Výsledky vyhledávání - "Chiu Hong Lin"

Dopamine D3 Receptor Antagonists. 1. Synthesis and Structure−Activity Relationships of 5,6-Dimethoxy-N-alkyl- and N-Alkylaryl-Substituted 2-Aminoindans

Autor: Martin W. Smith, Kjell Svensson, Matt J. Zaya, Susanne R. Haadsma-Svensson, Mary E. Lajiness, Nanette F. Nichols, Chiu-Hong Lin, Rita M. Huff, Christopher L. Haber, Kerry Anne Cleek, J. Neil Duncan, Dac M. Dinh, and Arvid Carlsson

Publikováno v: Journal of Medicinal Chemistry. 44:4716-4732

5,6-Dimethoxy-2-(N-dipropyl)-aminoindan (3, PNU-99194A) was found to be a selective dopamine D(3) receptor antagonist with potential antipsychotic properties in animal models. To investigate the effects of nitrogen substitution on structure-activity

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::50895a57b406c01e185736e122556b86
https://doi.org/10.1021/jm010145w

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Synthesis of isotopically labeled CIS-(3aR)-(-)-2,3,3a,4,5,9b-hexahydro-3-(N-propyl)-1H-benz[e]indole-9-carboxamide, a 5-HT1A receptor agonist

Autor: Wayne T. Stolle, Richard S. P. Hsi, Susanne R. Haadsma-Svensson, Chiu-Hong Lin, Mark J. Ackland, John A. Easter

Publikováno v: Journal of Labelled Compounds and Radiopharmaceuticals. 39:891-900

The title compound is a potent and selective 5-HT 1A receptor agonist with clinical potentials for treating anxiety and depression. It has been labeled with stable and radioactive isotopes to support ADME studies in animals and human subjects. Its ca

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::a8c4b82a6b4c5a1305e11b7c8a53f8bc
https://doi.org/10.1002/(sici)1099-1344(199711)39:11<891::aid-jlcr34>3.0.co

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(Dipropylamino)-tetrahydronaphthofurans: centrally acting serotonin agonists and dopamine agonists-antagonists

Autor: Stjernlöf P, Clas Sonesson, Kjell Svensson, Chiu-Hong Lin, Martin W. Smith

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 7:2759-2764

CNS-active aminotetralins containing phenolic moieties were transformed in a simple two-step procedure to the corresponding benzofurans. The compounds were tested in in vitro binding studies at serotonin 5-HT1A and 5-HT2 and dopamine D2, D3 and D4 re

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::9b32f3c076e1defee58eaa04f3152180
https://doi.org/10.1016/s0960-894x(97)10068-3

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Structure-Activity Relationships in the 8-Amino-6,7,8,9-tetrahydro-3H-benz[e]indole Ring System. Part 2: Effect of 8-Amino Nitrogen Substitution on Serotonin Receptor Binding and Pharmacology

Autor: Chiu-Hong Lin, Håkan Wikström, Ennis, Stjernlöf P, Nabil B. Ghazal, Kjell A. Svensson, Robert Louis Hoffman, M. W. Smith, Haadsma-Svensson

Publikováno v: Journal of Medicinal Chemistry, 38(12), 2217-2230. AMER CHEMICAL SOC

A series of analogs of the potent and selective 5-HT1A agonist 8-(di-n-propylamino)-6,7,8,9-tetrahydro-3H-benz[e]indole-1-carbaldehyde (2b) (OSU191) was prepared in which the dipropylamino group was modified to bear a variety of substituents. These c

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1675e7c91edcdcbeb73466dbd9cde2df
https://doi.org/10.1021/jm00012a022

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C-9 and N-Substituted Analogs of cis-(3aR)-(-)-2,3,3a,4,5,9b-Hexahydro-3-propyl-1H-benz[e]indole-9-carboxamide: 5-HT1A Receptor Agonists with Various Degrees of Metabolic Stability

Autor: Chiu-Hong Lin, Neil Duncan, Kjell Svensson, Susanne R. Haadsma-Svensson, M. W. Smith

Publikováno v: Journal of Medicinal Chemistry. 38:725-734

Closely related analogs of the 5-HT 1A receptor agonist cis-(3aR)-(-)-2,3,3a,4,5,9b-hexahydro-3-propyl-1H-benz[e]indole-9-carboxamide (1, U93385) were synthesized and pharmacologically evaluated. 9-Carboxamide analogs with varied nitrogen substitutio

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f2953485c308b7d3c7cac55d2cbb69c0
https://doi.org/10.1021/jm00004a018

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substituted (S)-Phenylpiperidines and Rigid Congeners as Preferential Dopamine Autoreceptor Antagonists: Synthesis and Structure-Activity Relationships

Autor: Arvid Carlsson, M. W. Smith, Kjell A. Svensson, Chiu-Hong Lin, Nicholas Waters, Håkan Wikström, Lars O. Hansson, Clas Sonesson

Publikováno v: Journal of Medicinal Chemistry. 37:2735-2753

A series of (S)-phenylpiperidines in which the substituents on the aromatic ring and nitrogen have been varied has been prepared. They have been evaluated pharmacologically to explore the importance of these substituents for the interaction with cent

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fe7035f690f32429555d4288e1a43e98
https://doi.org/10.1021/jm00043a013

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Synthesis and biological activity of C-5 modified derivatives of (+)-AJ76 and (+)-UH232: Increased dopamine D3 receptor preference and improved pharmacokinetic properties

Autor: Kjell Svensson, Nicholas Waters, Clas Sonesson, J. Neil Duncan, Arvid Carlsson, H»kan Wikström, M. W. Smith, Chiu-Hong Lin, Susanne R. Haadsma-Svensson

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 4:689-694

A series of (+)-AJ76 and (+)-UH232 analogs with the C-5 methoxy group modified was synthesized and biologically evaluated. Compounds with a triflate or nitrile group were found to be behavioral stimulants with high metabolic stability. The triflate a

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::424a5e415ffdb26beddfb35c84ee134c
https://doi.org/10.1016/s0960-894x(01)80181-5

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Synthesis of (r)- and (s)-1-formyl-6,7,8,9-tetrahydro-N,N-(dipropyl)-3H-benz[e]indol-8-amines: Potent and orally active 5-ht1areceptor agonists

Autor: N. B. Ghazal, Robert L. Hoffman, Michael D. Ennis, C. G. Chidester, Chiu-Hong Lin, G. Phillips, Susanne R. Haadsma-Svensson

Publikováno v: Journal of Heterocyclic Chemistry. 31:129-139

An efficient synthesis of the potent and orally active 5-HT 1A agonists, (R)-(+)- and (S)-(-)-1-formyl-6,7,8,9-tetrahydro-N,N-dipropyl-3H-benz[e]indol-8-amines 1a and 1b, is described. This synthesis was accomplished in twelve steps from commercially

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::4a110d46c9abdbf752b2be4b7d995a71
https://doi.org/10.1002/jhet.5570310123

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Synthesis and biological activity of cis-(3aR)-(-)-2,3,3a,4,5,9b-hexahydro-3-propyl-1H-benz[e]indole-9-carboxamide: A potent and selective 5-HT1A receptor agonist with good oral availability

Autor: Robert B. McCall, G. Phillips, Chiu-Hong Lin, C. G. Chidester, Montford F. Piercey, Kjell A. Svensson, M. W. Smith, Susanne R. Haadsma-Svensson, P. F. Von Voigtlander, Arvid Carlsson

Publikováno v: Journal of Medicinal Chemistry. 36:2208-2218

The synthesis and biological activity of cis-(3aR)-(-)-2,3,3a,4,5,9b- hexahydro-3-propyl-1H-benz[e]indole-9-carboxamide ((-)-3a), U93385, is described. The cis racemate and its enantiomer as well as the corresponding trans enantiomers were also synth

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0d36e0beb2ab84b15d7a18c18bf89062
https://doi.org/10.1021/jm00067a018

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Comparison of 5-HT1A and dopamine D2 pharmacophores. X-ray structures and affinities of conformationally constrained ligands

Autor: Robert A. Lahti, M. W. Smith, C. G. Chidester, Chiu Hong Lin, Susanne R. Haadsma-Svensson

Publikováno v: Journal of Medicinal Chemistry. 36:1301-1315

Conformational and molecular mechanics studies of a new series of tricyclic ligands with affinity for either the dopamine D2 receptor or the 5-HT1A receptor, or both, has enabled us to elaborate considerably on previous pharmacophore models for these

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d19f1dca16de0da5ca3717523bbfacb7
https://doi.org/10.1021/jm00062a001

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