Modification of behavioral effects of 8-hydroxy-2-(di-n-propylamino)tetralin following chronic ethanol consumption in the rat: evidence for the involvement of 5-HT1A receptors in ethanol dependence

Kleven, Mark S.; Ybema, Caroline E.; Carilla, Elisabeth; Hamon, Michel; Koek, Wouter

doi:10.1016/0014-2999(95)00324-e

Cited by 28 publications

(12 citation statements)

References 33 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Roles for 5-HT systems in cocaine reward (or aversion) are also less than clear from current data (Cunningham and Callahan, 1991;Kleven et al, 1995;Rocha et al, 1997;Kleven and Koek, 1998;Lee and Kornetsky, 1998;Parsons et al, 1998;Shippenberg et al, 2000;Baker et al, 2001;SasakiAdams and Kelley, 2001). Homozygous SERT-KO mice display enhanced cocaine CPP that is increased even more in combined SERT/NET double-KO mice (Sora et al, 1998;Hall et al, 2002).…”

Section: Introductionmentioning

confidence: 91%

Regional Differences in Extracellular Dopamine and Serotonin Assessed by In Vivo Microdialysis in Mice Lacking Dopamine and/or Serotonin Transporters

Shen

Hagino

Kobayashi

et al. 2004

Neuropsychopharmacol

184

View full text Add to dashboard Cite

Cocaine conditioned place preference (CPP) is intact in dopamine transporter (DAT) knockout (KO) mice and enhanced in serotonin transporter (SERT) KO mice. However, cocaine CPP is eliminated in double-KO mice with no DAT and either no or one SERT gene copy. To help determine mechanisms underlying these effects, we now report examination of baselines and drug-induced changes of extracellular dopamine (DA ex ) and serotonin (5-HT ex ) levels in microdialysates from nucleus accumbens (NAc), caudate putamen (CPu), and prefrontal cortex (PFc) of wild-type, homozygous DAT-or SERT-KO and heterozygous or homozygous DAT/SERT double-KO mice, which are differentially rewarded by cocaine. Cocaine fails to increase DA ex in NAc of DAT-KO mice. By contrast, systemic cocaine enhances DA ex in both CPu and PFc of DAT-KO mice though local cocaine fails to affect DA ex in CPu. Adding SERT to DAT deletion attenuates the cocaine-induced DA ex increases found in CPu, but not those found in PFc. The selective SERT blocker fluoxetine increases DA ex in CPu of DAT-KO mice, while cocaine and the selective DAT blocker GBR12909 increase 5-HT ex in CPu of SERT-KO mice. These data provide evidence that (a) cocaine increases DA ex in PFc independently of DAT and that (b), in the absence of SERT, CPu levels of 5-HT ex can be increased by blocking DAT. Cocaine-induced alterations in CPu DA levels in DAT-, SERT-, and DAT/SERT double-KO mice appear to provide better correlations with cocaine CPP than cocaine-induced DA level alterations in NAc or PFc.

show abstract

Section: Introductionmentioning

confidence: 91%

Regional Differences in Extracellular Dopamine and Serotonin Assessed by In Vivo Microdialysis in Mice Lacking Dopamine and/or Serotonin Transporters

Shen

Hagino

Kobayashi

et al. 2004

Neuropsychopharmacol

184

View full text Add to dashboard Cite

show abstract

“…Previous studies have shown that the plasticity of 5-HT 1A receptor is regulated by many different factors: developmental exposure to drugs such as para-chlorophenylalanine (Whitaker- Azmitia et al, 1987), alcohol (Kleven et al, 1995), cocaine (Akbari et al, 1994), and steroids (Nishi and Azmitia, 1996). In the adult brain, there are fewer reports of receptor plasticity.…”

Section: Discussionmentioning

confidence: 97%

Agonist- and antagonist-induced plasticity of rat 5-HT1A receptor in hippocampal cell culture

Nishi

Azmitia

1999

Synapse

View full text Add to dashboard Cite

We examined the response and regulation of 5-HT1A receptor on hippocampal cultured fetal neurons grown in the absence of serotonin and steroids using three experimental designs: 1) functional response using an antibody against phosphorylated cyclic adenosine monophosphate response element binding protein (pCREB); 2) transcriptional regulation using in situ hybridization; and 3) translational expression using antipeptide 5-HT1A receptor antibody. Pretreatment of cultured hippocampal cells with the agonist 8-hydroxy-2-(di-N-propylamino)-tetralin (8-OH-DPAT) (10(-8) M) or ipsapirone (IPS) (10(-9) M) for 10 min blocked the forskolin-stimulated increase in pCREB immunoreactivity. In situ hybridization radioautography revealed that IPS (10(-9) M) decreased the 5-HT1A receptor mRNA expression (-33%) after a 24-h treatment. The decrease in 5-HT1A receptor mRNAwas accompanied by a change in protein immunoreactivity using a 5-HT1A receptor antipeptide antibody. Computer-assisted morphometric analyses showed a reduction in the 5-HT1A receptor immunoreactive (IR) intensity as compared to control 24 h after treatment with 8-OH-DPAT (10(-7)-10(-12) M) and IPS (10(-9) M). Thus, fetal hippocampal neurons have a functional 5-HT1A receptor that is downregulated at both the transcription and translation levels. In addition, we found increased 5-HT1A receptor-IR intensity (+17% approximately +39%) 24 h after treatment with the antagonist N-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-N-(2-pyridinyl) cyclohexane carboxamide (WAY 100635) (10(-7)-10(-12) M). Our results indicate that the 5-HT1A receptor is sensitive to both agonists (downregulation) and antagonists (upregulation) in hippocampal fetal neurons grown in the absence of serotonin and steroids.

show abstract

“…20 Rats were observed at two time points, centered at 15 and 60 min after the injection and each lasting 10 min. During a 10 min period, an animal was observed once every minute for 10 s and the presence (1) or absence (0) of LLR was recorded.…”

Section: Pharmacologymentioning

confidence: 99%

“…This compound was prepared in 50% yield as described for 3a using 18b as starting material. 5-Methyl-6-chloro-2-(1.3-dioxolan-2-yl)-pyridine (20). To a solution of 17 (5.49 g, 34.8 mmol) and anhydrous CHCl3 (200 mL) was added MnO2 (26 g, 300 mmol), and the suspension was stirred under reflux for 3 h. Insoluble materials were filtered off, and then the compound was purified on a short silica gel column.…”

Section: N-(3-chlorobenzoyl)-4-fluoro-4-(4-methylphenylsulfonyloxymetmentioning

confidence: 99%

“…The product was extracted twice with EtOAc, washed with diluted NH4OH and brine, dried, and concentrated under vacuum. The product was purified by flash chromatography, eluent hexanes-EtOAc (80: 20), to give 0.29 g of 3e (55%) as a pale yellow oil which crystallized on standing: mp 46-48°C; 1 …”

Section: N-(3-chlorobenzoyl)-4-fluoro-4-(4-methylphenylsulfonyloxymetmentioning

confidence: 99%

See 1 more Smart Citation

Novel Derivatives of 2-Pyridinemethylamine as Selective, Potent, and Orally Active Agonists at 5-HT_1A Receptors

et al. 1999

Self Cite

View full text Add to dashboard Cite

The aim of this work was to improve the oral bioavailability of a recently discovered, novel structural class of 5-HT 1A receptor agonists: aryl-{[4-(6-R-pyridin-2-ylmethyl)-amino]-methyl}-piperidin-1-yl-methanone. Incorporation of a fluorine atom in the -position to the amino function in the side chain led to analogues that exhibited, in general, enhanced and longlasting 5-HT 1A agonist activity in rats after oral administration. Location of the fluorine atom at the C-4 position of the piperidine ring was the most favorable, and among the various substituents tested, the ability of the fluorine was unique in improving the oral activity of this family of ligands. Thus, the derivatives 39, 46, and 61 bound with higher affinity and selectivity to 5-HT 1A receptors (versus dopaminergic D 2 and adrenergic R 1 receptors) and displayed more potent 5-HT 1A agonist activity in vitro and in vivo than their C-4 desfluoro analogues. To examine the relationship between the conformation of the pharmacophore and the level of agonistic activity of this type of ligand, we synthesized a series of 3-chloro-4-fluorophenyl-(4-fluoro-4{[(5-(H or CH 3 )-6-R-pyridin-2-ylmethyl)-amino]-methyl}-piperidin-1-yl-methanone derivatives and found that the combination of a 5-methyl and a 6-methylamino substituent on the pyridine ring synergistically affected their 5-HT 1A agonist properties. Thus, the 3-chloro-4-fluorophenyl-(4-fluoro-4{[(5-methyl-6-methylamino-pyridin-2-ylmethyl)-amino]-methyl}-piperidin-1-yl-methanone 40 behaved as a more potent 5-HT 1A receptor agonist in vitro and in vivo than its 5-unsubstituted analogue 38. The antidepressant potential of the lead compounds 40, 45, and 54 was examined by means of the forced swimming test (FST) in rats. The results indicated that, after a single oral administration, these compounds inhibited immobility in the FST more potently and more extensively than the clinically used antidepressant imipramine. Thus, 40, 45, and 54 are potent, orally active 5-HT 1A receptor agonists with marked antidepressant potential.

show abstract

Modification of behavioral effects of 8-hydroxy-2-(di-n-propylamino)tetralin following chronic ethanol consumption in the rat: evidence for the involvement of 5-HT1A receptors in ethanol dependence

Cited by 28 publications

References 33 publications

Regional Differences in Extracellular Dopamine and Serotonin Assessed by In Vivo Microdialysis in Mice Lacking Dopamine and/or Serotonin Transporters

Regional Differences in Extracellular Dopamine and Serotonin Assessed by In Vivo Microdialysis in Mice Lacking Dopamine and/or Serotonin Transporters

Agonist- and antagonist-induced plasticity of rat 5-HT1A receptor in hippocampal cell culture

Novel Derivatives of 2-Pyridinemethylamine as Selective, Potent, and Orally Active Agonists at 5-HT_1A Receptors

Contact Info

Product

Resources

About

Modification of behavioral effects of 8-hydroxy-2-(di-n-propylamino)tetralin following chronic ethanol consumption in the rat: evidence for the involvement of 5-HT1A receptors in ethanol dependence

Cited by 28 publications

References 33 publications

Regional Differences in Extracellular Dopamine and Serotonin Assessed by In Vivo Microdialysis in Mice Lacking Dopamine and/or Serotonin Transporters

Regional Differences in Extracellular Dopamine and Serotonin Assessed by In Vivo Microdialysis in Mice Lacking Dopamine and/or Serotonin Transporters

Agonist- and antagonist-induced plasticity of rat 5-HT1A receptor in hippocampal cell culture

Novel Derivatives of 2-Pyridinemethylamine as Selective, Potent, and Orally Active Agonists at 5-HT1A Receptors

Contact Info

Product

Resources

About

Novel Derivatives of 2-Pyridinemethylamine as Selective, Potent, and Orally Active Agonists at 5-HT_1A Receptors