[3H]7-OH-DPAT is capable of labeling dopamine D2 as well as D3 receptors
| Autor: | David R. Sibley, Antonio M. Gonzalez |
|---|---|
| Rok vydání: | 1995 |
| Předmět: |
endocrine system
Tetrahydronaphthalenes Stereochemistry Guanine CHO Cells Binding Competitive Receptors Dopamine chemistry.chemical_compound Cricetulus Dopamine receptor D3 Cricetinae Dopamine receptor D2 polycyclic compounds Animals Receptor Pharmacology 7-OH-DPAT biology Receptors Dopamine D2 musculoskeletal neural and ocular physiology Chinese hamster ovary cell Receptors Dopamine D3 Brain biology.organism_classification Molecular biology Guanine Nucleotides Rats nervous system chemistry Spiperone Cell culture Dopamine Agonists |
| Zdroj: | European Journal of Pharmacology. 272:R1-R3 |
| ISSN: | 0014-2999 |
| Popis: | The binding of [3H](+)-7-hydroxy-2-(N,N-di-n-propylamino)tetralin ([3H]7-OH-DPAT) to dopamine D2 and D3 receptors expressed in Chinese hamster ovary (CHO) cells was investigated and compared with [3H]methylspiperone. [3H]7-OH-DPAT labeled the D3 receptor in the CHO cells in a guanine nucleotide-insensitive fashion and exhibited a Kd of about 0.5 nM. In the presence of MgCl2. [3H]7-OH-DPAT was also found to label the D2 receptor in CHO cells with high affinity (3.6 nM). The binding of [3H]7-OH-DPAT to the D2 receptor was sensitive to guanine nucleotides suggesting occupancy of a high affinity G protein-coupled state of the receptor. These results suggest that caution should be exercised when using [3H]7-OH-DPAT to label the dopamine D3 receptor in brain tissues. |
| Databáze: | OpenAIRE |
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