The 5-HT3 receptor (5-HT3R) is part of a superfamily of ligand-gated ion channels which includes nicotinic acetylcholine receptors (nAChR). cRNA derived from the long isoform cloned mouse 5-HT3R was used to drive expression of 5-HT3Rs in Xenopus oocytes. 5-HT-induced currents were monitored using two-electrode voltage-clamp. Eight nicotinic agonists, including ACh and nicotine, but not alpha-anatoxin, were found to antagonize 5-HT-induced currents. With the exception of 3-(2,4)-dimethoxybenzylidene-anabaseine (DMXB-anabaseine; GTS-21) this antagonism appeared to be competitive since it could be overcome by increasing concentrations of 5-HT. Potency of 5-HT3 antagonism was comparable to reported values for nAChR alpha7 activation. These results confirm the notion of families of receptors and further indicate that strong similarities can exist in some critical binding domains.
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http://dx.doi.org/10.1016/s0304-3940(98)00306-1 | DOI Listing |
Cochrane Database Syst Rev
January 2025
Department of Health Promotion and Policy, University of Massachusetts, Amherst, MA, USA.
Background: Electronic cigarettes (ECs) are handheld electronic vaping devices that produce an aerosol by heating an e-liquid. People who smoke, healthcare providers, and regulators want to know if ECs can help people quit smoking, and if they are safe to use for this purpose. This is a review update conducted as part of a living systematic review.
View Article and Find Full Text PDFExpert Opin Drug Discov
January 2025
Centro de Investigación en Reproducción Animal, Universidad Autónoma de Tlaxcala - CINVESTAV Tlaxcala, Tlaxcala, México.
Introduction: Existing pharmacotherapies for schizophrenia have not progressed beyond targeting dopamine and serotonin neurotransmission. Rodent models of schizophrenia are a necessary tool for elucidating neuropathological processes and testing potential pharmacotherapies, but positive preclinical results in rodent models often do not translate to positive results in the clinic.
Areas Covered: The authors reviewed PubMed for studies that applied rodent behavioral models of schizophrenia to assess the antipsychotic potential of several novel pharmacotherapies currently under investigation.
Neurochem Res
January 2025
Neurosciences Research Center, Tabriz University of Medical Sciences, Tabriz, Iran.
Alzheimer's disease (AD) is the most prevalent neurodegenerative disorder characterized by cognitive decline. Despite extensive research, therapeutic options remain limited. Varenicline, an αβ nicotinic acetylcholine receptor agonist, shows promise in enhancing cognitive function.
View Article and Find Full Text PDFChirality
February 2025
Daicel Chiral Technologies, West Chester, Pennsylvania, USA.
The influence of additives and modifiers on the chiral HPLC separation of the nicotine enantiomers using UV/Vis detection is discussed. Selected alcohols as modifiers and selected amines as additives were found to have a significant effect on the resolution and retention times of nicotine enantiomers even to the point of eliminating component elution. Systematic variations in the concentration of ethanol, methanol, and isopropanol, as modifiers, along with variations in the concentration of diethylamine, triethylamine, tributylamine, ethylenediamine, isopropylamine, as additives, revealed that the average resolution (R) of the nicotine enantiomers ranged from 2.
View Article and Find Full Text PDFInt J Environ Res Public Health
December 2024
Centre for Behavioural Research in Cancer, Cancer Council Victoria, Melbourne, VIC 3002, Australia.
Cigarette brand variant names and characteristics such as the taste and feel of the smoke can mislead consumers into believing some products are less harmful. We assessed the characteristics of three common cigarette variants sold in Australia, "gold", "blue" and "red", to determine which characteristics differed by color, and which affected tar, nicotine and carbon monoxide (TNCO) yields. TNCO yields, physical parameters, expanded tobacco and filter ventilation were measured in cigarette color variants from eight brands.
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