Access the full text.
Sign up today, get DeepDyve free for 14 days.
COSTALL (1987)
Effects of the 5-HT3 receptor antagonist, GR38032F, on raised dopaminergic activity in the mesolimbic system of the rat and marmoset brainBr. J. Pharmacol., 92
PETERS (1990)
Antagonism of 5HT3 receptor mediated currents in murine N1E-115 neuroblastoma cells by (+)-tubocurarineNeurosci. Lett., 119
RICHARDSON (1985)
Identification of serotonin M-receptor subtypes and their specific blockade by a new class of drugsNature, 316
FOZARD (1984)
MDL 72222, a potent and highly selective antagonist at neuronal 5-hydroxytryptamine receptorsNaunyn-Schmiedebergs Arch. Pharmacol., 326
LAMBERT (1989)
The properties of 5-HT3 receptors in clonal cell lines studies by patch-clamp techniquesBr. J. Pharmacol., 97
FAKE (1987)
BRL 43694: a potent and novel 5-HT3 receptor antagonistBr. J. Pharmacol., 91
MICHEL (1984)
Analysis of ligand binding data using a microcomputerBr. J. Pharmacol., 83
YAKEL (1988)
5-HT3 receptors mediate rapid responses in cultured hippocampus and a clonal cell lineNeuron, 1
SCHMDIT (1989)
‘[3H]quipazine’ degradation products label 5-HT uptake sitesEur. J. Pharmacol., 171
RICHARDSON (1986)
The pharmacology and function of 5-HT3 receptorsTrends Neurosci., 7
MILBURN (1989)
Characterization of [3H]quipazine binding to 5-hydroxytryptamine3 receptors in rat brain membranesJ. Neurochem., 52
SMITH
Zacopride, a potent 5-HT3 antagonistJ. Pharm. Pharmacol., 40
HIGGINS (1989)
5-HT3 receptor antagonists injected into the area postrema inhibit cisplatin-induced emesis in the ferretBr. J. Pharmacol., 97
SANGER (1987)
Increased gut cholinergic activity and antagonism of 5-hydroxytryptamine M-receptors by BRL 24924: potential clinical importance of BRL 24924Br. J. Pharmacol., 91
HOYER (1988)
Identification of serotonin 5HT3 recognition sites in membranes of N1E-115 neuroblastoma cells by radioligand bindingMol. Pharmacol., 33
NELSON (1989)
[3H]-BRL 43694 (Graniesetron), a specific ligand for 5-HT3 binding sites in rat brain cortical membranesBiochem. Pharmacol., 38
KILPATRICK (1989)
The distribution of specific binding of the 5-HT3 receptor ligand [3H]GR65630 in rat brain using quantitative autoradiographyNeurosci. Lett., 94
PERRY (1990)
Autoradiography of [3H]quipazine in rodent brainEur. J. Pharmacol., 187
CHENG (1973)
Relationship between inhibition constant (Ki) and the concentration of inhibitor which causes 50 percent inhibition (IC50) of an enzymatic reactionBiochem. Pharmacol., 22
BRADFORD (1976)
A rapid and sensitive method for the quantification of microgram quantities of protein utilizing the principle of protein-dye bindingAnal. Biochem., 72
MUNSON (1980)
LIGAND: a versatile computerized approach for characterization of ligand systemsAnal Biochem., 107
ROUND (1986)
The depolarising action of 5-hydroxytryptamine on rabbit vagal afferent and sympathetic neurones in vitro and its selective blockade by ICS 205-930Br. J. Pharmacol., 88
SHARIF (1990)
Pharmacological characterization of 5HT3 receptors in rat cerebral cortex, NG108-15 and NCB-20 neuroblastoma cells using [3H]quipazine bindingEur. J. Pharmacol., 183
WAEBER (1988)
Localisation by autoradiography of neuronal 5-HT3 receptors in the mouse CNSEur. J. Pharmacol., 151
MARCUSSON (1988)
Characterization of [3H]paroxetine binding in rat brainJ. Neurochem., 50
BARNES (1989a)
5-HT3 receptors mediate inhibition of acetylcholine release in cortical tissueNature, 338
BRADLEY (1986)
Proposals for the classification and nomenclature of functional receptors for 5-hydroxytryptamineNeuropharmacology, 25
BARNES (1988)
[3H]Zacopride: A ligand for the identification of 5HT3 recognition sitesJ. Pharm. Pharmacol., 40
WATLING (1988)
[3H]Quaternised ICS 205-930 labels 5-HT3 receptor binding sites in rat brainEur. J. Pharmacol., 149
WAEBER (1989)
5-Hydroxytryptamine3 receptors in the human brain: autoradiographic visualization using [3H]ICS 205-930Neuroscience, 31
BUTLER (1990)
The pharmacological characterization of 5-HT3 receptors in three isolated preparations derived from guinea-pig tissuesBr. J. Pharmacol., 101
COSTALL (1990)
Sites of action of ondansetron to inhibit withdrawal from drugs of abusePharmacol. Biochem. Behaviour, 36
NEIJT (1988b)
Characterisation of 5-HT3 recognition sites in membranes of NG108-15 neuroblastoma-glioma cells with [3H]ICS 205-930Naunyn-Schmidebergs Arch. Pharmacol., 337
CUNNINGHAM (1987)
Prevention of emesis in patients receiving cytotoxic drugs by GR 38032F, a selective 5-HT3 receptor antagonistLancet, i
JONES (1988)
The potential anxiolytic activity of GR38032F, a 5-HT3 receptor antagonistBr. J. Pharmacol., 93
BLANDINA (1988)
Activation of a 5-HT3 receptor releases dopamine from rat striatal slicesEur. J. Pharmacol., 155
KILPATRICK (1987)
Identification and distribution of 5HT3 receptors in rat brain using radioligand bindingNature, 330
BUTLER (1988)
Pharmacological properties of GR 38032F, a novel antagonist at 5HT3 receptorsBr. J. Pharmacol., 94
PINKUS (1990)
Antagonism of [3H]zacopride binding to 5-HT3 recognition sites by its (R) and (S) enantiomersEur. J. Pharmacol., 179
WONG (1989)
Specific [3H]LY278584 binding to 5-HT3 recognition sites in rat cerebral cortexEur. J. Pharmacol., 166
BARNES (1989b)
Identification and characterization of 5-hydroxytryptamine3 recognition sites in human brain tissueJ. Neurochem., 53
IRELAND (1987)
Pharmacological characterization of 5-hydroxytryptamine-induced depolarization of the rat isolated vagus nerveBr. J. Pharmacol., 90
LUMMIS (1990)
Target size of 5-HT3 receptors in N1E-115 neuroblastoma cells and brainEur. J. Pharmacol. (Mol. Pharmacol. Section), 189
NEIJT (1988a)
Pharmacological characterization of serotonin 5-HT3 receptor mediated electrical response in cultured mouse neuroblastoma cellsNeuropharmacology, 27
PEROUTKA (1988)
Species variations in 5-HT3 recognition sites labeled by [3H]-quipazine in the central nervous systemNaunyn-Schmiedebergs Arch. Pharmacol., 338
1 The biochemical and pharmacological properties of 5‐HT3 receptors in homogenates of NG108‐15 and NCB‐20 neuroblastoma cells and rat cerebral cortex have been ascertained by the use of (3H)‐quipazine and (3H)‐GR65630 binding. 2 In NG108‐15 and NCB‐20 cell homogenates, (3H)‐quipazine bound to a single class of high affinity (NG108‐15: Kd = 6.2 ± 1.1 nm, n = 4; NCB‐20: Kd = 3.0 ± 0.9 nm, n = 4; means ± s.e.means) saturable (NG108‐15: Bmax = 1340 ± 220 fmol mg−1 protein; NCB‐20: Bmax = 2300 ± 200 fmol mg−1 protein) binding sites. In rat cortical homogenates, (3H)‐quipazine bound to two populations of binding sites in the absence of the 5‐hydroxytryptamine (5‐HT) uptake inhibitor, paroxetine (Kd1 = 1.6 ± 0.5 nm, Bmax1 = 75 ± 14 fmol mg−1 protein; Kd2 = 500 ± 300 nm, Bmax2 = 1840 ± 1040 fmol mg−1 protein, n = 3), and to a single class of high affinity binding sites (Kd = 2.0 ± 0.5 nm, n = 3; Bmax = 73 ± 6 fmol mg−1 protein) in the presence of paroxetine. The high affinity (nanomolar) component probably represented 5‐HT3 binding sites and the low affinity component represented 5‐HT uptake sites. 3 (3H)‐paroxetine bound with high affinity (Kd = 0.02 ± 0.003 nm, n = 3) to a site in rat cortical homogenates in a saturable (Bmax = 323 ± 45 fmol mg−1 protein, n = 3) and reversible manner. Binding to this site was potently inhibited by 5‐HT uptake blockers such as paroxetine and fluoxetine (pKi s = 8.6–9.9), while 5‐HT3 receptor ligands exhibited only low affinity (pKi < 7). No detectable specific (3H)‐paroxetine binding was observed in NG108‐15 or NCB‐20 cell homogenates. 4 (3H)‐quipazine binding to homogenates of NG108‐15, NCB‐20 cells and rat cortex (in the presence of 0.1 μm paroxetine) exhibited similar pharmacological characteristics. 5‐HT3 receptor antagonists competed for (3H)‐quipazine binding with high nanomolar affinities in the three preparations and the rank order of affinity was: (S)‐zacopride > quarternized ICS 205–930 ≥ granisetron > ondansetron > ICS 205–209 ≥ (R)‐zacopride > quipazine > renzapride > MDL‐72222 > butanopride > metoclopramide. 5 (3H)‐GR65630 labelled a site in NCB‐20 cell homogenates with an affinity (Kd = 0.7 ± 0.1 nm, n = 4) and density (Bmax = 1800 ± 1000 fmol mg−1 protein) comparable to that observed with (3H)‐quipazine. Competition studies also indicated a good correlation between the pharmacology of 5‐HT3 binding sites when (3H)‐GR65630 and (3H)‐quipazine were used in these cells. 6 In conclusion, (3H)‐quipazine labelled 5‐HT3 receptor sites in homogenates of NG108‐15 cells, NCB‐20 cells and rat cerebral cortex. In rat cortical homogenates, (3H)‐quipazine also bound to 5‐HT uptake sites, which could be blocked by 0.1 μm paroxetine. The pharmacological specificity of the 5‐HT3 receptor labelled by (3H)‐quipazine was similar in the neuroblastoma cells and rat cortex and was substantiated in NCB‐20 cells by the binding profile of the selective 5‐HT3 receptor antagonist, (3H)‐GR65630.
British Journal of Pharmacology – Wiley
Published: Apr 1, 1991
Read and print from thousands of top scholarly journals.
Already have an account? Log in
Bookmark this article. You can see your Bookmarks on your DeepDyve Library.
To save an article, log in first, or sign up for a DeepDyve account if you don’t already have one.
Copy and paste the desired citation format or use the link below to download a file formatted for EndNote
Access the full text.
Sign up today, get DeepDyve free for 14 days.
All DeepDyve websites use cookies to improve your online experience. They were placed on your computer when you launched this website. You can change your cookie settings through your browser.