Interaction of chiral MS-245 analogs at h5-HT6 receptors

被引：18
作者：
Abate, C
Kolanos, R
Dukat, M
Setola, V
Roth, BL
Glennon, RA [1 ]
机构：
[1] Virginia Commonwealth Univ, Dept Med Chem, Sch Pharm, Richmond, VA 23298 USA
[2] Case Western Reserve Univ, Dept Biochem, Cleveland, OH 44106 USA
[3] Case Western Reserve Univ, Dept Psychiat & Neurosci, Sch Med, Cleveland, OH 44106 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2005年 / 15卷 / 15期
关键词：
serotonin; pyrrolidinylmethylindoles;
D O I：
10.1016/j.bmcl.2005.05.092
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Optically active pyrrolidinylmethylindole analogs related in structure to the benzenesulfonyltryptantine 5-HT6 receptor antagonist MS-245 were evaluated and their R-isomers were found to bind with affinity higher than their S-enantiomers. (c) 2005 Elsevier Ltd. All rights reserved.
引用
收藏
页码：3510 / 3513
页数：4
相关论文
共 20 条
  • [1] Discovery of 5-arylsulfonamido-3(pyrrolidin-2-ylmethyl)-1H-indole derivatives as potent, selective 5-HT6 receptor agonists and antagonists
    Cole, DC
    Lennox, WJ
    Lombardi, S
    Ellingboe, JW
    Bernotas, RC
    Tawa, GJ
    Mazandarani, H
    Smith, DL
    Zhang, GM
    Coupet, J
    Schechter, LE
    [J]. JOURNAL OF MEDICINAL CHEMISTRY, 2005, 48 (02) : 353 - 356
  • [2] BENZAZEPINONE CALCIUM-CHANNEL BLOCKERS .2. STRUCTURE-ACTIVITY AND DRUG-METABOLISM STUDIES LEADING TO POTENT ANTIHYPERTENSIVE AGENTS - COMPARISON WITH BENZOTHIAZEPINONES
    FLOYD, DM
    KIMBALL, SD
    KRAPCHO, J
    DAS, J
    TURK, CF
    MOQUIN, RV
    LAGO, MW
    DUFF, KJ
    LEE, VG
    WHITE, RE
    RIDGEWELL, RE
    MORELAND, S
    BRITTAIN, RJ
    NORMANDIN, DE
    HEDBERG, SA
    CUCINOTTA, GG
    [J]. JOURNAL OF MEDICINAL CHEMISTRY, 1992, 35 (04) : 756 - 772
  • [3] 2-Substituted tryptamines:: Agents with selectivity for 5-HT6 serotonin receptors
    Glennon, RA
    Lee, M
    Rangisetty, JB
    Dukat, M
    Roth, BL
    Savage, JE
    McBride, A
    Rauser, L
    Hufeisen, S
    Lee, DKH
    [J]. JOURNAL OF MEDICINAL CHEMISTRY, 2000, 43 (05) : 1011 - 1018
  • [4] Glennon RA, 1999, MED CHEM RES, V9, P108
  • [5] Higher-end serotonin receptors:: 5-HT5, 5-HT6, and 5-HT7
    Glennon, RA
    [J]. JOURNAL OF MEDICINAL CHEMISTRY, 2003, 46 (14) : 2795 - 2812
  • [6] Medicinal chemistry driven approaches toward novel and selective serotonin 5-HT6 receptor ligands
    Holenz, J
    Mercè, R
    Díaz, JL
    Guitart, X
    Codony, X
    Dordal, A
    Romero, G
    Torrens, A
    Mas, J
    Andaluz, B
    Hernández, S
    Monroy, X
    Sánchez, E
    Hernández, E
    Pérez, R
    Cubí, R
    Sanfeliu, O
    Buschmann, H
    [J]. JOURNAL OF MEDICINAL CHEMISTRY, 2005, 48 (06) : 1781 - 1795
  • [7] Molecular, pharmacological and functional diversity of 5-HT receptors
    Hoyer, D
    Hannon, JP
    Martin, GR
    [J]. PHARMACOLOGY BIOCHEMISTRY AND BEHAVIOR, 2002, 71 (04) : 533 - 554
  • [8] A PROPOSED NEW NOMENCLATURE FOR 5-HT RECEPTORS
    HUMPHREY, PPA
    HARTIG, P
    HOYER, D
    [J]. TRENDS IN PHARMACOLOGICAL SCIENCES, 1993, 14 (06) : 233 - 236
  • [9] Kohen R, 1996, J NEUROCHEM, V66, P47
  • [10] Binding of isotryptamines and indenes at h5-HT6 serotonin receptors
    Kolanos, R
    Siripurapu, U
    Pullagurla, M
    Riaz, M
    Setola, V
    Roth, BL
    Dukat, M
    Glennon, RA
    [J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2005, 15 (08) : 1987 - 1991
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