 alkyl including isomeric forms thereof; R
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Page/Page column 6
(2008/06/13)
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- PHENYLSULFONAMIDE-PHENYLETHYLAMINES USEFUL AS DOPAMINE RECEPTORS
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Compounds of Formula I and their pharmaceutically acceptable salts having selective dopamine D3 receptor activity suitable for treating central nervous system disorders. Formula I: STR1 R 1 is independently H or a C. sub.1-C 8 alkyl including isomeric forms thereof;R 2 is H, C 1-C 3 alkyl, a halogen, OCH 3 , OCF 3, CF 3, CN, SCH 3 or NHCOCH 3 ; andR 3 is H, C 1-C 3 alkyl, a halogen, OCH 3 , OCF 3, CF 3, CN, SCH 3 or NHCOCH 3.
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- Partial dopamine receptor agonists with different degrees of intrinsic activity within a series of 2-(4-aminophenyl)-N,N-dipropylethylamine derivatives: Synthetic chemistry and structure-activity relationships
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A series of 2-(4-aminophenyl)-N,N-dipropylethylamine derivatives were synthesized and tested for in vivo intrinsic activity at brain dopamine receptors in the rat. Differences in the sensitivity of dopamine receptors pre- and post-synaptically in the reserpine-treated rat were used to estimate the intrinsic activity of the various compounds as dopamine receptor agonists. Thus, the ability of the compounds to antagonize reserpine-induced increase in neostriatal dopamine synthesis and the suppression of spontaneous locomotor activity were taken as pre- and post-synaptic indices, respectively. The compounds in the present series display a gradient of intrinsic activity depending on the substituents in the aromatic ring. The presence of an amino group or an appropriate acylamino group in the 4-position was found to be critical for the biological activity of these compounds as agonists or antagonists. The introduction of halogen or a trifluoromethyl group in the 3-position resulted in high intrinsic activity (ie, agonist activity). The incorporation of a methyl group in the 3-position or halogens in the 3,5-positions resulted in a gradual decrease in intrinsic activity at rat brain dopamine receptors resulting in a series of compounds ranging from a full agonist to dopamine receptor blockade.
- Florvall,Hillegaart,Malmberg,Wijkstroem,Ahlenius
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p. 133 - 142
(2007/10/03)
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- Design, synthesis and properties of several heterocyclic dopaminergic ligands
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Two series of non-catechol dopamine (DA) bioisosteres with the hydroxyl groups on the benzene ring replaced by N-H groups were synthesized using phenethylamine as a parent molecule. Compounds from the first series (1-9) contained a primary amine group, wh
- Kostic,Soskic,Joksimovic
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p. 697 - 702
(2007/10/02)
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