IN-VIVO LABELING OF NICOTINIC ACETYLCHOLINE-RECEPTORS IN BRAIN WITH [H-3] EPIBATIDINE

被引：40

作者：

LONDON, ED

SCHEFFEL, U

KIMES, AS

KELLAR, KJ

机构：

[1] JOHNS HOPKINS MED INST, BALTIMORE, MD 21205 USA

[2] UNIV MARYLAND, SCH MED, BALTIMORE, MD 21201 USA

[3] GEORGETOWN UNIV, SCH MED, WASHINGTON, DC USA

来源：

EUROPEAN JOURNAL OF PHARMACOLOGY | 1995年 / 278卷 / 01期

关键词：

NICOTINIC ACETYLCHOLINE RECEPTOR; BRAIN IMAGING; ALZHEIMERS DISEASE;

D O I：

10.1016/0014-2999(95)00178-N

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

In vivo imaging of nicotinic acetylcholine receptors in brain has been hampered by lack of an adequate radioligand. In the present study, [H-3]epibatidine was administered to mice intravenously, and its time-course in brain regions and sensitivity to blockade by nicotinic drugs were studied. The distribution of radioligand accumulation in brain, and the pharmacological characteristics of binding indicate that radiolabeled forms of epibatidine would be exceptionally promising ligands for the study of nicotinic acetylcholine receptors in vivo.

引用

页码：R1 / R2

页数：2

共 7 条

[1]

Badio, Daly, Epibatidine, a potent analgetic and nicotinic agonist, Mol. Pharmacol., 45, (1994)

[2]

Broussolle, Wong, Fanelli, London, In vivo specific binding of [3H]l-nicotine in the mouse brain, Life Sci., 44, (1989)

[3]

Flesher, Scheffel, London, Frost, In vivo labeling of nicotinic cholinergic receptors in brain with [3H]cytisine, Life Sci., 54, (1994)

[4]

Houghtling, Davilla-Garcia, Hurt, Kellar, [3H]Epibatidine binding to nicotinic cholinergic receptors in brain, Med. Chem. Res., 4, (1994)

[5]

London, Waller, Wamsley, Autoradiographic localization of [3H]nicotine binding sites in the rat brain, Neurosci. Lett., 53, (1985)

[6]

Nyback, Nordberg, Langstrom, Halldin, Hartvig, Ahlin, Swan, Sedvall, Attempts to visualize nicotinic receptors in the brain of monkey and man by positron emission tomography, Prog. Brain Res., 79, (1989)

[7]

Sargent, The diversity of neuronal nicotinic acetylcholine receptors, Annu. Rev. Neurosci., 16, (1993)

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