Specific [3H]LY278584 binding to 5-HT3 recognition sites in rat cerebral cortex

Wong, David T.; Robertson, David W.; Reid, Leroy R.

doi:10.1016/0014-2999(89)90689-4

Cited by 70 publications

(33 citation statements)

References 7 publications

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“…ICS 205,930 is a potent antagonist to the 5-HT 3 receptor and also possesses affinity for the 5-HT 4 receptor (Jin et al, 1999). However, LY278-584 is a highly selective 5-HT 3 receptor antagonist with little apparent affinity for other 5-HT receptors (Wong et al, 1989), suggesting that local 5-HT 4 receptors are not involved in the effects of ICS 205,930. In addition, ICS 205,930 was reported to have affinity for the GABA A receptor (Klein et al, 1994).…”

Section: Icsa Of Etoh Andmentioning

confidence: 99%

Synergistic Self-Administration of Ethanol and Cocaine Directly into the Posterior Ventral Tegmental Area: Involvement of Serotonin-3 Receptors

Ding¹,

Oster²,

Hauser³

et al. 2012

The Journal of Pharmacology and Experimental Therapeutics

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Ethanol (EtOH) and cocaine are both self-administered into the posterior ventral tegmental area (VTA). Self-administration of either drug is prevented by coadministration of a serotonin (5-HT 3 ) receptor antagonist. Electrophysiological studies indicated that cocaine and EtOH can act synergistically to stimulate VTA dopamine neurons. The current experiment assessed whether cocaine and EtOH would synergistically interact to produce a reinforcing action within the posterior VTA. Adult female Wistar rats were randomly assigned to one of 13 groups. There were three control groups: artificial cerebrospinal fluid (aCSF), a subthreshold EtOH (100 mg%) group, and a subthreshold cocaine (25 pmol/100 nl) group. The other groups self-administered 50 or 75 mg% EtOH containing 6.25, 12.5, or 25 pmol/100 nl cocaine or 100 mg% EtOH containing 3.12, 6.25, 12.5, or 25 pmol/100 nl cocaine. All rats received the assigned infusate for sessions 1 through 4, aCSF alone in sessions 5 and 6, and the original infusate during session 7. The effects of adding a 5-HT 3 receptor antagonist [tropisetron, C 17 pmol/100 nl) were determined. Rats failed to self-administer aCSF or the subthreshold concentration of EtOH or cocaine. All three concentrations of EtOH (50, 75, and 100 mg%) combined with cocaine (12.5 and 25 pmol/100 nl) supported self-administration. Adding a 5HT 3 receptor antagonist attenuated coadministration of EtOH ϩ cocaine. Overall, the data indicate that the reinforcing properties of EtOH and cocaine interacted synergistically within the posterior VTA, and these synergistic effects were mediated, at least in part, by activation of local 5-HT 3 receptors.

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Section: Icsa Of Etoh Andmentioning

confidence: 99%

Synergistic Self-Administration of Ethanol and Cocaine Directly into the Posterior Ventral Tegmental Area: Involvement of Serotonin-3 Receptors

Ding¹,

Oster²,

Hauser³

et al. 2012

The Journal of Pharmacology and Experimental Therapeutics

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“…Neijt et al, 1988) and both peripheral and central tissues (e.g. Kilpatrick et al, 1987;Peroutka & Hamik, 1988;Waeber et al, 1988;Watling et al, 1988;Barnes et al, 1988;Nelson & Thomas, 1989;Pinkus et al, 1989;Wong et al, 1989;Bolanos et al, 1990;Robertson et al, 1990;Sharif et al, 1991). Highest densities within the brain are associated with the dorsal vagal complex (comprising area postrema, nucleus tractus solitarius and dorsal motor nucleus of the vagus nerve; for review see Pratt et al, 1990), limbic (e.g., amygdala, hippocampus) and cortical areas (e.g.…”

Section: Introductionmentioning

confidence: 99%

Agonist interactions with 5‐HT₃ receptor recognition sites in the rat entorhinal cortex labelled by structurally diverse radioligands

Barnes

Costall

et al. 1992

British J Pharmacology

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“…However, their presence in the CNS was only recently described (Kilpatrick et al, 1987), a discovery that was facilitated by the development of several 5-HT3 receptor antagonists. They have subsequently been characterized extensively in rat brain using a variety of radioligands, including [3H]quipazine (Peroutka and Hamik, 1988), [,-lH-indole-3-carboxylic acid ester] (Watling et al, 1988), [, [endo-N-(9-methyl-9-azabicyclo[3.3.1]-non-3-y1)-1 -methylindazole-3-carboxamide] (Nelson and Thomas, 1989), [3H]zacopride (Barnes et al, 1989), and [3H]LY278584 [ l-methyl-N(8-methyl-8-azabicyclo [ 3.2.1 ] oct-3 -y1)-1 H-indazole-3 -carboxamide] (Wong et al, 1989).…”

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confidence: 99%

Pharmacological and Regional Characterization of [³H]LY278584 Binding Sites in Human Brain

Abi‐Dargham

Laruelle

Wong

et al. 1993

Journal of Neurochemistry

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Binding of [,H]LY278584, which has been previously shown to label 5-hydroxytryptamine3 (5-HT3) receptors in rat cortex, was studied in human brain. Saturation experiments revealed a homogeneous population of saturable binding sites in amygdala (KD = 3.08 t-0.67 nM, B,, = 1 I .86 -t I .87 fmol/mg of protein) as well as in hippocampus, caudate, and putamen. Specific binding was also high in nucleus accumbens and entorhinal cortex. Specific binding was negligible in neocortical areas. Kinetic studies conducted in human hippocampus revealed a KO,, of 0.025 t 0.009 nM-' min-' and a KO, of 0.010 k 0.002 min-'. 5-Hydroxytryptamine3 (5-HT3) receptors, originally called 5-HT M receptors, were first described by Gaddum and Picarelli (1957) in the guinea pig ileum as a subtype of 5-HT receptors that mediated depolarization of cholinergic nerves. They were later found in various other peripheral nervous system neurons, and renamed 5-HT3 receptors in the general classification of Bradley et al. (1986). However, their presence in the CNS was only recently described (Kilpatrick et al., 1987), a discovery that was facilitated by the development of several 5-HT3 receptor antagonists. They have subsequently been characterized extensively in rat brain using a variety of radioligands, including et al., 1989). In addition to these biochemical studies, 5-HT3 antagonism was shown to modulate mesolimbicdopaminergic activity in rodents. The peripheral and central administration of GR38032F, a potent and selective 5-HT3 antagonist, blocked the hyperlocomotion induced by intraaccumbens and intraamygdala administration of dopamine and amphetamine; there was no rebound hyperactivity on discontinuation of the 5- 730

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Specific [3H]LY278584 binding to 5-HT3 recognition sites in rat cerebral cortex

Cited by 70 publications

References 7 publications

Synergistic Self-Administration of Ethanol and Cocaine Directly into the Posterior Ventral Tegmental Area: Involvement of Serotonin-3 Receptors

Synergistic Self-Administration of Ethanol and Cocaine Directly into the Posterior Ventral Tegmental Area: Involvement of Serotonin-3 Receptors

Agonist interactions with 5‐HT₃ receptor recognition sites in the rat entorhinal cortex labelled by structurally diverse radioligands

Pharmacological and Regional Characterization of [³H]LY278584 Binding Sites in Human Brain

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Specific [3H]LY278584 binding to 5-HT3 recognition sites in rat cerebral cortex

Cited by 70 publications

References 7 publications

Synergistic Self-Administration of Ethanol and Cocaine Directly into the Posterior Ventral Tegmental Area: Involvement of Serotonin-3 Receptors

Synergistic Self-Administration of Ethanol and Cocaine Directly into the Posterior Ventral Tegmental Area: Involvement of Serotonin-3 Receptors

Agonist interactions with 5‐HT3 receptor recognition sites in the rat entorhinal cortex labelled by structurally diverse radioligands

Pharmacological and Regional Characterization of [3H]LY278584 Binding Sites in Human Brain

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Agonist interactions with 5‐HT₃ receptor recognition sites in the rat entorhinal cortex labelled by structurally diverse radioligands

Pharmacological and Regional Characterization of [³H]LY278584 Binding Sites in Human Brain