Characterization of ZFOR1, a putative delta-opioid receptor from the teleost zebrafish ( Danio rerio)
ZFOR1 is a putative opioid receptor from zebrafish brain which has 66% homology with the mammalian δ-opioid receptor. When expressed in HEK293 cells ZFOR1 bound the non-selective opioid antagonist [ 3H]diprenorphine with high affinity. However, the binding of this ligand was not readily displaced by...
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Veröffentlicht in: | Neuroscience letters 2000-07, Vol.288 (3), p.207-210 |
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Sprache: | eng |
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Zusammenfassung: | ZFOR1 is a putative opioid receptor from zebrafish brain which has 66% homology with the mammalian δ-opioid receptor. When expressed in HEK293 cells ZFOR1 bound the non-selective opioid antagonist [
3H]diprenorphine with high affinity. However, the binding of this ligand was not readily displaced by opioids selective for μ, δ or κ opioid receptors (affinities>1000 nM). Rather non-selective ligands showed good affinity, as did the non-peptide δ-ligand BW373U86 (Ki 69 nM), the δ-antagonist naltrindole (Ki 28 nM) and the peptide β-endorphin (Ki 37 nM). Agonist binding to the receptor encoded by ZFOR1 receptor stimulated the binding of [
35S]GTPγS confirming coupling to G proteins. Study of the receptor should contribute to understanding of the evolution of the opioid system. |
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ISSN: | 0304-3940 1872-7972 |
DOI: | 10.1016/S0304-3940(00)01239-8 |