 |
 Previous Article | Next Article 
Journal of Neuroscience, Vol 4, 1021-1033, Copyright © 1984 by Society for Neuroscience
Cholecystokinin receptors: biochemical demonstration and autoradiographical localization in rat brain and pancreas using [3H] cholecystokinin8 as radioligand
A Van Dijk, JG Richards, A Trzeciak, D Gillessen and H Mohler
Since cholecystokinin8 (CCK8) seems to be the physiological ligand of CCK
receptors in the brain, it would be the most suitable probe for the
characterization of CCK receptors in radioligand binding studies. [3H]CCK8
was synthetized with a specific radioactivity sufficient for the detection
of high affinity binding sites. [3H]CCK8 binds saturably and reversibly to
distinct sites in rat brain and pancreas with nanomolar affinity. While the
C-terminal tetrapeptide of CCK is the minimal structure required for
nanomolar affinity in the brain, the entire octapeptide sequence is
required for binding affinity in pancreas. Desulfated CCK8 and several
gastrin-I peptides, which are likewise unsulfated, show virtually no
affinity to the binding sites in pancreas but high affinity in cerebral
cortex. The ligand specificity of the CCK peptides corresponds to their
electrophysiological potency in the brain and their stimulation of
secretion in pancreas, respectively. Autoradiographically, high densities
of [3H]CCK8 binding sites were found in cerebral cortex and olfactory bulb,
medium levels in nucleus accumbens, hippocampus, dentate gyrus, and
striatum with virtually no labeling in cerebellum. This pattern is similar
to the distribution of CCK-like immunoreactivity in the brain. In pancreas,
equally high levels of [3H]CCK8 labeling were found in the exocrine and
endocrine region. [3H]CCK8 binding sites differ from those identified
previously with [125I]Bolton-Hunter-CCK33 by their sensitivity to guanyl
nucleotides in the brain, their ion dependency in the brain, and pancreas,
and their different autoradiographical localization in some parts of the
brain. The distribution of CCK binding sites labeled with [3H]CCK8 appears
to correlate better with the CCK immunoreactivity than those labeled with
[125I]Bolton-Hunter-CCK33. Thus, [3H]CCK8 appears to be the radioligand of
choice for the investigation of CCK receptors.
This article has been cited by other articles:
|
|
|
|
 
G. E. Haley and F. W. Flynn
Tachykinin neurokinin 3 receptor signaling in cholecystokinin-elicited release of oxytocin and vasopressin
Am J Physiol Regulatory Integrative Comp Physiol,
May 1, 2008;
294(5):
R1760 - R1767.
[Abstract]
[Full Text]
[PDF]
|
|
|
|
|
|
|
C.-M. Lo, L. C. Samuelson, J. B. Chambers, A. King, J. Heiman, R. J. Jandacek, R. R. Sakai, S. C. Benoit, H. E. Raybould, S. C. Woods, et al.
Characterization of mice lacking the gene for cholecystokinin
Am J Physiol Regulatory Integrative Comp Physiol,
March 1, 2008;
294(3):
R803 - R810.
[Abstract]
[Full Text]
[PDF]
|
|
|
|
|
|
|
P.-Y. Deng and S. Lei
Bidirectional modulation of GABAergic transmission by cholecystokinin in hippocampal dentate gyrus granule cells of juvenile rats
J. Physiol.,
April 15, 2006;
572(2):
425 - 442.
[Abstract]
[Full Text]
[PDF]
|
|
|
|
|
|
|
S. B. Kombian, K. V. V. Ananthalakshmi, S. S. Parvathy, and W. C. Matowe
Cholecystokinin activates CCKB receptors to excite cells and depress EPSCs in the rat rostral nucleus accumbens in vitro
J. Physiol.,
February 15, 2004;
555(1):
71 - 84.
[Abstract]
[Full Text]
[PDF]
|
|
|
|
|
|
|
F. Noble, S. A. Wank, J. N. Crawley, J. Bradwejn, K. B. Seroogy, M. Hamon, and B. P. Roques
International Union of Pharmacology. XXI. Structure, Distribution, and Functions of Cholecystokinin Receptors
Pharmacol. Rev.,
December 1, 1999;
51(4):
745 - 781.
[Abstract]
[Full Text]
[PDF]
|
|
|
|
|
|
|
Z.-B. You, T. M. Tzschentke, E. Brodin, and R. A. Wise
Electrical Stimulation of the Prefrontal Cortex Increases Cholecystokinin, Glutamate, and Dopamine Release in the Nucleus Accumbens: an In Vivo Microdialysis Study in Freely Moving Rats
J. Neurosci.,
August 15, 1998;
18(16):
6492 - 6500.
[Abstract]
[Full Text]
[PDF]
|
|
|
|
|
|
|
A. A. Fossa, M. J. Depasquale, J. Morrone, S. H. Zorn, D. Bryce, J. A. Lowe, and S. McLean
Cardiovascular Effects of Cholecystokinin-4 Are Mediated By the Cholecystokinin-B Receptor Subtype In the Conscious Guinea Pig and Dog
J. Pharmacol. Exp. Ther.,
April 1, 1997;
281(1):
180 - 187.
[Abstract]
[Full Text]
|
|
|
|
|
|
|
J. Bradwejn, D. Koszycki, A. C. du Tertre, M. Bourin, R. Palmour, and F. Ervin
The cholecystokinin hypothesis of panic and anxiety disorders: a review
J Psychopharmacol,
January 1, 1992;
6(3):
345 - 351.
[Abstract]
[PDF]
|
|
|
|
|
|
|
A.J. Stoessl
Peptide-dopamine interactions in the central nervous system: implications for neuropsychiatric disorders
J Psychopharmacol,
January 1, 1989;
3(2):
99 - 120.
[PDF]
|
|
|
|
