Radioligand

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A radioligand is a radioactive biochemical substance (in particular, a ligand) 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 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 radio ligand. The higher the affinity of the molecule the more radio ligand is displaced from the binding site and the increasing radioactive decay can be measured by scintillography. This assay is commonly used to calculate binding constants of molecules to receptors.

The transport of the radioligand is described by receptor kinetics.

1 History
2 Radioactive isotopes commonly used
3 List of radioligands
4 See also
5 References

[edit] History

Radioligands are acredited for 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.

[edit] Radioactive isotopes commonly used

Main article: Radioactivity in biology

Tritium, ³H
Carbon-14, ¹⁴C
Sulfur-35, ³⁵S
Iodine-131, ¹³¹I
Fluorine-18, ¹⁸F

In PET the isotopes fluorine-18 and carbon-11 are often used in molecular neuroimaging.

[edit] 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]

Please help improve this section by expanding it.
Further information might be found on the talk page or at requests for expansion.

[edit] See also

[edit] References

^ Niehoff, Debra (2005). The Language of Life: How cells communicate in life & disease. Joseph Henry Press. ISBN 0309089891.
^ 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.; et al. (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.. 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.
^ 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]" (in French). Revue Neurologique 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.