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 influence of ethanol on 5-hydroxytryptamine (5-HT)-induced tachycardia mediated by 5-HT3 receptor activation in the isolated guinea-pig atrium was studied. Ethanol at 200 mM significantly inhibited 5-HT - but not isoproterenol- or histamine-induced tachycardia in the isolated guinea-pig atrium. The same inhibitory effect was observed in response to 2-propanol and chloral hydrate application. Both 2-propanol at 100 mM and chloral hydrate at 1 mM exhibited inhibitory effects on 5-HT -induced tachycardia as potent as those of ethanol at 200 mM. These alcohols did not inhibit the tachycardia induced by isoproterenol or histamine. The inhibitory effects of the alcohols seemed to be specific for 5-HT and to increase according to their lipophilicity. Our results suggest that the inhibitory effects of ethanol on 5-HT3 receptor-mediated tachycardia are related to the direct effect of ethanol on 5-HT3 receptors in the atrium.
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PMID:Inhibitory effect of ethanol on the 5-HT3 receptor-mediated tachycardia in isolated guinea-pig atrium. 908 82

A static headspace gas chromatographic method is developed and evaluated for the quantitation of residual 2-propanol, methanol, and toluene in bulk (2alpha, 6alpha, 8alpha, 9alpha beta)-octahydro-3-oxo-2,6-methanon-2H-quinolizin-8-yl-1H-indole-3-caboxylate methanesufonate hydrate, a serotonin 5-HT3 receptor antagonist drug compound. This method is accurate and precise, and it includes the use of 1-propanol as an internal standard. The gas chromatographic conditions utilize a dimethylpolysiloxane phase (SPB-1) capillary column and a flame ionization detector. Validation of this test method includes a recovery study of known levels of the three target analyte solvents to verify the accuracy of this method, because these solvents were used in the recrystallization and synthesis of all current and future lots of the bulk drug. The tested range is 0.05% to 1.0% (w/w) for 2-propanol and methanol and 0.01% to 0.10% (w/w) for toluene. Mean recovery of all spikes is 107% (w/w) of theory for methanol (n = 15) and 101% (w/w) for 2-propanol. Toluene mean recovery of all spikes is 98% (w/w) of theory within the tested range (n = 6). These data and other facets of the development of this headspace method are discussed.
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PMID:Evaluation of a headspace-GC method for residual solvents in a serotonin 5-HT3 antagonist compound. 1849 43