Dopamine agonist radioligand binds to both D2High and D2Low receptors, explaining why alterations in D2High are not detected in human brain scans

Synapse

Volumn 66, Issue 1, 2012, Pages 88-93

  Seeman, Philip ^a  

^a UNIVERSITY OF TORONTO   (Canada)

Author keywords

Addiction; Dopamine D2 receptor; Dopamine supersensitivity; Schizophrenia; Striatum

Indexed keywords

4 PROPYL 3,4,4A,5,6,10B HEXAHYDRO 2H NAPHTHO[1,2 B][1,4]OXAZIN 9 OL H 3; DOMPERIDONE; DOMPERIDONE H 3; DOPAMINE 2 RECEPTOR; DOPAMINE RECEPTOR STIMULATING AGENT; RACLOPRIDE; RACLOPRIDE H 3; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; BINDING AFFINITY; CORPUS STRIATUM; DRUG PROTEIN BINDING; NONHUMAN; PRIORITY JOURNAL; RAT;

ANIMALS; BINDING, COMPETITIVE; CORPUS STRIATUM; DOPAMINE AGONISTS; HUMANS; PROTEIN BINDING; RADIOPHARMACEUTICALS; RATS; RATS, SPRAGUE-DAWLEY; RECEPTORS, DOPAMINE D2; TRITIUM;

EID: 81555213468     PISSN: 08874476     EISSN: 10982396     Source Type: Journal    
DOI: 10.1002/syn.20987     Document Type: Article

References (21)

1. Dean T, Linglart A, Mahon MJ, Bastepe M, Jüppner H, Potts JT Jr, Gardella TJ. 2006. Mechanisms of ligand binding to the parathyroid hormone (PTH)/PTH-related protein receptor: Selectivity of a modified PTH(1-15) radioligand for GalphaS-coupled receptor conformations. Endocrinol 20: 931-943.
2. George SR, Watanabe M, Di Paolo T, Falardeau P, Labrie F, Seeman P. 1985. The functional state of the dopamine receptor in the anterior pituitary is in the high-affinity form. Endocrinology 117: 690-697.
3. Graff-Guerrero A, Mizrahi R, Agid O, Marcon H, Barsoum P, Rusjan P, Wilson AA, Zipursky R, Kapur S. 2009. The dopamine D2 receptors in high-affinity state and D3 receptors in schizophrenia: A clinical [11C]-(+)-PHNO PET study. Neuropsycho-pharmacology 34: 1078-1086.
4. Hirvonen J, Hietala J. 2011. Dysfunctional brain networks and genetic risk for schizophrenia: Specific neurotransmitter systems. CNS Neurosci Ther 17: 89-96.
5. Kara E, Lin H, Strange PG. 2010. Co-operativity in agonist binding at the D2 dopamine receptor: Evidence from agonist dissociation kinetics. J Neurochem 112: 1442-1453.
6. Lieberman JA, Kane JM, Alvir J. 1987. Provocative tests with psychostimulant drugs in schizophrenia. Psychopharmacology (Berl) 91: 415-433.
7. Longer receptor has a high-affinity state and inhibits adenylyl cyclase. Brain Res Mol Brain Res 77: 281-284.
8. 3H]raclopride are indistinguishably inhibited by D2 agonists and antagonists ex vivo. Nucl Med Biol 35: 11-17.
9. 11C]-(+)-PHNO binding is unchanged in animal models displaying increased high-affinity states of the D2 receptor in vitro. Synapse 63: 998-1009.
10. 11C]raclopride in baboons. J Pharmacol Exp Ther 315: 80-90.
11. 11C]NPA PET study. Synapse. Jul 20. doi: 10.1002/syn.20970. [Epub ahead of print].
12. Richfield EK, Young AB, Penney JB. 1986. Properties of D2 dopamine receptor autoradiography: High percentage of high-affinity agonist sites and increased nucleotide sensitivity in tissue sections. Brain Res 383: 121-128.
13. High receptors. Synapse 61: 1013-1018.
14. Seeman P, Ulpian C, Larsen RD, Anderson PS. 1993. Dopamine receptors labelled by PHNO. Synapse 14: 254-262.
15. High states, implying many paths to psychosis. Proc Natl Acad Sci USA 102: 3513-3518.
16. high dopamine receptors. Synapse 60: 319-346.
17. 3H](+)PHNO. Synapse 61: 263-267.
18. Skinbjerg M, Namkung Y, Halldin C, Innis RB, Sibley DR. 2009. Pharmacological characterization of 2-methoxy-N-propylnorapomorphine's interactions with D2 and D3 dopamine receptors. Synapse 63: 462-475.
19. 2 dopamine receptors in the high-affinity state based on in vivo PET imaging and in vitro radioligand binding. Synapse 64: 699-703.
20. Skinbjerg M, Liow JS, Seneca N, Hong J, Lu S, Thorsell A, Heilig M, Pike VW, Halldin C, Sibley DR, Innis RB. 2010b. D2 dopamine receptor internalization prolongs the decrease of radioligand binding after amphetamine: a PET study in a receptor internalization-deficient mouse model. Neuroimage 50: 1402-1407.
21. Wu Y, Buranda T, Simons PC, Lopez GP, McIntire WE, Garrison JC, Prossnitz ER, Sklar LA. 2007. Rapid-mix flow cytometry measurements of subsecond regulation of G protein-coupled receptor ternary complex dynamics by guanine nucleotides. Anal Biochem 371: 10-20.