Click here to close
Hello! We notice that you are using Internet Explorer, which is not supported by Xenbase and may cause the site to display incorrectly.
We suggest using a current version of Chrome,
FireFox, or Safari.
Proc Natl Acad Sci U S A
1997 Mar 18;946:2715-8. doi: 10.1073/pnas.94.6.2715.
Show Gene links
Show Anatomy links
Irreversible antagonism of 5HT2c receptors by N-ethoxycarbonyl-2-ethoxy-1,2-dihydroquinoline (EEDQ).
Ni YG
,
Camacho N
,
Miledi R
.
???displayArticle.abstract???
To determine if N-ethoxycarbonyl-2-ethoxy-1,2-dihydroquinoline (EEDQ), a carboxyl group activating agent, can inactivate 5HT2c receptors, we have examined the effects of EEDQ on 5HT2c receptor-mediated responses to 5-hydroxytryptamine (5HT) in Xenopus oocytes, and on the binding of [3H]5HT to 5HT2c receptors in transfected HeLa cells. In oocytes expressing rat 5HT2c receptors, EEDQ inhibited the 5HT2c receptor-mediated Cl- currents; and the response did not recover more than 24 h after removal of the EEDQ. To see if this effect of EEDQ was on the receptor itself, the binding of 5HT to 5HT2c receptors was studied in transfected HeLa cells. EEDQ decreased the specific binding of [3H]5HT to 5HT2c receptors. At approximately 22 degrees C, incubating the membranes with 2 x 10(-4) M EEDQ for 1 h caused a 40% decrease in the Bmax, without changing the K(d). At 37 degrees C, the same treatment with EEDQ blocked [3H]5HT binding completely. Half-maximal inhibition occurred at 5 microM EEDQ at both temperatures, and washing for 1.5 h did not restore the binding, suggesting that the inactivation of 5HT2c receptor binding was practically irreversible. Results from both systems showed clearly that EEDQ is an irreversible antagonist of 5HT2c receptors and therefore can be used for many studies of this receptor.
Adham,
Receptor reserve masks partial agonist activity of drugs in a cloned rat 5-hydroxytryptamine1B receptor expression system.
1993, Pubmed
Adham,
Receptor reserve masks partial agonist activity of drugs in a cloned rat 5-hydroxytryptamine1B receptor expression system.
1993,
Pubmed
Adham,
Cell-specific coupling of the cloned human 5-HT1F receptor to multiple signal transduction pathways.
1993,
Pubmed
Aiyar,
Full-length and truncated Kv1.3 K+ channels are modulated by 5-HT1c receptor activation and independently by PKC.
1993,
Pubmed
,
Xenbase
Battaglia,
In vitro and in vivo irreversible blockade of cortical S2 serotonin receptors by N-ethoxycarbonyl-2-ethoxy-1,2-dihydroquinoline: a technique for investigating S2 serotonin receptor recovery.
1986,
Pubmed
Belleau,
The mechanism of irreversible adrenergic blockade by N-carbethoxydihydroquinolines--model studies with typical serine hydrolases.
1969,
Pubmed
Boess,
Molecular biology of 5-HT receptors.
1994,
Pubmed
Bradford,
A rapid and sensitive method for the quantitation of microgram quantities of protein utilizing the principle of protein-dye binding.
1976,
Pubmed
Conn,
A unique serotonin receptor in choroid plexus is linked to phosphatidylinositol turnover.
1986,
Pubmed
Gozlan,
Differential effects of N-ethoxycarbonyl-2-ethoxy-1,2-dihydroquinoline (EEDQ) on various 5-HT receptor binding sites in the rat brain.
1994,
Pubmed
Hess,
Differential modification of striatal D1 dopamine receptors and effector moieties by N-ethoxycarbonyl-2-ethoxy-1,2-dihydroquinoline in vivo and in vitro.
1987,
Pubmed
Julius,
Molecular characterization of a functional cDNA encoding the serotonin 1c receptor.
1988,
Pubmed
,
Xenbase
Kathmann,
Nordimaprit, homodimaprit, clobenpropit and imetit: affinities for H3 binding sites and potencies in a functional H3 receptor model.
1993,
Pubmed
Kaufman,
Serotonin 5-HT2C receptor stimulates cyclic GMP formation in choroid plexus.
1995,
Pubmed
Kusano,
Cholinergic and catecholaminergic receptors in the Xenopus oocyte membrane.
1982,
Pubmed
,
Xenbase
Mattera,
Guanine nucleotide regulation of a mammalian myocardial muscarinic receptor system. Evidence for homo- and heterotropic cooperativity in ligand binding analyzed by computer-assisted curve fitting.
1985,
Pubmed
Meller,
Inactivation of D1 and D2 dopamine receptors by N-ethoxycarbonyl-2-ethoxy-1,2-dihydroquinoline in vivo: selective protection by neuroleptics.
1985,
Pubmed
Meller,
Receptor reserve for 5-hydroxytryptamine1A-mediated inhibition of serotonin synthesis: possible relationship to anxiolytic properties of 5-hydroxytryptamine1A agonists.
1990,
Pubmed
Miledi,
A calcium-dependent transient outward current in Xenopus laevis oocytes.
1982,
Pubmed
,
Xenbase
Miledi,
Chloride current induced by injection of calcium into Xenopus oocytes.
1984,
Pubmed
,
Xenbase
Miledi,
Effects of defolliculation on membrane current responses of Xenopus oocytes.
1989,
Pubmed
,
Xenbase
Norman,
Effects of in vivo and in vitro treatments with N-ethoxycarbonyl-2-ethoxy-1,2-dihydroquinoline on putative muscarinic receptor subtypes in rat brain.
1986,
Pubmed
Panicker,
Receptors of the serotonin 1C subtype expressed from cloned DNA mediate the closing of K+ membrane channels encoded by brain mRNA.
1991,
Pubmed
,
Xenbase
Parker,
Inositol trisphosphate activates a voltage-dependent calcium influx in Xenopus oocytes.
1987,
Pubmed
,
Xenbase
Pinto,
In vivo EEDQ dose-dependently inactivates rat brain 5-HT receptors but not 5-HT uptake sites.
1993,
Pubmed
Sallés,
Modulation of the phospholipase C activity in rat brain cortical membranes by simultaneous activation of distinct monoaminergic and cholinergic muscarinic receptors.
1993,
Pubmed
Tigyi,
A serum factor that activates the phosphatidylinositol phosphate signaling system in Xenopus oocytes.
1990,
Pubmed
,
Xenbase
Woodward,
Angiotensin II receptors in Xenopus oocytes.
1991,
Pubmed
,
Xenbase