Thiazoloindans and thiazolobenzopyrans: A novel class of orally active central dopamine (partial) agonists

Journal of Medicinal Chemistry

Volumn 43, Issue 19, 2000, Pages 3549-3557

  Van Vliet, L A ^a   Rodenhuis, N ^a   Wikstrom, H ^a   Pugsley, T A ^b   Serpa, K A ^b   Meltzer, L T ^b   Heffner, T G ^b   Wise, L D ^b   Lajiness, M E ^b   Huff, R M ^b   Svensson, K ^b   Haenen, G R M M ^c   Bast, A ^c  

^a UNIVERSITY OF GRONINGEN   (Netherlands)

^b PFIZER INC   (United States)

^c MAASTRICHT UNIVERSITY   (Netherlands)

Author keywords

[No Author keywords available]

Indexed keywords

2 AMINOTHIAZOLE DERIVATIVE; 6 AMINO 2 (N,N DI N PROPYLAMINO)THIAZOLO[4,5 F]INDAN; 6 AMINO 3 (N,N DI N PROPYLAMINO) 3,4 DIHYDRO 2H THIAZOLO[5,4 F] [1]BENZOPYRAN; BENZOPYRAN DERIVATIVE; DOPAMINE 2 RECEPTOR; DOPAMINE 3 RECEPTOR; DOPAMINE RECEPTOR STIMULATING AGENT; GMC 1111; HALOPERIDOL; INDAN DERIVATIVE; OXIDOPAMINE; QUINPIROLE; SPIPERONE; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANTIOXIDANT ACTIVITY; ARTICLE; CHO CELL; CIRCLING BEHAVIOR; CONTROLLED STUDY; CORPUS STRIATUM; DOPAMINE METABOLISM; DRUG BIOAVAILABILITY; DRUG DETERMINATION; DRUG RECEPTOR BINDING; DRUG SYNTHESIS; LIPID PEROXIDATION; MICRODIALYSIS; NONHUMAN; PARKINSON DISEASE; RAT; RECEPTOR AFFINITY;

ADMINISTRATION, ORAL; ANIMALS; BINDING, COMPETITIVE; CELL DIVISION; CHO CELLS; CORPUS STRIATUM; CRICETINAE; DOPAMINE AGONISTS; DRUG EVALUATION, PRECLINICAL; FREE RADICAL SCAVENGERS; HUMANS; INDANS; LIPID PEROXIDATION; MICRODIALYSIS; PYRANS; RATS; RECEPTORS, DOPAMINE; STEREOTYPED BEHAVIOR; STRUCTURE-ACTIVITY RELATIONSHIP; THIAZOLES;

EID: 0034699497     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm000087z     Document Type: Article

References (31)

1. Oxidants and the central nervous system: Some fundamental questions. Is oxidant damage relevant to Parkinson's disease, Alzheimer's disease, traumatic injury or stroke?
2. Reactive oxygen species and the central nervous system
3. Peripheral markers of oxidative stress in Parkinson's disease. The role of L-DOPA
4. Free Radical Scavengers: Chemical Concepts and Clinical Relevance
5. The role of dopamine agonists in early Parkinson's disease
6. Effects of B-HT 920 and B-HT 933 on dopamine and noradrenaline autoreceptors in the rat brain
7. 4-(1,2,5,6-tetrahydro-1-alkyl-3-pyridinyl)-2-thiazolamines: A novel class of compounds with central dopamine agonist properties
8. 4 receptors
9. Dopamine autoreceptor agonists: Resolution and pharmacological activity of 2,6-diaminotetrahydrobenzothiazole and an aminothiazole analogue of apomorphine
10. Coquelet, C. 2-(2-hydroxy-4-methylphenyl)-aminothiazole hydrochloride as a dual inhibitor of cyclooxygenase/lipoxygenase and a free radical scavenger. 2nd communication: Antiinflammatory activity
11. Neuroprotective effects of the dopamine D2/D3 agonist pramipexole against postischemic or methamphetamine-induced degeneration of nigrostriatal neurons
12. The reaction of thiocyanogen with nitrogen heterocycles; pyridines, pyrimidines and quinolines
13. Stereoselective synthesis of cis- and trans-3-amino-4-chromanols
14. Structure-activity relationships in the 8-amino-6,7,8,9-tetrahydro-3H-benz[e]indole ring system. 1. Effects of substituents in the aromatic system on serotonin and dopamine receptor subtypes
15. Comparison of biological effects of n-alkylated congeners of β-phenethylamine derived from 2-aminotetralin, 2-aminoindan, and 6-aminobenzocycloheptene
16. Protection against lipid peroxidation by a microsomal glutathione-dependent labile factor
17. D2 dopamine receptor stimulation of mitogenesis in transfected Chinese hamster ovary cells: Relationship to dopamine stimulation of tyrosine phosphorylations
18. Activation of heterologously expressed D3 dopamine receptors: Comparison with D2 dopamine receptors
19. Postsynaptic supersensitivity after 6-hydroxydopamine induced degeneration of the nigro-striatal dopamine system
20. Quantitative recording of rotational behavior in rats after 6-hydroxy-dopamine lesions of the nigrostriatal dopamine system
21. 6- and 8-hydroxy-3,4-dihydro-3-(dipropylamino)-2H-1-benzopyrans. Dopamine agonists with autoreceptor selectivity
22. Monophenolic 2-(dipropylamino)indans and related compounds: Central dopamine-receptor stimulating activity
23. Affinity for dopamine D2, D3, and D4 receptors of 2-aminotetralins. Relevance of D2 agonist binding for determination of receptor subtype selectivity
24. Dopamine agonists: Intrinsic activity vs state of the receptor
25. Central dopamine receptor agonist and antagonist actions of the enantiomers of 3-PPP
26. The dopamine D3-receptor: A postsynaptic receptor inhibitory on rat locomotor activity
27. Locomotor inhibition by the D3 ligand R-(+)-7-OH-DPAT is independent of changes in dopamine release
28. Evidence that striatal synthesis-inhibiting autoreceptors are dopamine D3 receptors
29. Dopamine (DA) autoreceptor efficacy of 3-PPP enantiomers after short-term synaptic DA deprivation
30. 3 receptor selective agonist (4aR,10bR)-(+)-trans-3,4,4a,10b-tetrahydro-4-n-propyl-2h,5h-[1]benzopyrano[4, 3-b]-1,4-oxazin-9-ol (PD 128907)