The in vitro binding of dopaminergic ligands to dopamine D-2 receptors is inhibited by ACTH/MSH-like peptides

Florijn, Wouter J.; Boer, Thijs de; Tonnaer, J. A. D. M.; Nispen, J. W. van; Versteeg, Dirk H.G.

doi:10.1016/0014-2999(90)94537-8

Cited by 1 publication

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“…Discrepancies between the functional state of the receptors and the number of receptors measured (with ligand-binding studies in supersensitization) demonstrate once again that one should be careful in interpreting results from in vivo scanning. ACTH-(I-24) and especially ACTH-(8-16)NH2 inhibited the binding of 3H-N-propyl-norapomorphine and 3H-spiperone to the dopamine D2 receptor in the striatum, septum and pituitary in the rat (Florijn et al 1990). However, ACTH-(4-9) increased apomorphine supersensitivity 2 weeks after a lesion of the striatum in the rat, as measured by testing rotational behaviour in a small open field (Vos et al 1990).…”

Section: Supersensitizationmentioning

confidence: 99%

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Pharmacological implications for neuroreceptor imaging

Verhoeff¹

1991

Eur J Nucl Med

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Neuroreceptor imaging is increasing in nuclear medicine. New generations of radioligands will be developed that will allow us to study neurotransmitter systems not studied before. In data interpretation, however, links will have to be made with the number of counts acquired in the image and the real radioactivity in the brain and then, via the specific activity (and known metabolic characteristics), with the concentration of the ligand. From this point, links will have to be made, via kinetic modelling, with receptor density and, if possible, with receptor affinity, with the final link with brain function at a neurophysiological level. In this article several properties of receptor pharmacology and function are discussed that might help with the interpretation. It is argued that there is a complex relationship between the data, as is apparent in the images recorded and the underlying pharmacology of the receptor. Caution should be exercised, however, when in drawing conclusions about the receptor status and the possible implications on pathophysiology.

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Section: Supersensitizationmentioning

confidence: 99%

“…It has already been mentioned for D2 receptors that a hormonally caused decrease in receptor binding may be paradoxically accompanied by increased receptor sensitivity to agonists (Cameron and Crocker 1990;Florijn et al 1990;Vos et al 1990).…”

Section: Interaction Between Neurotransmitters and Hormonesmentioning

confidence: 99%

Pharmacological implications for neuroreceptor imaging

Verhoeff¹

1991

Eur J Nucl Med

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The in vitro binding of dopaminergic ligands to dopamine D-2 receptors is inhibited by ACTH/MSH-like peptides

Cited by 1 publication

References 0 publications

Pharmacological implications for neuroreceptor imaging

Pharmacological implications for neuroreceptor imaging

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