SEROTONIN-5-O-CARBOXYMETHYL-GLYCYL[I-125]TYROSINAMIDE LABELS THE 5-HT(1D-BETA)-RECEPTOR SUBTYPE IN HUMAN CORTEX

被引:17
作者
BEER, MS
MIDDLEMISS, DN
机构
[1] Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Harlow, Essex CM20 2QR, Terlings Park, Eastwick Road
关键词
SEROTONIN-5-O-CARBOXYMETHYL-GLYCYL[I-125]TYROSINAMIDE ([I-125]GTI); 5-HT(1D-ALPHA/BETA)-RECEPTORS; CEREBRAL CORTEX (HUMAN);
D O I
10.1016/0014-2999(93)90080-2
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
This study, carried out in human cerebral cortical membranes, confirms previous findings in human substantia nigra that serotonin-5-O-carboxymethyl-glycyl[I-125]tyrosinamide ([I-125]GTI) labels a homogeneous population of recognition sites consistent with a 5-HT1D receptor pharmacology. In addition the results indicate that, under the assay conditions described, [I-125]GTI specifically labels the 5-HT1Dbeta recognition site since ketanserin and ritanserin display a low affinity consistent with their activities at this subtype of the 5-HT1D receptor.
引用
收藏
页码:195 / 198
页数:4
相关论文
共 12 条
  • [1] CLONING OF ANOTHER HUMAN SEROTONIN RECEPTOR (5-HT1F) - A 5TH 5-HT1 RECEPTOR SUBTYPE COUPLED TO THE INHIBITION OF ADENYLATE-CYCLASE
    ADHAM, N
    KAO, HT
    SCHECHTER, LE
    BARD, J
    OLSEN, M
    URQUHART, D
    DURKIN, M
    HARTIG, PR
    WEINSHANK, RL
    BRANCHEK, TA
    [J]. PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1993, 90 (02) : 408 - 412
  • [2] AN INVESTIGATION OF THE 5-HT1D RECEPTOR-BINDING AFFINITY OF 5-HYDROXYTRYPTAMINE, 5-CARBOXYAMIDOTRYPTAMINE AND SUMATRIPTAN IN THE CENTRAL-NERVOUS-SYSTEM OF 7 SPECIES
    BEER, MS
    STANTON, JA
    BEVAN, Y
    CHAUHAN, NS
    MIDDLEMISS, DN
    [J]. EUROPEAN JOURNAL OF PHARMACOLOGY, 1992, 213 (02) : 193 - 197
  • [3] BOULENGUEZ P, 1991, J PHARMACOL EXP THER, V259, P1360
  • [4] HOMOGENEOUS 5-HT1D RECOGNITION SITES IN THE HUMAN SUBSTANTIA-NIGRA IDENTIFIED WITH A NEW IODINATED RADIOLIGAND
    BRUINVELS, AT
    LANDWEHRMEYER, B
    WAEBER, C
    PALACIOS, JM
    HOYER, D
    [J]. EUROPEAN JOURNAL OF PHARMACOLOGY, 1991, 202 (01) : 89 - 91
  • [5] CHENG Y, 1973, BIOCHEM PHARMACOL, V22, P3099
  • [6] THE GENOMIC CLONE G-21 WHICH RESEMBLES A BETA-ADRENERGIC-RECEPTOR SEQUENCE ENCODES THE 5-HT1A RECEPTOR
    FARGIN, A
    RAYMOND, JR
    LOHSE, MJ
    KOBILKA, BK
    CARON, MG
    LEFKOWITZ, RJ
    [J]. NATURE, 1988, 335 (6188) : 358 - 360
  • [7] A SUBFAMILY OF 5-HT1D RECEPTOR GENES
    HARTIG, PR
    BRANCHEK, TA
    WEINSHANK, RL
    [J]. TRENDS IN PHARMACOLOGICAL SCIENCES, 1992, 13 (04) : 152 - 159
  • [8] HEURING RE, 1987, J NEUROSCI, V7, P894
  • [9] SPECIES-DIFFERENCES IN THE PHARMACOLOGY OF TERMINAL 5-HT AUTORECEPTORS IN MAMMALIAN BRAIN
    HOYER, D
    MIDDLEMISS, DN
    [J]. TRENDS IN PHARMACOLOGICAL SCIENCES, 1989, 10 (04) : 130 - 132
  • [10] MOLECULAR CHARACTERIZATION OF A FUNCTIONAL CDNA-ENCODING THE SEROTONIN 1C RECEPTOR
    JULIUS, D
    MACDERMOTT, AB
    AXEL, R
    JESSELL, TM
    [J]. SCIENCE, 1988, 241 (4865) : 558 - 564