Abstract:
:Melatonin binding sites were examined in the quail eye using 2-[125]iodomelatonin. Radioreceptor assays indicated similar binding sites in membrane preparations of neural retina (NR) and choroid-retinal pigment epithelium (C-RPE) eye components. In both tissues binding of the radioligand was specific, saturable, and of high affinity [Kd values NR 50.8 +/- 19.5 pM, C-RPE 98.2 +/- 35.4 pM, mean +/- SEM (n = 4)] and low capacity (Bmax values NR 12.4 +/- 2.7 fmol/mg protein, C-RPE 21.5 +/- 3.2 fmol/mg protein). Kinetic studies demonstrated that association of 2-[125I]iodomelatonin was rapid and further that this binding was reversible upon the addition of 1 microM melatonin. The order of pharmacological potencies of various indoles tested in 2-[125I]iodomelatonin displacement studies was melatonin > 6-chloromelatonin > 6-hydroxymelatonin > N-acetylserotonin > 5-methoxytryptophol > 5-hydroxytryptamine > 5-methoxytryptamine (5-hydroxytryptamine > 5-methoxytryptophol for C-RPE). Studies with guanine nucleotides indicated that the signal transduction mechanism of the binding site may involve a G-protein linkage. This melatonin binding site displays several pharmacological similarities with those investigated in the retina of other species and with those previously characterised in the quail brain.
journal_name
Gen Comp Endocrinoljournal_title
General and comparative endocrinologyauthors
James K,Skene DJ,Lucini V,Stankov B,Arendt Jdoi
10.1006/gcen.1995.1148subject
Has Abstractpub_date
1995-11-01 00:00:00pages
188-96issue
2eissn
0016-6480issn
1095-6840pii
S0016-6480(85)71148-3journal_volume
100pub_type
杂志文章abstract::Plasma concentrations of growth hormone (GH) were decreased following the intravenous administration of morphine sulfate. Maximum inhibition of GH secretion was observed 40 min after morphine sulfate challenge. At this time, doses of morphine sulfate (at 5 mg and 50 mg/kg) reduced the GH concentrations by 86 and 90%, ...
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journal_title:General and comparative endocrinology
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