| 词条 | Radioligand |
| 释义 |
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. HistoryRadioligands 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|Radioactivity in biology}}
In PET the isotopes fluorine-18, carbon-11, and copper-64 are often used in molecular imaging. List of radioligands{{main|List of PET radiotracers}}Radioligands may be constructed to bind selectively to a particular neuroreceptor or a particular neurotransmitter transporter. Examples of radioligands include:
See also
References1. ^{{Cite book | last = Niehoff | first = Debra | authorlink = Debra Niehoff | title = The Language of Life: How cells communicate in life & disease | year = 2005 | isbn = 0-309-08989-1 | publisher = Joseph Henry Press}} 2. ^{{Cite journal | author = Wong, Dean F. | title = Localization of serotonin 5-HT2 receptors in living human brain by positron emission tomography using N1-([11C]-methyl)-2-bromo-LSD | journal = Synapse | year = 1987 | volume = 1 | issue = 5 | pages = 393–398. | pmid = 2905532 | doi = 10.1002/syn.890010502 | last2 = Lever | first2 = John R. | last3 = Hartig | first3 = Paul R. | last4 = Dannals | first4 = Robert F. | last5 = Villemagne | first5 = Victor | last6 = Hoffman | first6 = Beth J. | last7 = Wilson | first7 = Alan A. | last8 = Ravert | first8 = Hayden T. | last9 = Links | first9 = Jonathan M. }} 3. ^{{Cite journal | author = 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 | title = A database of [18F]-altanserin binding to 5-HT2A receptors in normal volunteers: normative data and relationship to physiological and demographic variables | journal = NeuroImage | volume = 21 | issue = 3 | pages = 1105–1113 |date=March 2004 | issn = 1053-8119 | doi = 10.1016/j.neuroimage.2003.10.046 | pmid = 15006678}} 4. ^{{Cite journal |author1=J. C. Baron |author2=Y. Samson |author3=D. Comar |author4=C. Crouzel |author5=P. Deniker |author6=Y. Agid | title = 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] | language = French | year = 1985 | journal = Revue neurologique | volume = 141 | issue = 8–9 | pages = 537–545 | pmid = 2935920}} 5. ^{{cite journal|author=Reimold M|title=Reduced availability of serotonin transporters in obsessive-compulsive disorder correlates with symptom severity - a [11C]DASB PET study|journal=J Neural Transm|volume=114|issue=12|pages=1603–9|year=2007|pmid=17713719|doi=10.1007/s00702-007-0785-6|name-list-format=vanc|author2=Smolka MN|author3=Zimmer A|display-authors=3|last4=Batra|first4=A.|last5=Knobel|first5=A.|last6=Solbach|first6=C.|last7=Mundt|first7=A.|last8=Smoltczyk|first8=H. U.|last9=Goldman|first9=D.}} 6. ^{{cite journal|author=Pertwee RG|title=Pharmacology of cannabinoid receptor ligands|journal=Curr. Med. Chem.|volume=6|issue=8|pages=635–64|year=1999|pmid=10469884|doi=}} 7. ^{{Cite journal | author = Alexander Hammers, Matthias J. Koepp, Mark P. Richardson, Rene Hurlemann, David J. Brooks & John S. Duncan | title = Grey and white matter flumazenil binding in neocortical epilepsy with normal MRI. A PET study of 44 patients | journal = Brain | volume = 126 | issue = Pt 6 | pages = 1300–1308 |date=June 2003 | pmid = 12764053 | url = http://brain.oxfordjournals.org/cgi/content/abstract/126/6/1300 | doi = 10.1093/brain/awg138}} 8. ^{{Cite journal |vauthors=Seeman P, Ulpian C, Larsen RD, Anderson PS |title = Dopamine receptors labelled by PHNO |journal = Synapse | volume = 14 | issue = 4 | pages = 254–262 |date=August 1993 | pmid = 7902615 | doi = 10.1002/syn.890140403 | url = http://www3.interscience.wiley.com/journal/109702957/abstract}}{{dead link|date=February 2019|bot=medic}}{{cbignore|bot=medic}} 9. ^{{Cite journal |author1=Volkow ND |author2=Wang GJ |author3=Fowler JS |author4=Logan J |author5=Franceschi D |author6=Maynard L |author7=Ding YS |author8=Gatley SJ |author9=Gifford A |author10=Zhu W |author11=Swanson JM. |title = Relationship between blockade of dopamine transporters by oral methylphenidate and the increases in extracellular dopamine: therapeutic implications |journal = Synapse | volume = 43 | issue = 3 | pages = 181–187 |date=March 2002 | pmid = 11793423 | doi = 10.1002/syn.10038}} Further reading
| author = John Charles Matthews | title = Fundamentals of Receptor, Enzyme, and Transport Kinetics | publisher = CRC Press | year = 1993 | isbn = 0-8493-4426-3 }} 3 : Biochemistry methods|Biomolecules|Receptors |
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