放射リガンドアッセイ
- 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
PrepTutorEJDIC
- (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)
Wikipedia preview
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)
[Wiki en表示]
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.
Contents
- 1 History
- 2 Radioactive isotopes commonly used
- 3 List of radioligands
- 4 See also
- 5 References
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
Main article: Radioactivity in biology
- 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
Main article: List of PET radiotracers
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-HT1A receptor
- N(1)-([11C]-methyl)-2-Br-LSD ([11C]-MBL) for 5-HT2 receptors[2]
- 18F-altanserin and 18F-setoperone for the 5-HT2A 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 GABAA receptors.[7]
- (+)PHNO for D2 dopamine receptors.[8]
- [11C]raclopride for D2 dopamine receptors.[9]
See also
- Binding potential
- Distribution volume
- PET radiotracer
- Radioactivity in biology
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-HT2A 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.
Further reading
- John Charles Matthews (1993). Fundamentals of Receptor, Enzyme, and Transport Kinetics. CRC Press. ISBN 0-8493-4426-3.
UpToDate Contents
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English Journal
- Design and synthesis of fluorescent ligands for the detection of cannabinoid type 2 receptor (CB2R).
- Spinelli F, Giampietro R, Stefanachi A, Riganti C, Kopecka J, Abatematteo FS, Leonetti F, Colabufo NA, Mangiatordi GF, Nicolotti O, Perrone MG, Brea J, Loza MI, Infantino V, Abate C, Contino M.
- European journal of medicinal chemistry. 2020 Feb;188()112037.
- The Cannabinoid 2 receptor, CB2R, belonging to the endocannabinoid system, ECS, is involved in the first steps of neurodegeneration and cancer evolution and progression and thus its modulation may be exploited in the therapeutic and diagnostic fields. However, CB2Rs distribution and signaling pathwa
- PMID 31954990
- Affinity, binding kinetics and functional characterization of draflazine analogues for human equilibrative nucleoside transporter 1 (SLC29A1).
- Vlachodimou A, Konstantinopoulou K, IJzerman AP, Heitman LH.
- Biochemical pharmacology. 2020 Feb;172()113747.
- In the last decade it has been recapitulated that receptor-ligand binding kinetics is a relevant additional parameter in drug discovery to improve in vivo drug efficacy and safety. The equilibrative nucleoside transporter-1 (ENT1, SLC29A1) is an important drug target, as transporter inhibition is a
- PMID 31830468
- Autoimmunity plays a role in the onset of diabetes after 40 years of age.
- Rolandsson O, Hampe CS, Sharp SJ, Ardanaz E, Boeing H, Fagherazzi G, Mancini FR, Nilsson PM, Overvad K, Chirlaque MD, Dorronsoro M, Gunter MJ, Kaaks R, Key TJ, Khaw KT, Krogh V, Kühn T, Palli D, Panico S, Sacerdote C, Sánchez MJ, Severi G, Spijkerman AMW, Tumino R, van der Schouw YT, Riboli E, Forouhi NG, Langenberg C, Wareham NJ.
- Diabetologia. 2020 Feb;63(2)266-277.
- Type 1 and type 2 diabetes differ with respect to pathophysiological factors such as beta cell function, insulin resistance and phenotypic appearance, but there may be overlap between the two forms of diabetes. However, there are relatively few prospective studies that have characterised the relatio
- PMID 31713011
Japanese Journal
- Muscarinic Receptor Binding in Rat Bladder Urothelium and Detrusor Muscle by Intravesical Solifenacin
- Novel enzyme-linked immunosorbent assay for bivalent ZnT8 autoantibodies
- Endothelin-1 Receptors in Rat Tissues: Characterization by Bosentan, Ambrisentan and CI-1020
Related Links
- 1. Methods Mol Biol. 2012;897:31-77. doi: 10.1007/978-1-61779-909-9_3. Radioligand binding assays and their analysis. Maguire JJ(1), Kuc RE, Davenport AP. Author information: (1)Clinical Pharmacology Unit ...
- Radioligand assay synonyms, Radioligand assay pronunciation, Radioligand assay translation, English dictionary definition of Radioligand assay. n. 1. a. Qualitative or quantitative analysis of a metal or ore to determine its ? A A ...
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★リンクテーブル★
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- 英
- radioligand assay
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- ラジオレセプターアッセイ
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- 関
- anal、analyse、analyses、analysis、analytical、analyze、determination、determine、dissect、method、method for measurement、-metry、quantitative determination、statistical method、test
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- 関
- radioactive ligand