Autoradiographic distribution of [H-3]sumatriptan-binding sites in post-mortem human brain

被引:45
作者
Pascual, J [1 ]
delArco, C [1 ]
Romon, T [1 ]
delOlmo, E [1 ]
Castro, E [1 ]
Pazos, A [1 ]
机构
[1] UNIV CANTABRIA,UNIV HOSP MARQUES VALDECILLA,DEPT PHYSIOL & PHARMACOL,PHARMACOL UNIT,E-39008 SANTANDER,SPAIN
关键词
5HT(1D) receptor subtype; nucleus tractus solitarius; nucleus trigeminalis caudalis; quantitative autoradiography; H-3]sumatriptan;
D O I
10.1046/j.1468-2982.1996.1605317.x
中图分类号
R74 [神经病学与精神病学];
学科分类号
摘要
The anatomical distribution of [H-3]sumatriptan-binding sites was analysed in brain tissue sections from 11 subjects. Relevant concentrations of [3H]sumatriptan-binding sites were seen in areas such as visual cortex>locus niger>globus pallidus>layers IV-V of the frontal cortex>subiculum>entorhinal cortex>nucleus tractus solitarius>nucleus trigeminalis caudalis. This distribution of [H-3]sumatriptan-binding sites in the human brain shows some differences when compared with that of 5HT(1D) receptors, confirming that, besides 5HT(1D), sumatriptan also binds to 5HT(1F) receptor subtype. Some species differences are evident between the distribution of [H-3]sumatriptan-binding sites in the human brain and that reported for guinea-pig and rat brains, emphasizing that caution is needed in extrapolating experimental data from animals to humans. Furthermore, these data help to explain some of the therapeutic actions of sumatriptan. The remarkable levels of binding found in areas such as nucleus tractus solitarius and nucleus trigeminalis caudalis suggest that in migraine attacks sumatriptan could exert its specific anti-emetic effects and, partly at least, induce analgesia by directly acting over these brain nuclei.
引用
收藏
页码:317 / 322
页数:6
相关论文
共 28 条
[1]   CLONING OF ANOTHER HUMAN SEROTONIN RECEPTOR (5-HT1F) - A 5TH 5-HT1 RECEPTOR SUBTYPE COUPLED TO THE INHIBITION OF ADENYLATE-CYCLASE [J].
ADHAM, N ;
KAO, HT ;
SCHECHTER, LE ;
BARD, J ;
OLSEN, M ;
URQUHART, D ;
DURKIN, M ;
HARTIG, PR ;
WEINSHANK, RL ;
BRANCHEK, TA .
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1993, 90 (02) :408-412
[2]   MOLECULAR-BIOLOGY OF 5-HT RECEPTORS [J].
BOESS, FG ;
MARTIN, IL .
NEUROPHARMACOLOGY, 1994, 33 (3-4) :275-317
[3]   A COMPARATIVE AUTORADIOGRAPHIC STUDY OF 5-HT1D BINDING-SITES IN HUMAN AND GUINEA-PIG BRAIN USING DIFFERENT RADIOLIGANDS [J].
BRUINVELS, AT ;
LANDWEHRMEYER, B ;
PROBST, A ;
PALACIOS, JM ;
HOYER, D .
MOLECULAR BRAIN RESEARCH, 1994, 21 (1-2) :19-29
[4]   NEURAL MECHANISMS OF EMESIS [J].
CARPENTER, DO .
CANADIAN JOURNAL OF PHYSIOLOGY AND PHARMACOLOGY, 1990, 68 (02) :230-236
[5]  
delOlmo E, 1996, EUR J NEUROSCI, V8, P53
[6]   CLINICAL AND EXPERIMENTAL EFFECTS OF SUMATRIPTAN IN HUMANS [J].
FERRARI, MD ;
SAXENA, PR .
TRENDS IN PHARMACOLOGICAL SCIENCES, 1993, 14 (04) :129-133
[7]   MIGRAINE PAIN ASSOCIATED WITH MIDDLE CEREBRAL-ARTERY DILATATION - REVERSAL BY SUMATRIPTAN [J].
FRIBERG, L ;
OLESEN, J ;
IVERSEN, HK ;
SPERLING, B .
LANCET, 1991, 338 (8758) :13-17
[8]  
GOASDBY PJ, 1993, ANN NEUROL, P48
[9]   SEROTONIN RECEPTORS IN THE HUMAN-BRAIN .1. CHARACTERIZATION AND AUTORADIOGRAPHIC LOCALIZATION OF 5-HT1A RECOGNITION SITES - APPARENT ABSENCE OF 5-HT1B RECOGNITION SITES [J].
HOYER, D ;
PAZOS, A ;
PROBST, A ;
PALACIOS, JM .
BRAIN RESEARCH, 1986, 376 (01) :85-96
[10]  
HOYER D, 1994, PHARMACOL REV, V46, P157