Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UNIPROT:P46098 (5-HT3 receptor)
 2,290 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

The effects of chlorpromazine and the lidocaine derivative QX222, which block nicotinic acetylcholine receptors, were examined on 5-HT3 receptors in N1E-115 mouse neuroblastoma cells, using whole cell voltage-clamp and radioligand binding. Electrophysiological studies examining the effects of chlorpromazine and QX222 on 5-HT3 agonist-induced responses revealed IC50s of 0.2 and 8.5 microM respectively. The action was not voltage- or use-dependent and there was no blocking action when chlorpromazine was applied from inside the cell. Chlorpromazine and QX222 inhibited the binding of a radiolabelled 5-HT3 receptor antagonist, [3H]GR65630, with IC50s of 0.9 and 29 microM respectively. Scatchard plots revealed a decrease in affinity (Kd) in the presence of chlorpromazine, but no change in the maximum number of binding sites (Bmax). The results suggest differential actions of the compounds at 5-HT3 and acetylcholine receptors.
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PMID:Chlorpromazine and QX222 block 5-HT3 receptors in N1E-115 neuroblastoma cells. 798 88

The effects of a range of phenothiazines were examined on 5-hydroxytryptamine3 (5-HT3) receptors in membranes from NIE-115 neuroblastoma cells using radioligand binding. Chlorpromazine, fluphenazine, perphenazine, trifluoperazine and prochlorperazine inhibited specific binding of both the 5-HT3 receptor antagonist [3H]GR65630 and agonist [3H]meta-chlorophenylbiguanide (mCPBG), with Ki values ranging from 0.4 to 3.9 microM. The mode of action of chlorpromazine was further examined using photoaffinity labelling in the presence and absence of 5-HT. Saturation radioligand binding data with both [3H]GR65630 and [3H]mCPBG showed that photoaffinity labelling with chlorpromazine (1 microM) caused a decrease in the maximum number of binding sites observed (35% and 28% for agonist and antagonist, respectively). This decrease was not observed when the membranes were incubated in the presence of 5-HT. The results demonstrate a direct interaction of a range of phenothiazines at the 5-HT3 receptor binding site.
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PMID:Radioligand binding and photoaffinity labelling studies show a direct interaction of phenothiazines at 5-HT3 receptors. 922 92