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pubmed-article:9029495pubmed:abstractText5-HT3 receptor-mediated ion currents evoked by the full agonists 5-hydroxy-tryptamine (5-HT), quaternary 5-HT (5-HTQ), meta-chlorophenylbiguanide (mCPBG) and the partial agonists dopamine and tryptamine have been investigated in whole-cell voltage clamp experiments on N1E-115 mouse neuroblastoma cells. All agonists desensitize the 5-HT3 receptor completely with a steep concentration dependence and a potency order of: mCPBG > 5-HTQ approximately 5-HT > > tryptamine > dopamine. The time course of recovery from desensitization depends on the agonist used. Recovery from partial agonist-induced desensitization is single exponential, whereas the desensitization induced by full agonists recovers with sigmoid kinetics, suggesting at least 3 transitions between 4 states. It is concluded that full and partial agonists induce distinct desensitized states.lld:pubmed
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pubmed-article:9029495pubmed:articleTitleFull and partial agonists induce distinct desensitized states of the 5-HT3 receptor.lld:pubmed
pubmed-article:9029495pubmed:affiliationResearch Institute of Toxicology, Utrecht University, The Netherlands.lld:pubmed
pubmed-article:9029495pubmed:publicationTypeJournal Articlelld:pubmed
pubmed-article:9029495pubmed:publicationTypeResearch Support, Non-U.S. Gov'tlld:pubmed