関: radioreceptor assay

WordNet

a quantitative or qualitative test of a substance (especially an ore or a drug) to determine its components; frequently used to test for the presence or concentration of infectious agents or antibodies etc.
analyze (chemical substances)
a substance that is undergoing an analysis of its components
an appraisal of the state of affairs; "they made an assay of the contents"; "a check on its dependability under stress" (同)check
a written report of the results of an analysis of the composition of some substance
hardy and sure-footed animal smaller and with longer ears than the horse
a pompous fool

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(金属の品質・鉱石の金属含有量・薬品の)分析,試金 / 試金物,分析物 / …'を'試金する,分析する
ロバ / ばか者
《米俗》しり,けつ(《英俗》arse)

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2016/02/25 00:59:06」(JST)

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A radioligand is a radioactive biochemical substance (in particular, a ligand that is radiolabeled) that is used for diagnosis or for research-oriented study of the receptor systems of the body.

In a neuroimaging application the radioligand is injected into the pertinent tissue, or infused into the bloodstream. It binds to its receptor. When the radioactive isotope in the ligand decays it can be measured by positron emission tomography (PET) or single photon emission computed tomography (SPECT). In in vivo systems it is often used to quantify the binding of a test molecule to the binding site of radioligand. The higher the affinity of the molecule the more radioligand is displaced from the binding site and the increasing radioactive decay can be measured by scintillography. This assay is commonly used to calculate binding constant of molecules to receptors.

The transport of the radioligand is described by receptor kinetics.

History

Radioligands are credited with making possible the study of biomolecular behaviour, a previously mysterious area of research that had evaded researchers.^[1] With this capacity radioligand techniques enabled researchers to identify receptor devices within cells.

Radioactive isotopes commonly used

Tritium, ³H
Carbon-14, ¹⁴C
Sulfur-35, ³⁵S
Iodine-131, ¹³¹I
Fluorine-18, ¹⁸F
Technetium-99m, ^99mTc
Copper-64, ⁶⁴Cu

In PET the isotopes fluorine-18, carbon-11, and copper-64 are often used in molecular imaging.

List of radioligands

Radioligands may be constructed to bind selectively to a particular neuroreceptor or a particular neurotransmitter transporter. Examples of radioligands include:

¹¹C-WAY-100635 for the 5-HT_1A receptor
N(1)-([¹¹C]-methyl)-2-Br-LSD ([¹¹C]-MBL) for 5-HT2 receptors^[2]
¹⁸F-altanserin and ¹⁸F-setoperone for the 5-HT_2A receptor^[3]
¹¹C-ketanserin^[4] and tritiated ketanserin
¹¹C-DASB for the serotonin transporter^[5]
³H-WIN55,212-2 for cannabinoid receptors^[6]
[¹¹C]flumazenil for GABA_A receptors.^[7]
(+)PHNO for D₂ dopamine receptors.^[8]
[¹¹C]raclopride for D₂ dopamine receptors.^[9]

References

^ Niehoff, Debra (2005). The Language of Life: How cells communicate in life & disease. Joseph Henry Press. ISBN 0-309-08989-1.
^ Wong, Dean F.; Lever, John R.; Hartig, Paul R.; Dannals, Robert F.; Villemagne, Victor; Hoffman, Beth J.; Wilson, Alan A.; Ravert, Hayden T.; Links, Jonathan M. (1987). "Localization of serotonin 5-HT2 receptors in living human brain by positron emission tomography using N1-([11C]-methyl)-2-bromo-LSD". Synapse 1 (5): 393–398. doi:10.1002/syn.890010502. PMID 2905532.
^ Karen H. Adams, Lars H. Pinborg, Claus Svarer, S. G. Hasselbalch, Søren Holm, Steven Haugbøl, K. Madsen, Vibe G. Frøkjær, L. Martiny Olaf B. Paulson, Gitte Moos Knudsen (March 2004). "A database of [¹⁸F]-altanserin binding to 5-HT_2A receptors in normal volunteers: normative data and relationship to physiological and demographic variables". NeuroImage 21 (3): 1105–1113. doi:10.1016/j.neuroimage.2003.10.046. ISSN 1053-8119. PMID 15006678.
^ J. C. Baron, Y. Samson, D. Comar, C. Crouzel, P. Deniker, Y. Agid (1985). "Etude in vivo des recepteurs serotoninergiques centraux chez l'homme par tomographie a positions. [In vivo study of central serotoninergic receptors in man using positron tomography]". Revue neurologique (in French) 141 (8–9): 537–545. PMID 2935920.
^ Reimold M, Smolka MN, Zimmer A, et al. (2007). "Reduced availability of serotonin transporters in obsessive-compulsive disorder correlates with symptom severity - a [11C]DASB PET study". J Neural Transm 114 (12): 1603–9. doi:10.1007/s00702-007-0785-6. PMID 17713719.
^ Pertwee RG (1999). "Pharmacology of cannabinoid receptor ligands". Curr. Med. Chem. 6 (8): 635–64. PMID 10469884.
^ Alexander Hammers, Matthias J. Koepp, Mark P. Richardson, Rene Hurlemann, David J. Brooks & John S. Duncan (June 2003). "Grey and white matter flumazenil binding in neocortical epilepsy with normal MRI. A PET study of 44 patients". Brain 126 (Pt 6): 1300–1308. doi:10.1093/brain/awg138. PMID 12764053.
^ Seeman P, Ulpian C, Larsen RD, Anderson PS (August 1993). "Dopamine receptors labelled by PHNO". Synapse 14 (4): 254–262. doi:10.1002/syn.890140403. PMID 7902615.
^ Volkow ND, Wang GJ, Fowler JS, Logan J, Franceschi D, Maynard L, Ding YS, Gatley SJ, Gifford A, Zhu W, Swanson JM. (March 2002). "Relationship between blockade of dopamine transporters by oral methylphenidate and the increases in extracellular dopamine: therapeutic implications". Synapse 43 (3): 181–187. doi:10.1002/syn.10038. PMID 11793423.

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